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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.).
Catalogue Number
538763
Brand Family
Calbiochem®
Synonyms
Compound 78c, CD38i_78c, 78c, Cluster of Differentiation 38 Inhibitor
References
References
Haffner, C.D., et al. 2015. J. Med. Chem.58, 3548. Tarrago, M.G., et al. 2018 Cell. Metab.27, 1081.
CD38 Inhibitor - CAS 1700637-55-3 - Calbiochem 分析证书
标题
批号
538763
参考
参考信息概述
Haffner, C.D., et al. 2015. J. Med. Chem.58, 3548. Tarrago, M.G., et al. 2018 Cell. Metab.27, 1081.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
15-July-2019 JSW
Synonyms
Compound 78c, CD38i_78c, 78c, Cluster of Differentiation 38 Inhibitor
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.).
Form
White to light brown to brown solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1700637-55-3
Chemical formula
C₂₂H₂₇N₃O₃S
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Haffner, C.D., et al. 2015. J. Med. Chem.58, 3548. Tarrago, M.G., et al. 2018 Cell. Metab.27, 1081.
