Free shipping on all orders over $ 500

BMS-986278

Cat. No. M21207
BMS-986278 Structure
Size Price Availability Quantity
5mg USD 700  USD700 In stock
10mg USD 1100  USD1100 In stock
25mg USD 2200  USD2200 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

BMS-986278 is a potentially first-in-class, potent, small molecule LPA1 antagonist with a Kb of 6.9 nM that can be used in studies related to lung injury and pulmonary fibrosis.

Chemical Information
Molecular Weight 445.51
Formula C22H31N5O5
CAS Number 2170126-74-4
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Michael W Gill, et al. Toxicol Appl Pharmacol. Mechanism of hepatobiliary toxicity of the LPA1 antagonist BMS-986020 developed to treat idiopathic pulmonary fibrosis: Contrasts with BMS-986234 and BMS-986278

[2] L Sivaraman, et al. Toxicol Appl Pharmacol. Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA1) antagonists

[3] Tamera J Corte, et al. BMJ Open Respir Res. Phase 2 trial design of BMS-986278, a lysophosphatidic acid receptor 1 (LPA1) antagonist, in patients with idiopathic pulmonary fibrosis (IPF) or progressive fibrotic interstitial lung disease (PF-ILD)

[4] Peter T W Cheng, et al. J Med Chem. Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases

[5] Wenjie Liu, et al. Bioorg Chem. The development of modulators for lysophosphatidic acid receptors: A comprehensive review

Related LPL Receptor Products
Ceralifimod

Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.

CYM-5478 

CYM-5478 is a potent and highly selective S1P2 agonist with an EC50 of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity.

Mocravimod

Mocravimod is an oral activity amphematoshenol-1-1-phosphate receptor (S1PR) regulator, which can block the required signal from lymph organs to prevent the migration of effect cells from migrating to non-lymph hematopoietic tissue. Mocravimod can be used for cancer research.

CAY10444

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors.

SLF1081851 TFA 

SLF1081851 (TFA) is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 (TFA) plays a key role in development and immune system.

  Catalog
Abmole Inhibitor Catalog




Keywords: BMS-986278 supplier, LPL Receptor, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.