For research purposes only

Cat. No BA94673207

Availability Please, check stock availability.

Description of biological activity

Chemokine Receptors CXCR4 and CXCR7 blocker. In a radioligand assay [WO2007/115232 A2, 2007] using a labeled natural chemokine, 25I-labeled SDF-I, the compound showed EC50 < 1000 nm/l for both receptors (on Cell Lines CEM-Nkr, CCRF-CEM, Jurkat, Molt-4 all endogenously expressing CXCR4, were used in assays for CXCR4 and MCF-7 cells and/or MDA-MB-435S cells for CXCR7).

Keywords: Others Anti-cancer

TECHNICAL INFORMATION

2-(8-Methoxy-5-methyl-4-oxo-4,5-dihydro-pyrazolo[4,3-c]quinolin-1-yl)- N-[2-(octahydro-quinolin-1-yl)-ethyl]-acetamide Chemokine Receptors CXCR4 and CXCR7 blocker.

IUPAC Name: 2-(8-Methoxy-5-methyl-4-oxo-4,5-dihydro-pyrazolo[4,3-c]quinolin-1-yl)- N-[2-(octahydro-quinolin-1-yl)-ethyl]-acetamide

Purity: > 96% chemical purity (LCMS)

1H-NMR spectrum (click to enlarge)

REFERENCES

Latest added compounds

5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione

Selective inhibitor of MCT1 with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited.

Anti-cancer

Inhibitors

 
5-(4-chlorophenyl)-N-{[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl}pyridine-3-carboxamide

selective inhibitor of Nav1.8 sodium channel (IC50 = 3 nM); for TRPV1, P2X2/3, Cav2.2 calcium channels, KCNQ2/3 potassium channels IC50 >10 µM

Analgesic

Inhibitors

 
1-[4-chloro-3-(trifluoromethyl)benzenesulfonyl]-4-[4-(5-methyl-1H-pyrazol-1-yl)benzoyl]piperazine

inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1)

Bone disorders

Inhibitors