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BMS 986120

Catalog No.GC18717

A selective PAR4 antagonist

Products are for research use only. Not for human use. We do not sell to patients.

BMS 986120 Chemical Structure

Cas No.:1478712-37-6

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1mg
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5mg
$634.00
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10mg
$1,123.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

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].

References:

[1]. Pancras C Wong, et al. Abstract 175: A Novel Orally-Active Small-Molecule Antagonist of the Platelet Protease-Activated Receptor-4, BMS-986120, Inhibits Arterial Thrombosis With Limited Impact on Hemostasis in Cynomolgus Monkeys. Stroke. 2018;47:A175.
[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.
[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).

Background

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].

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].

In monkeys, BMS (1 mg/kg) does not inhibit PA induced by PAR1-AP, ADP and collagen, supporting selectivity. BMS (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].

References:
[1]. Pancras C Wong, et al. Abstract 175: A Novel Orally-Active Small-Molecule Antagonist of the Platelet Protease-Activated Receptor-4, BMS-986120, Inhibits Arterial Thrombosis With Limited Impact on Hemostasis in Cynomolgus Monkeys. Stroke. 2018;47:A175.
[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.
[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).

Chemical Properties

Cas No. 1478712-37-6 SDF
Chemical Name 2-methoxy-6-[6-methoxy-4-[[5-methyl-2-(4-morpholinyl)-4-thiazolyl]methoxy]-2-benzofuranyl]-imidazo[2,1-b]-1,3,4-thiadiazole
Canonical SMILES COC1=CC2=C(C=C(C3=CN4C(SC(OC)=N4)=N3)O2)C(OCC5=C(C)SC(N6CCOCC6)=N5)=C1
Formula C23H23N5O5S2 M.Wt 513.6
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.
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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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