BMS-654457
BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.
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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: 1004551-41-0
- 分子式: C36H37N5O4
- 分子量:603.71
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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
BMS-654457 shows comparable in vitro potency against FXIa in humans (Ki=0.2 nM) and in rabbits (Ki =0.42 nM), and was over 500-fold selective against coagulation-related proteases (thrombin, FXa and FVIIa) in these species[1].
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.
化学情報
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CAS 番号 1004551-41-0
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分子量 603.71
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分子式 C36H37N5O4
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SMILES
NC(C1=CC=C(N[C@H](C2=CC(C3=CC=C(C(N)=O)C=C3C(O)=O)=CC(NC(CC(C)C)=O)=C2)C[C@]4(C)C5=CC=CC=C5)C4=C1)=N
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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.
プロトコル
Platelet aggregation is measured in hirudin-treated rabbit platelet-rich plasma (PRP) with a platelet aggregometer. PRP is mixed with 2.5 μL of vehicle or BMS-654457 at 1 and 10 μM and incubated for 2 min at 37°C. Peak platelet aggregation is determined after the addition of 2.5 μL of the agonist (ADP at 10 μM, arachidonic acid at 250 μM and collagen at 10 μg/mL, final concentration)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rabbits[1]
[1]BMS-654457 or vehicle (10 % N-N-dimethylacetamide:90 % of 5 % dextrose) is administered as a bolus plus sustaining IV infusion begun 30 min prior to each protocol. Treatment groups include BMS-654457 (mg/kg+mg/kg/h) at 0.011+0.008, 0.037+0.027, 0.11+0.08, 0.37+0.27 and 1.1 +0.8 or vehicle (n=6 per group). The plasma concentration that increased iCBF to EC50 was estimated for BMS654457[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)