CD38 inhibitor 1 - ≥98%(HPLC), high purity , CAS No.1700637-55-3

  • ≥98%(HPLC)
Item Number
C287543
Grouped product items
SKUSizeAvailabilityPrice Qty
C287543-1mg
1mg
In stock
$35.90
C287543-5mg
5mg
In stock
$147.90
C287543-10mg
10mg
In stock
$256.90
C287543-25mg
25mg
In stock
$513.90
C287543-50mg
50mg
In stock
$870.90

Potent CD38 inhibitor; activein vivo

View related series
CD38 Immunology/Inflammation

Basic Description

SynonymsSY325926 | BCP31569 | 4-[[trans-4-(2-Methoxyethoxy)cyclohexyl]amino]-1-methyl-6-(5-thiazolyl)-2(1H)-quinolinone | compound 78c | E85684 | 5,12-NAPHTHACENEDIONE, 8-ACETYL-10-((3-AMINO-2,3,6-TRIDEOXY-.ALPHA.-L-LYXO-HEXOPYRANOSYL)OXY)-7,8,9,10-TETRAHYDRO-1,6
Specifications & Purity≥98%(HPLC)
Biochemical and Physiological MechanismsPotent CD38 (ADP ribosyl cyclase/hydrolase) inhibitor (IC50values 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 NA
Storage TempProtected from light,Store at -20°C
Shipped InIce chest + Ice pads
Product Description

product 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.).


Associated Targets(Human)

CD38 Tclin Lymphocyte differentiation antigen CD38 (364 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDCK (10148 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[[4-(2-methoxyethoxy)cyclohexyl]amino]-1-methyl-6-(1,3-thiazol-5-yl)quinolin-2-one
INCHI InChI=1S/C22H27N3O3S/c1-25-20-8-3-15(21-13-23-14-29-21)11-18(20)19(12-22(25)26)24-16-4-6-17(7-5-16)28-10-9-27-2/h3,8,11-14,16-17,24H,4-7,9-10H2,1-2H3
InChi Key VJQALSOBHVEJQM-UHFFFAOYSA-N
Canonical SMILES CN1C2=C(C=C(C=C2)C3=CN=CS3)C(=CC1=O)NC4CCC(CC4)OCCOC
Isomeric SMILES CN1C2=C(C=C(C=C2)C3=CN=CS3)C(=CC1=O)NC4CCC(CC4)OCCOC
PubChem CID 118736856
Molecular Weight 413.54

Certificates

Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
L2109475Certificate of AnalysisSep 11, 2024 C287543
L2109476Certificate of AnalysisSep 11, 2024 C287543
L2109477Certificate of AnalysisSep 11, 2024 C287543
L2109478Certificate of AnalysisSep 11, 2024 C287543
L2109479Certificate of AnalysisSep 11, 2024 C287543

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 41.35, Max Conc. mM: 100
SensitivityLight sensitive

Related Documents

Citations of This Product

1. Yang Guo, Yi-Hong Bao, Yang-Yang Chai.  (2019)  Preparation of microcapsule antioxidative wall materials of pine nut oil by the Maillard reaction.  JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE,  99  (6): (2793-2801).  [PMID:30430591] [10.1002/jsfa.9488]
2. Zhan Gao, Lei Zhu, Xinyao Zou, Chunpeng Liu, Bo Tian, Zhen Huang.  (2019)  Soot reduction effects of dibutyl ether (DBE) addition to a biodiesel surrogate in laminar coflow diffusion flames.  PROCEEDINGS OF THE COMBUSTION INSTITUTE,  37  (1265).  [PMID:] [10.1016/j.proci.2018.05.083]

References

1. Yang Guo, Yi-Hong Bao, Yang-Yang Chai.  (2019)  Preparation of microcapsule antioxidative wall materials of pine nut oil by the Maillard reaction.  JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE,  99  (6): (2793-2801).  [PMID:30430591] [10.1002/jsfa.9488]
2. Zhan Gao, Lei Zhu, Xinyao Zou, Chunpeng Liu, Bo Tian, Zhen Huang.  (2019)  Soot reduction effects of dibutyl ether (DBE) addition to a biodiesel surrogate in laminar coflow diffusion flames.  PROCEEDINGS OF THE COMBUSTION INSTITUTE,  37  (1265).  [PMID:] [10.1016/j.proci.2018.05.083]

Solution Calculators