tylosin

别名: Fradizine; Tylocine; Tylosin; Tylosin A; Tilosina; Tylan; Vubityl 200. 泰乐菌素; 太乐菌素; 泰乐霉素; 泰洛霉素; 泰洛星; 泰乐菌素标准品; 泰乐菌素 EP标准品; 泰乐菌素D; 泰乐菌素D EP标准品; 泰乐菌素-D3; 泰乐菌素标准品; 亦称泰农; 泰乐菌素碱; 亦称泰农、泰乐霉素;TYLOSIN 泰乐菌素
目录号: V3559 纯度: ≥98%
泰乐菌素(也称为 Fradizine、Tylocine、Tylosin A)是一种广谱抗生素和抑菌剂,针对革兰氏阳性菌和有限范围的革兰氏阴性菌。
tylosin CAS号: 1401-69-0
产品类别: Bacterial
产品仅用于科学研究,不针对患者销售
规格 价格 库存 数量
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of tylosin:

  • Tylvalosin tartrate (Acetylisovaleryltylosin tartrate)
  • 酒石酸泰洛星
  • 磷酸泰乐菌素
  • Tylosin-d3 (tylosin d3)
  • 3-O-Acetyltylosin-d3
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InvivoChem产品被CNS等顶刊论文引用
纯度/质量控制文件

