CD38 inhibitor 78c

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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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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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