An LPA1 receptor antagonist
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BMS 986020

Item No. 22049

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl][1,1'-biphenyl]-4-yl]-cyclopropanecarboxylic acid
CAS Number
1257213-50-5
Synonyms
  • AM-000152
Molecular Formula
C29H26N2O5
Formula Weight
482.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMF:PBS (pH7.2) (1:40): 0.02 mg/mlDMSO: 25 mg/mlEthanol: 20 mg/ml
λmax
297 nm
SMILES
O=C(O)C1(CC1)C(C=C2)=CC=C2C(C=C3)=CC=C3C4=C(NC(O[C@H](C)C5=CC=CC=C5)=O)C(C)=NO4
InChi Code
InChI=1S/C29H26N2O5/c1-18-25(30-28(34)35-19(2)20-6-4-3-5-7-20)26(36-31-18)23-10-8-21(9-11-23)22-12-14-24(15-13-22)29(16-17-29)27(32)33/h3-15,19H,16-17H2,1-2H3,(H,30,34)(H,32,33)/t19-/m1/s1
InChi Key
GQBRZBHEPUQRPL-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    500 µg

    $36

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    1 mg

    $68

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    5 mg

    $169

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    Product Description

    BMS 986020 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; Kb = 0.0067 µM).1 It is selective for LPA1 over LPA3 in CHO cells expressing the human receptors (IC50s = 0.3 and >1 µM, respectively).2 BMS 986020 also inhibits organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, the bile salt export pump (BSEP), multidrug resistant protein 3 (MDR3), multidrug resistance-associated protein 3 (MRP3), and MRP4 (IC50s = 0.17, 0.57, 4.8, 7.5, 22, and 6.2 µM, respectively).1 It reduces bleomycin-induced lung fibrosis in rats when administered at a dose of 30 mg/kg twice per day. BMS 986020 (225 and 500 mg/kg per day) decreases total biliary bile acid levels and induces bile duct hyperplasia, cholangitis, and cholestasis in monkeys.3 It decreases infarct volume and neurological deficits in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (MCAO) when administered at a dose of 5 mg/kg.4

    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. Hutchinson, J.H., Seiders, T.J., Wang, B., et al. Polycyclic antagonists of lysophosphatidic acid receptors. (2010).

    3. 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).

    4. Gaire, B.P., Sapkota, A., and Choi, J.W. BMS-986020, a specific LPA1 antagonist, provides neuroprotection against ischemic stroke in mice. Antioxidants (Basel) 9(11), 1097 (2020).