纯度: ≥98%

产品描述
泰乐菌素(也称为 Fradizine、Tylocine、Tylosin A)是一种广谱抗生素,对革兰氏阳性菌和有限范围的革兰氏阴性菌具有抑菌作用。泰乐菌素作为弗拉迪链霉菌的发酵产物天然存在。它是一种大环内酯类抗生素。泰乐菌素在兽医学中用于治疗多种物种的细菌感染,并且具有很高的安全性。它还被用作某些物种的生长促进剂,以及伴侣动物结肠炎的治疗方法。
生物活性&实验参考方法
靶点
Macrolide
Bacterial 50S ribosomal subunit (binding to 23S rRNA nucleotides G748 and A2058) [1]
Bacterial ribosome (common binding site for veterinary macrolides, involved in protein synthesis inhibition) [3]
体外研究 (In Vitro)
泰乐菌素与细菌核糖体 50S 亚基的 23S rRNA 结合产生抗菌作用 [1]。
最低抑菌浓度 (MIC) 为 64 μg/mL、32 μg/mL、512 μg/mL 和 1 μg/mL泰乐菌素还分别抑制溶血性分枝杆菌 11935、多杀性分枝杆菌 4407、大肠杆菌 ATCC 25922 和大肠杆菌 AS19rlmAI 等革兰氏阴性菌株的生长[3]。
泰乐菌素(Tylosin) 的耐药性由23S rRNA核苷酸G748和A2058的单一甲基化协同作用赋予,单独任一甲基化均不足以产生耐药性。这种协同耐药机制对泰乐菌素(Tylosin) 和霉素霉素(mycinamycin)具有特异性(二者大环内酯环的5位和14位延伸有糖基),对碳霉素、螺旋霉素、红霉素等其他大环内酯类抗生素无此现象 [1]
- 浓度为0.2 g/L的泰乐菌素(Tylosin) 与犬粪便微生物群共孵育6小时后,可降低总挥发性脂肪酸含量和乳酸菌数量,增加梭菌属I群数量;在24小时孵育全程中,可升高pH值、亚精胺水平和大肠杆菌数量。当与1 g/L的益生元(FOS、GOS、XOS)联用时,益生元可抵消泰乐菌素(Tylosin) 的部分不良影响,如乳酸菌和梭菌属XIVa群数量的减少 [2]
- 泰乐菌素(Tylosin) 是16元大环内酯类兽医抗生素,通过结合核糖体抑制细菌蛋白质合成,与其他兽医大环内酯类抗生素(替地吡罗辛、替米考星、泰拉霉素)共享核糖体结合位点 [3]
体内研究 (In Vivo)
当给予泰乐菌素(10-500 mg/kg;皮下注射)时,用脂多糖(LPS)治疗的动物表现出 IL-10 增加,并且 TNF-α 和 IL-1β 水平升高普遍受到抑制[4]。
在健康小鼠中,10 mg/kg和100 mg/kg剂量的泰乐菌素(Tylosin) 不诱导细胞因子产生;500 mg/kg剂量对TNF-α和IL-1β的产生无影响,但可诱导IL-10产生 [4]
- 在脂多糖(LPS)处理的小鼠中,所有测试剂量的泰乐菌素(Tylosin)(10 mg/kg、100 mg/kg、500 mg/kg)均能降低升高的血清TNF-α和IL-1β水平,并升高IL-10水平,表现出免疫调节作用 [4]
酶活实验
甲基转移酶活性及耐药性验证实验:构建表达TlrB(靶向G748的甲基转移酶)和/或TlrD(靶向A2058的甲基转移酶)的细菌菌株,将菌株与相关浓度的泰乐菌素(Tylosin) 共孵育。测定泰乐菌素(Tylosin) 对各菌株的最低抑菌浓度(MIC),评估G748和A2058的单一或联合甲基化是否赋予耐药性;通过测试其他大环内酯类抗生素(碳霉素、螺旋霉素、红霉素、霉素霉素)验证该耐药机制的特异性 [1]
- 核糖体蛋白质合成抑制实验:分离细菌核糖体(如来自大肠杆菌或兽医致病菌溶血性曼海姆菌、多杀性巴氏杆菌),制备包含核糖体、mRNA、氨酰-tRNA及其他必需因子的无细胞蛋白质合成系统。向系统中加入泰乐菌素(Tylosin) 并在最适条件下孵育,通过监测目标蛋白质的合成(如放射性标记或荧光检测法),评估泰乐菌素(Tylosin) 对核糖体蛋白质合成的抑制作用 [3]
细胞实验
犬粪便微生物群体外孵育实验:收集健康成年犬粪便并制备粪便悬液,将悬液与体外消化后的干狗粮残渣在烧瓶中混合。设置8个处理组:对照组(无添加剂)、泰乐菌素(Tylosin) 组(0.2 g/L)、FOS组(1 g/L)、GOS组(1 g/L)、XOS组(1 g/L)、泰乐菌素(Tylosin) + FOS组、泰乐菌素(Tylosin) + GOS组、泰乐菌素(Tylosin) + XOS组(每组5个烧瓶)。将烧瓶置于39 °C厌氧培养箱中孵育,分别在6小时和24小时收集样本,分析微生物组成(log₁₀ copies DNA/ng DNA)和代谢参数(pH值、挥发性脂肪酸、生物胺)[2]
- 细菌蛋白质合成抑制细胞实验:在适宜的培养基中培养细菌细胞(如溶血性曼海姆菌、多杀性巴氏杆菌),加入梯度浓度的泰乐菌素(Tylosin) 并孵育特定时间。通过测定细菌蛋白质含量或检测特定蛋白质的表达,评估泰乐菌素(Tylosin) 对细菌蛋白质合成的抑制作用 [3]
动物实验
Animal Model: Balb/C mice (2-3 months old, 20-25 g)[4]
Dosage: 10 mg/kg, 100 mg/kg, 500 mg/kg
Administration: Subcutaneous injection
Result: raised the levels of IL-10 in mice treated with 250 µg of LPS, but decreased the elevated levels of TNF-α and IL-1β.
Mouse cytokine response assay: Divide mice into seven groups: positive control group (injected with LPS), and six treatment groups (10 mg/kg tylosin, 100 mg/kg tylosin, 500 mg/kg tylosin, 10 mg/kg tylosin + LPS, 100 mg/kg tylosin + LPS, 500 mg/kg tylosin + LPS). Administer tylosin and LPS concurrently via appropriate routes. Collect serum samples at 0, 1, 2, 3, 6, 12, and 24 hours after treatment. Determine serum TNF-α, IL-1β, and IL-10 levels using enzyme-linked immunosorbent assay (ELISA) [4]
药代性质 (ADME/PK)
Absorption, Distribution and Excretion
