Terbogrel
Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 149979-74-8
- 分子式: C23H27N5O2
- 分子量:405.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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TXA2/TP |
Pretreatment of platelets with terbogrel 1 μM completely inhibits thrombin-induced thromboxane A2 formation (2±1 ng/mL) but does not result in any inhibition of platelet aggregation. Terbogrel (1 μM) completely inhibits U46619-induced platelet aggregation, and the IC50 value is 10 nM. Terbogrel inhibits both platelet aggregation and thromboxane A2 formation with an IC50 of about 10 nM[1]. Terbogrel inhibits the thromboxane A2 synthase in human gel-filtered platelets with an IC50 value of 4.0 ± 0.5 nM. Terbogrel blocks the thromboxane A2/endoperoxide receptor on washed human platelets with an IC50 of 11 ± 6 nM (n = 2) and with an IC50 of 38 ± 1 nM (n = 15) in platelet-rich plasma. Terbogrel inhibits the collagen-induced platelet aggregation in human platelet-rich plasma and whole blood with an IC50 of 310 ± 18 nM (n = 8) and 52 ± 20 nM (n = 6), respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 149979-74-8
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分子量 405.49
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分子式 C23H27N5O2
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SMILES
O=C(O)CCC/C=C(C1=CC=CC(/N=C(NC#N)/NC(C)(C)C)=C1)/C2=CC=CN=C2
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別名
BIBV 308SE
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Muck S, et al. Effects of terbogrel on platelet function and prostaglandin endoperoxide transfer. Eur J Pharmacol. 1998 Feb 26;344(1):45-8. [Content Brief]
[2]. Soyka R, et al. Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors. J Med Chem. 1999 Apr 8;42(7):1235-49. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)