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SML3630

Sigma-Aldrich

MK-0159

≥98% (HPLC)

Synonym(s):

MK 0159, MK0159, N-((1r,4r)-4-(2-Methoxyethoxy)cyclohexyl)-6-(thiazol-5-yl)-1H-pyrrolo[2,3-b]pyridine-4-carboxamide, N-[trans-4-(2-Methoxyethoxy)cyclohexyl]-6-(5-thiazolyl)-1H-pyrrolo[2,3-b]pyridine-4-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C20H24N4O3S
CAS Number:
2641484-61-7
Molecular Weight:
400.49
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(C1=C2C(NC=C2)=NC(C3=CN=CS3)=C1)N[C@H]4CC[C@@H](CC4)OCCOC

Biochem/physiol Actions

MK-0159 is an orally active, potent and selective CD38 inhibitor (h/m/r CD38 IC50 = 22/3/70 nM) that increases extra- and intracellular NAD+ levels in high CD38-expressing human epithelial A549 cultures, as well as intracellular NAD+/NADP+ in HMVECs (0.3-50 µM). MK-0159 (3-30 mg/kg p.o.) increases systemic NAD+ and decreases ADPR levels in mice, providing protection from myocardial damage upon cardiac I/R injury in vivo (30 mg/kg p.o.).

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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Ping-Min Chen et al.
Science advances, 8(24), eabo4271-eabo4271 (2022-06-16)
Infection is one of the major causes of mortality in patients with systemic lupus erythematosus (SLE). We previously found that CD38, an ectoenzyme that regulates the production of NAD+, is up-regulated in CD8+ T cells of SLE patients and correlates
Bharat Lagu et al.
Journal of medicinal chemistry, 65(13), 9418-9446 (2022-06-29)
CD38 is one of the major nicotinamide adenine dinucleotide (NAD+)- and nicotinamide adenine dinucleotide phosphate (NADP+)-consuming enzymes in mammals. NAD+, NADP+, and their reduced counterparts are essential coenzymes for numerous enzymatic reactions, including the maintenance of cellular and mitochondrial redox

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