The pharmacokinetics and oral bioavailability of tylosin tartrate and tylosin phosphate were carried out in broiler chickens according to a principle of single dose, random, parallel design. The two formulations of tylosin were given orally and intravenously at a dose level of 10 mg/kg b.w to chicken after an overnight fasting (n = 10 chickens/group). Serial blood samples were collected at different time points up to 24 hr postdrug administration. A high performance liquid chromatography method was used for the determination of tylosin concentrations in chicken plasma. The tylosin plasma concentration's time plot of each chicken was analyzed by the 3P97 software. The pharmacokinetics of tylosin was best described by a one-compartmental open model 1st absorption after oral administration. After intravenous administration the pharmacokinetics of tylosin was best described by a two-compartmental open model, and there were no significant differences between tylosin tartrate and tylosin phosphate. After oral administration, there were significant differences in the Cmax (0.18 + or - 0.01, 0.44 + or - 0.09) and AUC (0.82 + or - 0.05, 1.57 + or - 0.25) between tylosin phosphate and tylosin tartrate. The calculated oral bioavailability (F) of tylosin tartrate and tylosin phosphate were 25.78% and 13.73%, respectively. Above all, we can reasonably conclude that, the absorption of tylosin tartrate is better than tylosin phosphate after oral administration.
/MILK/ The aim of this study is to determine the pharmacokinetics of tylosin and tilmicosin in serum and milk in healthy Holstein breed cows (n = 12) and reevaluate the amount of residue in milk. Following the intramuscular administration of tylosin, the maximum concentrations (C max) in serum and milk were found to be 1.30 + or - 0.24 and 4.55 + or - 0.23 ug/mL, the time required to reach the peak concentration (t max) was found to be 2nd and 4th hour, and elimination half-live were found to be 20.46 + or - 2.08 and 26.36 + or - 5.55 hour, respectively. Following the subcutaneous administration of tilmicosin, the C max in serum and milk were found to be 0.86 + or - 0.20 and 20.16 + or - 1.13 ug/mL, the t max was found to be 1st and 8th hr, and the elimination half life were found to be 29.94 + or - 6.65 and 43.02 + or - 5.18 hr, respectively. AUCmilk/AUCserum and C max-milk/C max-serum rates, which are indicators for determining the rate of drugs that pass into milk, were, respectively, calculated as 5.01 + or - 0.72 and 3.61 + or - 0.69 for tylosin and 23.91 + or - 6.38 and 20.16 + or - 1.13 for tilmicosin. In conclusion, it may be stated that milk concentration of tylosin after parenteral administration is higher than expected like tilmicosin and needs more withdrawal period for milk than reported.
Biological availability and pharmacokinetic properties of tylosin were determined in broiler chickens after oral and iv administration at a dose of 10 mg/kg. The calculated bioavailability--F%, by comparing AUC values--oral and AUC--iv, ranged from 30%-34%. After intravenous injection tylosin was rapidly distributed in the organism, showing elimination half-life values of 0.52 hr and distribution volume (Vd) of 0.69 L/kg, at a clearance rate (Cl) of 5.30 +/- 0.59 mL/min/kg. After oral administration, tylosin has a similar distribution volume (Vd = 0.85 L/kg), while the elimination half-life of 2.07 hr was four times bigger than after iv administration at Cl = 4.40 +/- 0.27 mL/min/kg. The obtained value tmax = 1.5 hr for tylosin after oral administration indicates that using this antibiotic with drinking water in broiler chickens is the method of choice. However, a relatively low value Cmax = 1.2 micrograms/ml after oral administration of tylosin shows that dosing of this antibiotic in broiler chickens should be higher than in other food producing animals.
