BMS-986278 free base · Synonyms: Admilparant

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 antagonist.

For research use only. Not for human or veterinary use.

Target LPL Receptor

Research area Others

Purity >98% Stock Inquire

Data Sheet SDS COA

BMS-986278 structure

CAS No.: 2170126-74-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 480.00	BP-01982-250mg	In stock	Get quote
500 mg	USD 780.00	BP-01982-500mg	In stock	Get quote
1 g	USD 1,250.00	BP-01982-1g	In stock	Get quote
5 g	Inquire	BP-01982-5g	Inquire	Inquire

Need another size or custom synthesis? Request a quote.

Description

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic disease.

Biological activity

In Vitro BMS-986278 is a high-affinity LPA1 antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1 in CHO cells overexpressing LPA1. BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a Kb of 5.8 nM. In Vivo BMS-986278 (0.1-10 mg/kg; a single p.o.) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner in CD1 mice. BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats.

Identifiers

SMILES: CC1=NC(C2=C(COC(N(C)CCC)=O)N(C)N=N2)=CC=C1O[C@@H]3C[C@@H](C(O)=O)CCC3
InChIKey: UEUNDURNLYLSNB-HOTGVXAUSA-N

Specifications

MW (average): 445.5120
Formula: C₂₂H₃₁N₅O₅
CAS No.: 2170126-74-4
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 100 mg/mL

Documents

References

[1]. Cheng PTW, 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. 2021 Nov 11;64(21):15549-15581.

Same target

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