BMS-986202|Tyk2 inhibitor|DC Chemicals

Cas No.:
Chemical Name:	BMS986202
Synonyms:	BMS986202;BMS-986202,BMS 986202
SMILES:	C1(C2N=CC(F)=CN=2)C=CC=C(NC2C=C(NC(=O)C3CC3)N=CC=2C(NC([2H])([2H])[2H])=O)C=1OC
Formula:	C₂₂H₂₁FN₆O₃
M.Wt:	439.456
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	J Med Chem . 2021 Jan 14;64(1):677-694. doi: 10.1021/acs.jmedchem.0c01698. Epub 2020 Dec 28.

Description:

BMS-986202 (BMS-986202, AM-152) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 18 and 9 nM in calcium mobilisation and β-arrestin assays; fully inhibits the response to LPA in calcium mobilisation, β-arrestin, cAMP, GTPγS and RhoA functional assays; BMS-986202 is currently in Phase II clinical trials for idiopathic pulmonary fibrosis.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC73453	ACT-1016-0707	ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.
DC70752	S1P5-IN-15	S1P5-IN-15 is a potent, selective, orally active and brain-penetrant S1P5 antagonist with IC50 of 0.1 nM, no effect on S1P1-4.
DC47017	Vibozilimod	Vibozilimod (example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1).
DC28233	CYM 50308	CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
DC10561	GSK-2018682	GSK-2018682 is a sphingosine 1 phosphate receptor (S1PR)-1 agonist potentially for the treatment of multiple sclerosis.
DC10923	TAK-615	TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays..
DC10925	SAR-100842	SAR-100842 (SAR100842) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 31 nM in β-arrestin assays.
DC10924	BMS986202	BMS-986202 is a clinical Tyk2 inhibitor that binds to Tyk2 JH2 with IC50 of 0.19 nM and shows remarkably selectivity over other kinases including Jak family members.
DC8622	AM095 free acid	AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
DC11754	AD 2900	AD 2900 (AD2900, AD-2900) is a novel potent, broad S1P receptor antagonist with IC50 of 3.8, 3.2, 6.2, 5.9 and 0.405 uM for S1P1, 2, 3, 4 and 5 respectively.

BMS986202