BMS-986120

Name: BMS-986120
Brand: TargetMol
SKU: T14684
Rating: 4.5 (1 reviews)

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Catalog No. T14684Cas No. 1478712-37-6

BMS-986120 is a first-in-class oral, reversible protease-activated receptor 4 (PAR4) antagonist with IC50s of 9.5 nM in human blood and 2.1 nM in monkey blood, exhibiting potent and selective antiplatelet effects[1][2].

BMS-986120

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Catalog No. T14684Cas No. 1478712-37-6

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,080	10-14 weeks	10-14 weeks
50 mg	$1,410	10-14 weeks	10-14 weeks
100 mg	$2,250	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	BMS-986120 is a first-in-class oral, reversible protease-activated receptor 4 (PAR4) antagonist with IC50s of 9.5 nM in human blood and 2.1 nM in monkey blood, exhibiting potent and selective antiplatelet effects[1][2].
Targets&IC50	PAR4 (monkey):2.1 nM, PAR4 (human):9.5 nM
In vitro	BMS-986120 has high binding affinity to PAR4 expressed on HEK293 cells. And it inhibition of PAR4-induced calcium mobilization with an IC50 of 0.56 nM[3].
In vivo	BMS, administered at dosages of 0.2, 0.5, and 1 mg/kg, decreases tail withdrawal (TW) by 35±5, 49±4, and 83±4%, respectively. In monkeys, a 1 mg/kg dose of BMS shows no inhibition of platelet aggregation (PA) triggered by PAR1-AP, ADP, and collagen, indicating selectivity. The maximum increases observed in kaolin bleeding time (KBT) and mepacrine bleeding time (MBT) are limited to 2.2-fold and 1.8-fold, respectively[1].

Chemical Properties

Molecular Weight	513.59
Formula	C₂₃H₂₃N₅O₅S₂
Cas No.	1478712-37-6
Smiles	COc1nn2cc(nc2s1)-c1cc2c(OCc3nc(sc3C)N3CCOCC3)cc(OC)cc2o1
Relative Density.	1.57 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc