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Submit ReviewCD38 inhibitor 78c is a potent CD38 (ADP ribosyl cyclase/hydrolase) inhibitor (IC50 values 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 NAD+ levels >5-fold in liver and >1.2-fold in muscle of diet-induced obese (DIO) C57Bl6 mice. Also prevents age-related NAD+ decline in mice. Improves glucose intolerance, cardiac function and improves physiological and metabolic parameters in old mice.
分子量 | 413.54 |
公式 | C22H27N3O3S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1700637-55-3 |
PubChem ID | 118736856 |
InChI Key | VJQALSOBHVEJQM-QAQDUYKDSA-N |
Smiles | COCCO[C@H]1CC[C@H](NC2=CC(N(C3=CC=C(C4=CN=CS4)C=C23)C)=O)CC1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 41.35 | 100 |
以下数据基于产品分子量 413.54。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.42 mL | 12.09 mL | 24.18 mL |
5 mM | 0.48 mL | 2.42 mL | 4.84 mL |
10 mM | 0.24 mL | 1.21 mL | 2.42 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
Tarrago et al (2018) A potent and specific CD38 inhibitor ameliorates age-related metabolic dysfunction by reversing tissue NAD+ decline. Cell Metab. 27 1081 PMID: 29719225
Haffner et al (2015) Discovery, synthesis, and biological evaluation of thiazoloquin(az)olin(on)es as potent CD38 inhibitors. J.Med.Chem. 58 3548 PMID: 25828863
If you know of a relevant reference for CD38 inhibitor 78c, please let us know.
关键词: CD38 inhibitor, CD38 inhibitor supplier, CD38, inhibitor, 78c, Potent, inhibitors, inhibits, ADP, ribosyl, cyclases, CD157, hydrolases, Other, Hydrolases, 6391, Tocris Bioscience
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