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5.38763

Sigma-Aldrich

CD38 Inhibitor

≥98% (HPLC), solid, CD38 inhibitor, Calbiochem®

Synonym(s):

CD38 Inhibitor, Compound 78c, CD38i_78c, 78c, Cluster of Differentiation 38 Inhibitor

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About This Item

Empirical Formula (Hill Notation):
C22H27N3O3S
CAS Number:
Molecular Weight:
413.53
UNSPSC Code:
12352200
NACRES:
NA.77

product name

CD38 Inhibitor,

Assay

≥98% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light brown to brown
white to light brown

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

General 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.).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
CD38
Reversible: yes
Target IC50: 7.3 & 1.9 nM for human & mouse CD38, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Haffner, C.D., et al. 2015. J. Med. Chem.58, 3548.
Tarrago, M.G., et al. 2018 Cell. Metab.27, 1081.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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