An antagonist of LPA1
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BMS 986278

Item No. 43597

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S,3S)-3-[[2-methyl-6-[1-methyl-5-[[[(methylpropylamino)carbonyl]oxy]methyl]-1H-1,2,3-triazol-4-yl]-3-pyridinyl]oxy]-cyclohexanecarboxylic acid
CAS Number
2170126-74-4
Synonyms
  • Admilparant
Molecular Formula
C22H31N5O5
Formula Weight
445.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(N(C)CCC)OCC1=C(C(N=C2C)=CC=C2O[C@@H](CCC3)C[C@H]3C(O)=O)N=NN1C
InChi Code
InChI=1S/C22H31N5O5/c1-5-11-26(3)22(30)31-13-18-20(24-25-27(18)4)17-9-10-19(14(2)23-17)32-16-8-6-7-15(12-16)21(28)29/h9-10,15-16H,5-8,11-13H2,1-4H3,(H,28,29)/t15-,16-/m0/s1
InChi Key
UEUNDURNLYLSNB-HOTGVXAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $193

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    10 mg

    $290

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    25 mg

    $530

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    50 mg

    $675

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    Product Description

    BMS 986278 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; Kb = 0.0069 µM).1 It is selective for LPA1 over a panel of 44 receptors, ion channels, and enzymes when used at concentrations ranging from 30 to 150 µM, including the bile salt export pump (BSEP), multidrug resistance protein 3 (MDR3), multidrug resistance-associated protein 3 (MRP3), MRP4, organic anion transporting polypeptide 1B1 (OATP1B1), and OATP1B3 (IC50s = >100, >100, 66, 47, 36, and 10 µM, respectively). BMS 986278 inhibits LPA-induced histamine release in mice in a dose-dependent manner. Oral administration of BMS 986278 (3 and 10 mg/kg) reduces bleomycin-induced lung fibrosis in rats. Unlike BMS 986020 (Item No. 22049), BMS 986278 does not induce bile duct hyperplasia, cholangitis, or cholestasis in cynomolgus monkeys.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cheng, P.T.W., Kaltenbach, R.F., III, Zhang, H., et al. Discovery of an oxycyclohexyl acid lysophosphatidic acid receptor 1 (LPA1) antagonist BMS-986278 for the treatment of pulmonary fibrotic diseases. J. Med. Chem. 64(21), 15549-15581 (2021).

    2. Sivaraman, L., Gill, M., Nelson, D.M., et al. Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA1) antagonists. Toxicol. Appl. Pharmacol. 438, 115846 (2021).