| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| Other Sizes |
| 靶点 |
Cell wall synthesis
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|---|---|---|
| 体外研究 (In Vitro) |
flucloxacillin对金黄色葡萄球菌的最低抑菌浓度（MIC）为0.25-2 μg/mL。当与阿莫西林联合使用时，对产β-内酰胺酶菌株的协同作用显著，部分抑菌浓度（FIC）指数≤0.5，显示出相加或协同效应
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| 体内研究 (In Vivo) |
氟氯西林的血清消除半衰期为1.31-1.39小时，单次250mg剂量给药后6小时，氟氯西林的血清浓度为0.46微克/mL[1]。口服氟氯西林不会影响汗液电解质，也不是汗液检测的禁忌症[2]。据报道，氟氯西林在人体内代谢为青霉霉酸、抗菌活性5-羟甲基衍生物和5-羟甲基衍生物的青霉霉酸。氟氯西林在大鼠体内的代谢相似[3]。
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| 动物实验 |
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| 药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
Bioavailability is 50–70% following oral administration. Metabolism / Metabolites Hepatic. Flucloxacillin has known human metabolites that include 6-[[3-(2-Chloro-6-fluorophenyl)-5-(hydroxymethyl)-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid. Biological Half-Life 0.75–1 hour |
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| 毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Floxacillin (flucloxacillin) is not approved for marketing in the United States by the U.S. Food and Drug Administration. It is acceptable to use during breastfeeding and is frequently used abroad to treat mastitis in nursing mothers. Limited information indicates that floxacillin levels in milk are low and are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with penicillins, but these effects have not been adequately evaluated. Floxacillin is acceptable in nursing mothers. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| 参考文献 | ||
| 其他信息 |
Flucloxacillin is a penicillin compound having a 6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido] side-chain. It has a role as an antibacterial drug. It is a penicillin and a penicillin allergen. It is a conjugate acid of a flucloxacillin(1-).
Antibiotic analog of [cloxacillin]. Flucloxacillin is a narrow-spectrum, semisynthetic isoxazolyl penicillin with antibacterial activity. Floxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. Antibiotic analog of CLOXACILLIN. Drug Indication Used to treat bacterial infection by susceptible microorganisms. Mechanism of Action By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, flucloxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that flucloxacillin interferes with an autolysin inhibitor. |
| 分子式 |
C19H16CLFN3NAO5S
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|---|---|
| 分子量 |
475.8512
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| 精确质量 |
475.038
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| 元素分析 |
C, 47.96; H, 3.39; Cl, 7.45; F, 3.99; N, 8.83; Na, 4.83; O, 16.81; S, 6.74
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| CAS号 |
1847-24-1
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| 相关CAS号 |
Flucloxacillin;5250-39-5
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| PubChem CID |
21319
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| 外观&性状 |
Solid powder
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| 沸点 |
677.3ºC at 760 mmHg
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| 熔点 |
176-178ºC
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| 闪点 |
363.4ºC
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| 蒸汽压 |
2.86E-19mmHg at 25°C
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| LogP |
1.681
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| tPSA |
140.87
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| 氢键供体(HBD)数目 |
2
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| 氢键受体(HBA)数目 |
8
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| 可旋转键数目(RBC) |
4
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| 重原子数目 |
30
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| 分子复杂度/Complexity |
758
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| 定义原子立体中心数目 |
3
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| SMILES |
ClC1=C([H])C([H])=C([H])C(=C1C1C(=C(C([H])([H])[H])ON=1)C(N([H])[C@]1([H])C(N2[C@@]([H])(C(=O)[O-])C(C([H])([H])[H])(C([H])([H])[H])S[C@@]21[H])=O)=O)F.[Na+]
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| InChi Key |
OTEANHMVDHZOPB-SLINCCQESA-M
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| InChi Code |
InChI=1S/C19H17ClFN3O5S.Na/c1-7-10(12(23-29-7)11-8(20)5-4-6-9(11)21)15(25)22-13-16(26)24-14(18(27)28)19(2,3)30-17(13)24/h4-6,13-14,17H,1-3H3,(H,22,25)(H,27,28)/q+1/p-1/t13-,14+,17-/m1./s1
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| 化学名 |
Sodium (2S-(2alpha,5alpha,6beta))-6-(((3-(2-chloro-6-fluorophenyl)-5-methylisoxazol-4-yl)carbonyl)amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylate
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| 别名 |
Floxapen;Floxacillin;Flucloxacillin; Floxacillin sodium; Floxapen sodium; Sodium flucloxacillin; Monosodium flucloxacillin; Stafopen sodium salt; Staphylex Sodium salt; MFI-PC; ...; 1847-24-1; Fluorochloroxacillin
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。 |
| 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)
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| 溶解度 (体外实验) |
H2O : ~100 mg/mL (~210.15 mM )
DMSO : ≥ 100 mg/mL (~210.15 mM) |
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| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (5.25 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 (5.25 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。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (5.25 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。 配方 4 中的溶解度: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (5.25 mM) 配方 5 中的溶解度: 100 mg/mL (210.15 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶. 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 | 2.1015 mL | 10.5075 mL | 21.0150 mL | |
| 5 mM | 0.4203 mL | 2.1015 mL | 4.2030 mL | |
| 10 mM | 0.2102 mL | 1.0508 mL | 2.1015 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：取 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) 。
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