/MILK/ Antibiotic residues in milk above tolerance levels interfere with dairy product processing and pose potential health risks to consumers. Residue avoidance programmes include, among other components, the observance of withdrawal times indicated in label instructions. Persistence of antibiotics in milk following treatment is influenced by drug, dosage, route of administration, body weight and mammary gland health status. Compositional changes that take place during intramammary infection (IMI) can affect antibiotic excretion in milk, thus modifying milk withdrawal time. The objectives of this study were to validate sensitivity and specificity of a qualitative microbiological method (Charm AIM-96) to detect tylosin in bovine composite milk and to determine the influence of subclinical IMI in tylosin excretion following intramuscular administration. For test validation, two groups of approximately 120 cows were used; one received a single intramuscular injection of tylosin tartrate at a dose of 20 mg/kg, while the other group remained as untreated control. Test sensitivity and specificity were 100% and 94.1% respectively. To determine the influence of subclinical IMI in tylosin excretion, two groups of seven cows, one with somatic cell counts (SCC) < or =250 000 cells/ml and the other with SCC > or =900 000, were administered a single intramuscular injection of tylosin tartrate at a dose of 20 mg/kg. Milk samples were obtained every 12 h for 10 days following treatment. Milk tylosin excretion averaged between 5 and 9 days for cows with low and high SCC respectively (P < 0.0001). Compositional changes in cows with high SCC most likely affect the pharmacokinetic characteristics of tylosin, extending the presence of the antibiotic in milk, thus influencing milk withdrawal times.
For more Absorption, Distribution and Excretion (Complete) data for TYLOSIN (10 total), please visit the HSDB record page.
Metabolism / Metabolites
The tylosin-biosynthetic (tyl) gene cluster of Streptomyces fradiae contains ancillary genes that encode functions normally associated with primary metabolism. These can be disrupted without loss of viability, since equivalent genes (presumably used for 'housekeeping' purposes) are also present elsewhere in the genome. The tyl cluster also contains two genes that encode products unlike any proteins in the databases. Two ancillary genes, metF (encoding N5,N10-methylenetetrahydrofolate reductase) and metK, encoding S-adenosylmethionine synthase, flank one of the 'unknown' genes (orf9) in the tyl cluster. In a strain of S. fradiae in which all three of these genes were disrupted, tylosin production was reduced, although this effect was obscured in media supplemented with glycine betaine which can donate methyl groups to the tetrahydrofolate pool. Apparently, one consequence of the recruitment of ancillary genes into the tyl cluster is enhanced capacity for transmethylation during secondary metabolism.
Studies on the susceptibility of pathogenic Nocardia to macrolide antibiotics, chalcomycin and tylosin, showed that most of the Nocardia species examined were highly resistant to both antibiotics, although N. nova was moderately susceptible. N. asteroides IFM 0339 converted these macrolides into inactive metabolites by glycosylation at 2'-OH or glycosylation and reduction of the 20-formyl group. The structures of the metabolites were determined from NMR and MS data to be 2'-[O-(beta-D-glucopyranosyl)]chalcomycin (2), 2'-[O-(beta-D-glucopyranosyl)]tylosin (5) and 20-dihydro-2'-[O-(beta-D-glucopyranosyl)]tylosin (4).
Tylosin is produced by Streptomyces fradiae via a combination of polyketide metabolism and synthesis of three deoxyhexose sugars, of which mycaminose is the first to be added to the polyketide aglycone, tylactone (protylonolide). Previously, disruption of the gene (tylMII) encoding attachment of mycaminose to the aglycone unexpectedly abolished accumulation of the latter, raising the possibility of a link between polyketide metabolism and deoxyhexose biosynthesis in S. fradiae. However, at that time, it was not possible to eliminate an alternative explanation, namely, that downstream effects on the expression of other genes, not involved in mycaminose metabolism, might have contributed to this phenomenon. Here, it is shown that disruption of any of the four genes (tylMI--III and tylB) specifically involved in mycaminose biosynthesis elicits a similar response, confirming that production of mycaminosyl-tylactone directly influences polyketide metabolism in S. fradiae. Under similar conditions, when mycaminose biosynthesis was specifically blocked by gene disruption, accumulation of tylactone could be restored by exogenous addition of glycosylated tylosin precursors. Moreover, certain other macrolides, not of the tylosin pathway, were also found to elicit qualitatively similar effects. Comparison of the structures of stimulatory macrolides will facilitate studies of the stimulatory mechanism.
Three glycosyltransferases are involved in tylosin biosynthesis in Streptomyces fradiae. The first sugar to be added to the polyketide aglycone (tylactone) is mycaminose and the gene encoding mycaminosyltransferase is orf2* (tylM2). However, targeted disruption of orf2* did not lead to the accumulation of tylactone under conditions that normally favor tylosin production; instead, the synthesis of tylactone was virtually abolished. This may, in part, have resulted from a polar effect on the expression of genes downstream of orf2*, particularly orf4* (ccr) which encodes crotonyl-CoA reductase, an enzyme that supplies 4-carbon extender units for polyketide metabolism. However, that cannot be the entire explanation, since tylosin production was restored at about 10% of the wild-type level when orf2* was re-introduced into the disrupted strain. When glycosylated precursors of tylosin were fed to the disrupted strain, they were converted to tylosin, confirming that two of the three glycosyltransferase activities associated with tylosin biosynthesis were still intact. Interestingly, however, tylactone also accumulated under such conditions and, to a much lesser extent, when tylosin was added to similar fermentations. It is concluded that glycosylated macrolides exert a pronounced positive effect on polyketide metabolism in S. fradiae.
For more Metabolism/Metabolites (Complete) data for TYLOSIN (6 total), please visit the HSDB record page.
Biological Half-Life
Biological availability and pharmacokinetic properties of tylosin were determined in broiler chickens after oral and iv administration at a dose of 10 mg/kg. ... After intravenous injection, tylosin ... /had an/ elimination half-life value of 0.52 .. . After oral administration, tylosin /had an / elimination half-life of 2.07 hr ... .
The elimination half-life of tylosin is reportedly 54 minutes in small animals, 139 minutes in newborn calves, and 64 minutes in calves 2 months of age or older.
参考文献

