BMS-986120
Based on 1 publication(s) in Google Scholar
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
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。
- 純度: 98.14%
- CAS 番号: 1478712-37-6
- 分子式: C23H23N5O5S2
- 分子量:513.59
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 BMS-986120
More
生物活性
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PAR1 |
PAR4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
>200 nM
Compound: 43; BMS-986120
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Antiplatelet activity against ADP agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against ADP agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
>200 nM
Compound: 43; BMS-986120
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Antiplatelet activity against collagen agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against collagen agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
>200 nM
Compound: 43; BMS-986120
|
Antiplatelet activity against PAR1 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against PAR1 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
>200 nM
Compound: 43; BMS-986120
|
Antiplatelet activity against U46619 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against U46619 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
17.5 nM
Compound: 43; BMS-986120
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Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
7.6 nM
Compound: 43; BMS-986120
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Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
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[PMID: 35729784] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1478712-37-6
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性状 Solid
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分子量 513.59
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分子式 C23H23N5O5S2
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Color White to off-white
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SMILES
CC(SC(N1CCOCC1)=N2)=C2COC3=CC(OC)=CC4=C3C=C(O4)C5=CN6N=C(OC)SC6=N5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 3.33 mg/mL (6.48 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Monkeys[1]
Individual anesthetized monkeys are given orally of BMS-986120 (BMS: 0.2, 0.5,1 mg/kg) or vehicle (n=8/group) 2 hour before a combination of thrombosis, BT and ex vivo biomarker experiments. Aspirin alone (ASA, 4 mg/kg/h IV) or in combination with BMS-986120 (0.5, 1 mg/kg) is also studied (n=8/group). Thrombus weight (TW) reduction, BT increase over vehicle in kidney (KBT) and mesenteric artery (MBT), and platelet aggregation (PA) inhibition are determined. Peak PA responses to activation peptides selective for PAR4 (PAR4-AP, 12.5 μM) and PAR1 (PAR1-AP, 18 μM), ADP (20 μM), and collagen (5 μg/mL) are determined by whole blood aggregometry[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
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データシート (277 KB)
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SDS (557 KB)
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- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Wilson SJ, et al. PAR4 (Protease-Activated Receptor 4) Antagonism With BMS-986120 Inhibits Human Ex VivoThrombus Formation. Arterioscler Thromb Vasc Biol. 2018 Feb;38(2):448-456. [Content Brief]
[3]. Wong PC, et al. Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding. Sci Transl Med. 2017 Jan 4;9(371). [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9471 mL | 9.7354 mL | 19.4708 mL | 48.6770 mL |
| 5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | 9.7354 mL |
BMS-986120 関連分類
HY-19837 関連分類
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