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Submit ReviewCD38 inhibitor 78c
Description: Potent CD38 inhibitor; active in vivo
Chemical Name: 4-[[trans-4-(2-Methoxyethoxy)cyclohexyl]amino]-1-methyl-6-(5-thiazolyl)-2(1H)-quinolinone
Purity: ≥98% (HPLC)
Biological Activity for CD38 inhibitor 78c
CD38 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.
Technical Data for CD38 inhibitor 78c
| M. Wt | 413.54 |
| Formula | C22H27N3O3S |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CD38 inhibitor 78c
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.35 | 100 |
Preparing Stock Solutions for CD38 inhibitor 78c
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for CD38 inhibitor 78c
References for CD38 inhibitor 78c
References are publications that support the biological activity of the product.
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.
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Keywords: 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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