S18886
(Synonyms: 特鲁曲班,Terutroban,Triplion) 目录号 : GC17410
A TP receptor antagonist
Cas No.:165538-40-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 16.4 nM for TP receptor
S18886 is a potent thromboxane A2 (TP) inhibitor.
The lipid mediator thromboxane A2 (TXA2) plays a critical role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated via the specific G protein coupled-receptor, TXA2 receptor (TP).
In vitro: S18886 was identified as the active isomer of the potent TP receptor antagonist S18204. S18886 was also found to be a selective antagonist of thromboxaneprostaglandin receptors in platelets and in the vessel wall [1].
In vivo: In a previous animal study, it was found that S18886 treatment could reduce the portal pressure in both animal models without producing significant changes in portal blood flow, indicating a reduction in hepatic vascular resistance. S18886 could not significantly change arterial pressure in CCl4 -cirrhotic rats but could significantly decrease it in BDL-cirrhotic rats [2].
Clinical trial: A previoius trial aiming to evaluate S18886 versus aspirin in patients with cerebral ischaemic events showed similar rates of the primary endpoint with S18886 and aspirin, without safety advantages for S18886 [3].
References:
[1] Cimetière B, Dubuffet T, Landras C, Descombes JJ, Simonet S, Verbeuren TJ, Lavielle G. New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors. Bioorg Med Chem Lett. 1998 Jun 2;8(11):1381-6.
[2] Rosado E, Rodríguez-Vilarrupla A, Gracia-Sancho J, Tripathi D, García-Calderó H, Bosch J, García-Pagán JC. Terutroban, a TP-receptor antagonist, reduces portal pressure in cirrhotic rats. Hepatology. 2013 Oct;58(4):1424-35.
[3] Bousser MG, Amarenco P, Chamorro A, Fisher M, Ford I, Fox KM, Hennerici MG, Mattle HP, Rothwell PM, de Cordoüe A, Fratacci MD; PERFORM Study Investigators. Terutroban versus aspirin in patients with cerebral ischaemic events (PERFORM): a randomised, double-blind, parallel-group trial. Lancet. 2011 Jun 11;377(9782):2013-22.
| Cas No. | 165538-40-9 | SDF | |
| 别名 | 特鲁曲班,Terutroban,Triplion | ||
| 化学名 | (6R)-6-[[(4-chlorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydro-2-methyl-1-naphthalenepropanoic | ||
| Canonical SMILES | CC1=C(CCC(O)=O)C2=C(C=C1)C[C@H](NS(C3=CC=C(Cl)C=C3)(=O)=O)CC2 | ||
| 分子式 | C20H22ClNO4S | 分子量 | 407.9 |
| 溶解度 | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4516 mL | 12.2579 mL | 24.5158 mL |
| 5 mM | 0.4903 mL | 2.4516 mL | 4.9032 mL |
| 10 mM | 0.2452 mL | 1.2258 mL | 2.4516 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet