CD38 inhibitor 1 - ≥98%(HPLC), high purity , CAS No.1700637-55-3

Item Number

C287543

• Synonyms: CD38 inhibitor 1 | 1700637-55-3 | CD38-IN-78c | 4-((trans-4-(2-Methoxyethoxy)cyclohexyl)amino)-1-methyl-6-(thiazol-5-yl)quinolin-2(1H)-one | CHEMBL3426034 | 4-(((1r,4r)-4-(2-Methoxyethoxy)cyclohexyl)amino)-1-methyl-6-(thiazol-5-yl)quinolin-2(1H)-one | compound 78c | MD
• Specifications & Purity: ≥98%(HPLC)
• Biochemical and Physiological Mechanisms: Potent CD38 (ADP ribosyl cyclase/hydrolase) inhibitor (IC50values are 1.9 and 7.3 nM at mouse and human CD38, respectively). Catalyzes breakdown of NAD to nicotinamide and ADPR, and hydrolyzes NAADP to adenosine-5'-O-diphosphoribose phosphate. Elevates NA
• Storage Temp: Protected from light,Store at -20°C
• Shipped In: Ice chest + Ice pads

Product Description

product description：

A cell-permeable, orally bioavailable, non-toxic thiazolyl-quinolinone derived compound that acts as a potent, selective and reversible inhibitor of CD38 (IC50 = 7.3 & 1.9 nM for human & mouse CD38, respectively; Ki = 0.3 nM for human wt-CD38). Shown to bind to the catalytic active site. Displays attractive PK properties in mice (p.o. 30 mg/kg: t1/2 = 3.5 h, Cmax = 10.8 µg/ml; i.v. 2 mg/kg: t1/2 = 5.3 h, Cmax = 2.98 µg/ml, Cl = 21 ml/min/kg, Vdss = 1.3 L/kg). Rapidly elevates NAD levels by several folds in both liver and gastrocnemius tissue in a diet induced obese mouse (30 mg/kg, p.o.).