SSR182289
SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
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- CAS No.: 363151-21-7
- Formule: C30H33F2N5O4S
- Masse moléculaire:597.68
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[2]|
human Thrombin 0.031 nM (Ki) |
Trypsin 54 nM (Ki) |
Factor VIIa/tissue factor 167 μM (Ki) |
Factor IXa >250 μM (Ki) |
Factor Xa >250 μM (Ki) |
Plasmin >250 μM (Ki) |
Urokinase >250 μM (Ki) |
tPA >250 μM (Ki) |
Kallikrein >250 μM (Ki) |
Activated protein C >250 μM (Ki) |
Chemical Information
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CAS No. 363151-21-7
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Masse moléculaire 597.68
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Formule C30H33F2N5O4S
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SMILES
CC(NC1=C(S(=O)(N[C@H](C(N2CC/C(CC2)=C(F)/F)=O)CCCC3=NC=C(N)C=C3)=O)C=CC=C1C4=CC=CC=C4)=O
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Synonyms
SSR182289A free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
[1]. Jean-Michel Altenburger, et al. SSR182289A, a selective and potent orally active thrombin inhibitor. Bioorg Med Chem. 2004 Apr 1;12(7):1713-30. [Content Brief]
[2]. Jean-Michel Altenburger, et al. SSR182289A, a selective and potent orally active thrombin inhibitor. Bioorg Med Chem. 2004 Apr 1;12(7):1713-30. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SSR182289 Related Classifications
HY-19674 Related Classifications
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