Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
SKU | Size | Availability | Price | 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
Synonyms | SY325926 | 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 Mechanisms | Potent 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 Temp | Protected from light,Store at -20°C |
Shipped In | Ice 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.). |
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
---|
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 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
L2109475 | Certificate of Analysis | Sep 11, 2024 | C287543 |
L2109476 | Certificate of Analysis | Sep 11, 2024 | C287543 |
L2109477 | Certificate of Analysis | Sep 11, 2024 | C287543 |
L2109478 | Certificate of Analysis | Sep 11, 2024 | C287543 |
L2109479 | Certificate of Analysis | Sep 11, 2024 | C287543 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 41.35, Max Conc. mM: 100 |
---|---|
Sensitivity | Light sensitive |
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] |
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] |