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Submit ReviewFR 171113
说明： PAR1 antagonist
化学名： 2-[3-(4-Chlorophenyl)-2-[(2,4-dichlorobenzoyl)imino]-4-oxo-5-thiazolidinylidene]-acetic acid methyl ester
纯度： ≥98% (HPLC)
生物活性 for FR 171113
FR 171113 is a protease-activated receptor 1 (PAR1) antagonist. Exhibits potent antiplatelet activity in vitro; inhibits thrombin TRAP-6-induced platelet aggregation (IC50 = 2.5 μM) with no effect on coagulation time.
技术数据 for FR 171113
| 分子量 | 469.73 |
| 公式 | C19H11Cl3N2O4S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 173904-50-2 |
| PubChem ID | 25015749 |
| InChI Key | SDGLYCKTPKZBGI-DALCUZTNSA-N |
| Smiles | O=C(/N=C(N(C3=CC=C(Cl)C=C3)C2=O)\S/C2=C/C(OC)=O)C1=CC=C(Cl)C=C1Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for FR 171113
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 4.7 | 10 |
制备储备液 for FR 171113
以下数据基于产品分子量 469.73。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 21.29 mL | 106.44 mL | 212.89 mL |
| 0.5 mM | 4.26 mL | 21.29 mL | 42.58 mL |
| 1 mM | 2.13 mL | 10.64 mL | 21.29 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
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产品说明书 for FR 171113
参考文献 for FR 171113
参考文献是支持产品生物活性的出版物。
Kato et al (1999) In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist. Eur.J.Pharmacol. 384 197 PMID: 10611442
Kato et al (2003) Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig. Eur.J.Pharmacol. 473 163 PMID: 12892834
If you know of a relevant reference for FR 171113, please let us know.
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关键词: FR 171113, FR 171113 supplier, FR171113, thrombin, protease-activated, receptor, 1, PAR1, antagonist, antagonists, antithrombotic, antiplatelet, Protease-Activated, Receptors, 3643, Tocris Bioscience
1 篇 FR 171113 的引用文献
引用文献是使用了 Tocris 产品的出版物。 FR 171113 的部分引用包括：
Eum et al (2014) Disruption of epithelial barrier by quorum-sensing N-3-(oxododecanoyl)-homoserine lactone is mediated by matrix metalloproteinases. Am J Physiol Gastrointest Liver Physiol 306 G992 PMID: 24742991
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FR 171113 的评论
平均评分: 3 (Based on 1 Review.)
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PAR1 antagonism not awesome - perhaps SCH compound a better choice.
By
Andrew Randall on 10/17/2019
分析类型： In Vitro
种属： Human
细胞系/组织： Brain Pericytes
To attempt to block TRAP6 mediated Ca2+ mobilization in human pericytes. Its lack of potency and low solubility means it was not especially effective even with sub-maximal agonist concentrations - some antagonism or slowing of response - but not the complete block I had hoped for even when pre-equilibrated prior to agonist activation. We will now save our pennies to try the more potent SCH PAR1 antag
Really could not get this to dissolve at 10 mM in DMSO as website suggests - probably goes in around 7 mM. As this is not a very potent antagonist you will need to have quite a bit of DMSO around to get even partial antagonism.