[1]. Resistance to the macrolide antibiotic tylosin is conferred by single methylations at 23S rRNA nucleotides G748 and A2058 acting in synergy. Proc Natl Acad Sci U S A. 2002 Nov 12; 99(23): 14658-14663.

[2]. In Vitro Evaluation of the Effects of Tylosin on the Composition and Metabolism of Canine Fecal Microbiota. Animals (Basel). 2020 Jan; 10(1): 98.

[3]. Inhibition of Protein Synthesis on the Ribosome by Tildipirosin Compared with Other Veterinary Macrolides. Antimicrob Agents Chemother. 2012 Nov; 56(11): 6033-6036.

[4]. Effects of tylosin on serum cytokine levels in healthy and lipopolysaccharide-treated mice. Acta Vet Hung. 2010 Mar;58(1):75-81.

其他信息
Tylosin is a macrolide antibiotic that is tylonolide having mono- and diglycosyl moieties attached to two of its hydroxy groups. It is found naturally as a fermentation product of Streptomyces fradiae. It has a role as a bacterial metabolite, an allergen, a xenobiotic and an environmental contaminant. It is an aldehyde, a disaccharide derivative, an enone, a leucomycin, a monosaccharide derivative and a macrolide antibiotic. It is functionally related to a tylactone. It is a conjugate base of a tylosin(1+).
Tylosin is a bacteriostatic macrolide antibiotic and feed additive used in veterinary medicine. It has a broad spectrum of activity against Gram-positive organisms and a limited range of Gram-negative organisms. Tylosin is produced as a fermentation product of Streptomyces fradiae.
Tylosin has been reported in Bos taurus, Streptomyces fradiae, and Streptomyces venezuelae with data available.
Macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.
See also: Tylosin Tartrate (has salt form); Tylosin Phosphate (has salt form); Monensin; Tylosin (component of) ... View More ...
Mechanism of Action
The inhibition of peptide bond formation by tylosin, a 16-membered ring macrolide, was studied in a model system derived from Escherichia coli. In this cell-free system, a peptide bond is formed between puromycin (acceptor substrate) and AcPhe-tRNA (donor substrate) bound at the P-site of poly(U)-programmed ribosomes. It is shown that tylosin inhibits puromycin reaction as a slow-binding, slowly reversible inhibitor. Detailed kinetic analysis reveals that tylosin (I) reacts rapidly with complex C, i.e., the AcPhe-tRNA. poly(U).70S ribosome complex, to form the encounter complex CI, which then undergoes a slow isomerization and is converted to a tight complex, CI, inactive toward puromycin. These events are described by the scheme C + I <==> (K(i)) CI <==> (k(4), k(5)) CI. The K(i), k(4), and k(5) values are equal to 3 microM, 1.5 min(-1), and 2.5 x 10(-3) min(-1), respectively. The extremely low value of k(5) implies that the inactivation of complex C by tylosin is almost irreversible. The irreversibility of the tylosin effect on peptide bond formation is significant for the interpretation of this antibiotic's therapeutic properties; it also renders the tylosin reaction a useful tool in the study of other macrolides failing to inhibit the puromycin reaction but competing with tylosin for common binding sites on the ribosome. Thus, the tylosin reaction, in conjunction with the puromycin reaction, was applied to investigate the erythromycin mode of action. It is shown that erythromycin (Er), like tylosin, interacts with complex C according to the kinetic scheme C + Er <==> (K(er)) CEr <==> (k(6), k(7)) C*Er and forms a tight complex, CEr, which remains active toward puromycin. The determination of K(er), k(6), and k(7) enables us to classify erythromycin as a slow-binding ligand of ribosomes
Tylosin is a macrolide antibiotic extensively used in veterinary medicine, exerting potent antimicrobial activity against Gram-positive bacteria [1]
- The producer strain Streptomyces fradiae protects itself from tylosin via differential expression of four resistance determinants: tlrA, tlrB, tlrC, and tlrD. TlrB and TlrD encode methyltransferases that target G748 and A2058 of 23S rRNA, respectively [1]
- Tylosin has a 16-membered macrolactone (tylonolide) ring and contains the 5-mycaminose amino sugar and mycarose sugar [3]
- Tylosin exhibits an immunomodulatory effect at the recommended dose for treating infections [4]
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C46H77NO17
分子量
916.1001
精确质量
915.519
元素分析
C, 60.31; H, 8.47; N, 1.53; O, 29.69
CAS号
1401-69-0
相关CAS号
Tylosin tartrate;74610-55-2;Tylosin phosphate;1405-53-4;Tylosin-d3
PubChem CID
5280440
外观&性状
White to light yellow solid powder
密度
1.2±0.1 g/cm3
沸点
980.7±65.0 °C at 760 mmHg
熔点
18-132ºC
闪点
546.9±34.3 °C
蒸汽压
0.0±0.6 mmHg at 25°C
折射率
1.549
LogP
3.27
tPSA
238.67
氢键供体(HBD)数目
5
氢键受体(HBA)数目
18
可旋转键数目(RBC)
13
重原子数目
64
分子复杂度/Complexity
1560
定义原子立体中心数目
21
SMILES
O1[C@]([H])(C([H])([H])[H])C([H])([C@@]([H])(C([H])(C1([H])OC1([H])C([H])(C([H])([H])[H])[C@@]([H])(C([H])([H])C(=O)OC([H])(C([H])([H])C([H])([H])[H])C([H])(C([H])=C(C([H])([H])[H])C([H])=C([H])C(C([H])(C([H])([H])[H])C([H])([H])[C@]1([H])C([H])([H])C([H])=O)=O)C([H])([H])OC1([H])C([H])([C@@]([H])(C([H])(C([H])(C([H])([H])[H])O1)O[H])OC([H])([H])[H])OC([H])([H])[H])O[H])O[H])N(C([H])([H])[H])C([H])([H])[H])OC1([H])C([H])([H])C(C([H])([H])[H])([C@]([H])([C@]([H])(C([H])([H])[H])O1)O[H])O[H] |c:45,52|
InChi Key
WBPYTXDJUQJLPQ-VMXQISHHSA-N
InChi Code
InChI=1S/C46H77NO17/c1-13-33-30(22-58-45-42(57-12)41(56-11)37(52)26(5)60-45)18-23(2)14-15-31(49)24(3)19-29(16-17-48)39(25(4)32(50)20-34(51)62-33)64-44-38(53)36(47(9)10)40(27(6)61-44)63-35-21-46(8,55)43(54)28(7)59-35/h14-15,17-18,24-30,32-33,35-45,50,52-55H,13,16,19-22H2,1-12H3/b15-14+,23-18+/t24-,25+,26-,27-,28+,29+,30-,32-,33-,35+,36-,37-,38-,39-,40-,41-,42-,43+,44+,45-,46-/m1/s1
化学名
2-((4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4R,5S,6R)-5-(((2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-16-ethyl-4-hydroxy-15-((((2R,3R,4R,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)methyl)-5,9,13-trimethyl-2,10-dioxooxacyclohexadeca-11,13-dien-7-yl)acetaldehyde
别名
Fradizine; Tylocine; Tylosin; Tylosin A; Tilosina; Tylan; Vubityl 200.
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
DMSO : ≥ 100 mg/mL (~109.16 mM)
H2O : ~0.67 mg/mL (~0.73 mM)
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 2.5 mg/mL (2.73 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。
*生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。

配方 2 中的溶解度: ≥ 2.5 mg/mL (2.73 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。
*20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (2.73 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。


请根据您的实验动物和给药方式选择适当的溶解配方/方案:
1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL;

3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果,工作液请现配现用!
6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 1 mg 5 mg 10 mg
1 mM 1.0916 mL 5.4579 mL 10.9158 mL
5 mM 0.2183 mL 1.0916 mL 2.1832 mL
10 mM 0.1092 mL 0.5458 mL 1.0916 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;

3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);

4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。

计算器

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度,具体如下:

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示:
假如化合物的分子量为350.26 g/mol,在5mL DMSO中制备10mM储备液所需的化合物的质量是多少?
  • 在分子量(MW)框中输入350.26
  • 在“浓度”框中输入10,然后选择正确的单位(mM)
  • 在“体积”框中输入5,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式,您可以计算体积和浓度。

稀释计算器可计算如何稀释已知浓度的储备液。例如,可以输入C1、C2和V2来计算V1,具体如下:

制备25毫升25μM溶液需要多少体积的10 mM储备溶液?
使用方程式C1V1=C2V2,其中C1=10mM,C2=25μM,V2=25 ml,V1未知:
  • 在C1框中输入10,然后选择正确的单位(mM)
  • 在C2框中输入25,然后选择正确的单位(μM)
  • 在V2框中输入25,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案62.5μL(0.1 ml)出现在V1框中
g/mol

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成,具体如下:

注:化学分子式大小写敏感:C12H18N3O4  c12h18n3o4
计算化合物摩尔质量(分子量)的说明:
  • 要计算化合物的分子量 (摩尔质量),请输入化学/分子式,然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义:
  • 分子质量(或分子量)是一种物质的一个分子的质量,用统一的原子质量单位(u)表示。(1u等于碳-12中一个原子质量的1/12)
  • 摩尔质量(摩尔重量)是一摩尔物质的质量,以g/mol表示。
/

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器(澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶/难溶于水的化合物),不同的产品和批次配方组成不同,如对配方有疑问,可先联系我们提供正确的体内实验配方。此外,请注意这只是一个配方计算器,而不是特定产品的确切配方。
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计算结果:

工作液浓度 mg/mL;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

生物数据图片
  • (A) Structures of the antibiotics used in this study. (B) Comparison of the structures of ribosome-bound tylosin obtained by crystallography (thick lines; ref. 52) and modeling (thin lines; this study). [1]. Proc Natl Acad Sci U S A. 2002 Nov 12; 99(23): 14658-14663.
  • (A) Stereoview of tylosin in its binding site. The figure is based on the crystal structure (52), in which key bases are substituted for those in the Escherichia and Streptomyces rRNA sequences. (B and C) Enlargement of the targets for TlrB and TlrD methyltransferases at nucleotides G748 and A2058, respectively, showing how methylation here impinges on tylosin's binding space. [1]. Proc Natl Acad Sci U S A. 2002 Nov 12; 99(23): 14658-14663.
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