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BMS-986278

Catalog No. T39647 CAS 2170126-74-4

BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.

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BMS-986278, CAS 2170126-74-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 578.00
10 mg	In stock	$ 928.00
25 mg	In stock	$ 1,870.00
50 mg	In stock	$ 2,970.00
100 mg	In stock	$ 3,970.00
1 mL * 10 mM (in DMSO)	In stock	$ 638.00

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Purity: 99.86%

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Description	BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.
In vitro	With Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, BMS-986278 is a high-affinity LPA1 antagonist. These values were determined in CHO cells overexpressing LPA1[1]. BMS-986278 also antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, exhibiting a Kb of 5.8 nM[1].
In vivo	In CD1 mice, a single oral administration of BMS-986278 (0.1-10 mg/kg) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner[1]. Furthermore, when administered orally twice daily for 14 days at doses ranging from 3 to 30 mg/kg, BMS-986278 reduces Bleomycin-induced collagen deposition and lung fibrosis in rats[1].

Molecular Weight	445.51
Formula	C22H31N5O5
CAS No.	2170126-74-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (202.02 mM), Sonication is recommended.

References and Literature

1. Cheng PTW, et al. Murphy BJ. Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases. J Med Chem. 2021 Nov 11;64(21):15549-15581.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Drug Repurposing Compound Library GPCR Compound Library

Related Products

Related compounds with same targets

Ki16198 GRI977143 1-Oleoyl lysophosphatidic acid sodium ONO-7300243 AM095 Ki16425 Tetradecyl Phosphonate H2L 5765834

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Keywords

BMS-986278 2170126-74-4 GPCR/G Protein LPA Receptor BMS986278 BMS 986278 inhibitor inhibit

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