A selective PAR4 antagonist
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BMS 986120

Item No. 23497

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
1478712-37-6
Molecular Formula
C23H23N5O5S2
Formula Weight
513.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
305 nm
SMILES
COC1=CC2=C(C=C(C3=CN4C(SC(OC)=N4)=N3)O2)C(OCC5=C(C)SC(N6CCOCC6)=N5)=C1
InChi Code
InChI=1S/C23H23N5O5S2/c1-13-17(25-21(34-13)27-4-6-31-7-5-27)12-32-18-8-14(29-2)9-19-15(18)10-20(33-19)16-11-28-22(24-16)35-23(26-28)30-3/h8-11H,4-7,12H2,1-3H3
InChi Key
MINMDCMSHDBHKG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $134

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    5 mg

    $598

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    10 mg

    $1,058

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    Product Description

    BMS 986120 is an orally bioavailable, selective, and reversible antagonist of proteinase-activated receptor 4 (PAR4; IC50 = 0.56 nM to inhibit calcium mobilization induced by PAR4 agonist peptide (PAR4-AP) in HEK293 cells).1 It is selective for PAR4 over PAR1, PAR2, and a panel of purified proteases, including thrombin. It inhibits platelet aggregation in vitro in human platelet-rich plasma (IC50 = 7.3 nM). BMS 986120 (0.2-1 mg/kg) decreases platelet aggregation induced by PAR4-AP ex vivo in a dose-dependent manner, but does not increase clotting times. In vivo, BMS 986120 (1 mg/kg) prevents vascular occlusion and reduces thrombus formation by 82% in cynomolgus monkeys.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wong, P.C., Seiffert, D., Bird, J.E., et al. Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding. Sci. Transl. Med. 9(371), eaaf5294 (2017).