GSK2973980A is a novel, potent and selective inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with an IC50 of 3 nM. DGAT1 plays an important role in triglyceride synthesis and is a target of interest for the treatment of metabolic disorders. GSK2973980A has excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in […]

BMS-066 is a novel and potent tricyclic pseudokinase inhibitors of IKKβ/Tyk2 with IC50s of 9 nM and 72 nM, respectively. It demonstrates potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease.

BMS-346567, an analog of Sparsentan, is a novel, potent and selective dual angiotensin II and endothelin A receptor antagonist. BMS-346567 demonstrated superiority over irbesartan (an AT(1) receptor antagonist) in the normal SHR model of hypertension in a dose-dependent manner, demonstrating the synergy of AT(1) and ET(A) receptor blockade in a single molecule. Sparsentan (formerly known […]

BMS-986163, a novel water-soluble phosphate prodrug of BMS-986169 designed for IV administration, is a negative allosteric modulator of GluN2B which is a N-methyl-d-aspartate receptor subtype. The prodrug BMS-986163 can be rapidly convertd to its active form BMS-986169 which has Ki of 4 nM and IC50 of 24 nM. BMS-986163 has potential to be used in […]

TBK1 PROTAC 1 is a novel, potent and selective TBK1 PROTAC with DC50 of 12nM that selectively degrades TBK1 with excellent selectivity against a related kinase IKKε; It is a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells. Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase […]

BMS-986169 is a novel and potent negative allosteric modulator of GluN2B which is a N-methyl-d-aspartate receptor subtype. BMS-986169 has potential to be used in major depressive disorder. BMS-986169 exhibited high binding affinity for the GluN2B allosteric site (Ki = 4.0 nM) and selective inhibition of GluN2B receptor function (IC50 = 24 nM) in cells. BMS-986169 […]

Sofosbuvir D6 is the deuterated form and less active impurity of Sofosbuvir. Sofosbuvir (also known as PSI-7977, GS-7977; trade names Sovaldi and Virunon) is a HCV NS5B polymerase inhibitor that is used for the treatment of chronic hepatitis C virus (HCV) infection. Sofosbuvir acts by inhibiting the RNA polymerase that the hepatitis C virus uses […]

Peliglitazar is a novel dual α/γ PPAR (peroxisome proliferator-activated receptor) activator. The major clearance pathway of peliglitazar was through biliary elimination of glucuronide conjugates, which were hydrolyzed to peliglitazar and its oxidative metabolites in the intestines before excretion.

KRN 7000 is a novel, potent and selective synthetic α-galactosylceramide which activates NKT immune cells by association with the antigen-presenting CD1d protein. As these cells have important roles in the rejection of malignant tumors and in the regulation of several autoimmune diseases, KRN 7000 has activity in many diseases, including cancer, lupus, diabetes, malaria, and […]

Garenoxacin mesylate (formerly known as T-3811ME; BMS-284756; tradename: Geninax), the mesylate salt of Garenoxacin, is a novel and orally bioavailable quinolone antibiotic effective against both Gram-positive and Gram-negative bacterial infections.