Admilparant (BMS-986278) | LPA1 antagonist

Chemical Structure : Admilparant

CAS No.: 2170126-74-4

Admilparant (BMS-986278, BMS986278)

Catalog No.: PC-72349Not For Human Use, Lab Use Only.

Admilparant (BMS-986278) is a potent, selective lysophosphatidic acid receptor 1 (LPA1, LPAR1) antagonist with Kb of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.

Packing	Price	Stock
5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$188	In stock
50 mg	$298	In stock
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Biological Activity

Admilparant (BMS-986278) is a potent, selective lysophosphatidic acid receptor 1 (LPA1, LPAR1) antagonist with Kb of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.

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.

BMS-986278 is under clinical trials, including an ongoing Phase 2 clinical trial in patients with lung fibrosis.

Physicochemical Properties

M.Wt	445.52
Formula	C22H31N5O5
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Cyclohexanecarboxylic acid, 3-[[2-methyl-6-[1-methyl-5-[[[(methylpropylamino)carbonyl]oxy]methyl]-1H-1,2,3-triazol-4-yl]-3-pyridinyl]oxy]-, (1S,3S)-

References

1. Cheng PTW, et al. J Med Chem. 2021 Nov 11;64(21):15549-15581.

2. Corte TJ, et al. BMJ Open Respir Res. 2021 Dec;8(1):e001026.

Admilparant (BMS-986278, BMS986278)

Biological Activity

Physicochemical Properties

References

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