2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. BMS-986120

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.

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BMS-986120

BMS-986120 構造式

CAS 番号 : 1478712-37-6

容量 価格（税別） 在庫状況 数量
5 mg $350 在庫あり
10 mg $550 在庫あり
25 mg $1100 在庫あり
50 mg $1700 在庫あり
100 mg $2720 在庫あり
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500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

BMS-986120 関連抗体

Top Publications Citing Use of Products

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PAR1 PAR2 PAR4

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  • 純度とドキュメンテーション

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製品説明

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[1][2].

IC50 & Target

PAR1

 

PAR4

 

Cellular Effect
Cell Line Type Value Description References
Platelet IC50
>200 nM
Compound: 43; BMS-986120
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
[PMID: 35729784]
Platelet IC50
>200 nM
Compound: 43; BMS-986120
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
[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
[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
[PMID: 35729784]
Platelet IC50
17.5 nM
Compound: 43; BMS-986120
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
[PMID: 35729784]
Platelet IC50
7.6 nM
Compound: 43; BMS-986120
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
[PMID: 35729784]
体外実験

BMS-986120 has high binding affinity to PAR4 expressed on HEK293 cells and inhibition of PAR4-induced calcium mobilization with an IC50 of 0.56 nM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986120 関連抗体
体内実験

In monkeys, BMS-986120 (1 mg/kg) does not inhibit PA induced by PAR1-AP, ADP and collagen, supporting selectivity. BMS-986120 (0.2, 0.5, 1 mg/kg) reduces TW by 35±5, 49±4, and 83±4%, respectively. Maximum KBT and MBT increases are only 2.2-fold and 1.8-fold, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

513.59

分子式

C23H23N5O5S2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC(SC(N1CCOCC1)=N2)=C2COC3=CC(OC)=CC4=C3C=C(O4)C5=CN6N=C(OC)SC6=N5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9471 mL 9.7354 mL 19.4708 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 mL
10 mM --- --- ---
View the 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.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 98.22%

COA (253 KB) HNMR (363 KB) RP-HPLC (276 KB) MS (485 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[1]

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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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
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BMS-986120 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-9861201478712-37-6BMS986120BMS 986120Protease Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-19837
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