规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
Vasopressin V1 receptor
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体外研究 (In Vitro) |
特利加压素(25 nM;24-72 小时;IEC-6 细胞)治疗可显着改善 IEC-6 细胞的细胞活力、增殖和凋亡[1]。 Terlipressin 可抑制缺氧和葡萄糖剥夺/复氧 (OGD/R) 后 IEC-6 细胞分泌 TNF-α 和 15-F2t-异前列腺素。 OGD 后给予特利加压素可通过 PI3K 信号通路减轻 OGD/R 诱导的细胞损伤[1]。细胞增殖测定[1] 细胞系:氧气和葡萄糖剥夺/复氧 (OGD/R) 诱导的 IEC-6 细胞 浓度:25 nM 孵育时间:24 小时、48 小时、72 小时 结果:显着增加细胞增殖IEC-6 电池。
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体内研究 (In Vivo) |
使用小鼠非致死性肝缺血再灌注 (IR) 模型,给予特利加压素可显着改善 IR 诱导的肝细胞凋亡、坏死和炎症[3]。
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细胞实验 |
细胞系:氧气和葡萄糖剥夺/复氧 (OGD/R) 诱导的 IEC-6 细胞
浓度:25 nM 孵育时间:24 小时、48 小时、72 小时 结果:显着增加IEC-6细胞的增殖。 |
参考文献 |
分子式 |
C52H74N16O15S2
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分子量 |
1227.3722
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精确质量 |
1227.38
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元素分析 |
C, 50.89; H, 6.08; N, 18.26; O, 19.55; S, 5.22
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CAS号 |
14636-12-5
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相关CAS号 |
Terlipressin diacetate; 1884420-36-3; Terlipressin acetate; 914453-96-6
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外观&性状 |
Solid powder
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SMILES |
C1C[C@H](N(C1)C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)NC(=O)CNC(=O)CNC(=O)CN)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N
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InChi Key |
BENFXAYNYRLAIU-QSVFAHTRSA-N
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InChi Code |
InChI=1S/C52H74N16O15S2/c53-17-5-4-9-31(45(76)60-23-41(57)72)63-51(82)38-10-6-18-68(38)52(83)37-27-85-84-26-36(61-44(75)25-59-43(74)24-58-42(73)22-54)50(81)65-34(20-29-11-13-30(69)14-12-29)48(79)64-33(19-28-7-2-1-3-8-28)47(78)62-32(15-16-39(55)70)46(77)66-35(21-40(56)71)49(80)67-37/h1-3,7-8,11-14,31-38,69H,4-6,9-10,15-27,53-54H2,(H2,55,70)(H2,56,71)(H2,57,72)(H,58,73)(H,59,74)(H,60,76)(H,61,75)(H,62,78)(H,63,82)(H,64,79)(H,65,81)(H,66,77)(H,67,80)/t31-,32-,33-,34-,35-,36-,37-,38-/m0/s1
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化学名 |
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-[[2-[[2-[(2-aminoacetyl)amino]acetyl]amino]acetyl]amino]-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-6-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxohexan-2-yl]pyrrolidine-2-carboxamide
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别名 |
Glycylpressin; Remestyp; Terlipressin
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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 |
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) |
DMSO: ~100 mg/mL (~81.5 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 | 0.8148 mL | 4.0738 mL | 8.1475 mL | |
5 mM | 0.1630 mL | 0.8148 mL | 1.6295 mL | |
10 mM | 0.0815 mL | 0.4074 mL | 0.8148 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) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04460560 | Active Recruiting |
Drug: Terlipressin | Hepatorenal Syndrome | University of Pennsylvania | December 11, 2020 | Phase 3 |
NCT05170230 | Recruiting | Drug: Terlipressin | Myoma | Wael Elbanna Clinic | February 27, 2022 | Not Applicable |
NCT05242783 | Recruiting | Drug: Terlipressin | Myoma | Wael Elbanna Clinic | February 1, 2022 | Not Applicable |
NCT05154279 | Recruiting | Drug: Terlipressin | Laparoscopic Myomectomy | Wael Elbanna Clinic | February 27, 2022 | Not Applicable |
NCT04961528 | Recruiting | Drug: Terlipressin Drug: Placebo Drug: Tranexamic Acid 500 MG |
Hemoptysis | Assistance Publique - Hôpitaux de Paris |
March 27, 2022 | Phase 3 |
Forest plot showing the difference in the control of bleeding in patients treated with terlipressin compared with no vasoactive drugs. Medicine (Baltimore) . 2018 Nov;97(48):e13437. td> |
Forest plot showing the difference in the rebleeding in patients treated with terlipressin compared with balloon tamponade. Medicine (Baltimore) . 2018 Nov;97(48):e13437. td> |
The effect of Terlipressin on the overall mouse hepatic blood perfusion in vivo. Oncotarget . 2016 Oct 25;7(43):69276-69290. td> |
Terlipressin treatment ameliorates hepatic injury and inflammation. Oncotarget . 2016 Oct 25;7(43):69276-69290. td> |
Changes in IEC-6 cell viability following OGD/R. (A) Effect of different concentrations of terlipressin on IEC-6 cell viability following OGD/R. Exp Ther Med . 2017 Jul;14(1):260-266. td> |