CHEMBL1270208

For research purposes only

Cat. No BA20112015

Availability In Stock

Description of biological activity

The compound is a 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 was observed. [1] The oral administration of this blocker evokes the dose-dependent reversal of allodynia in the spinal nerve ligation model of neuropathic pain in rat. [1]

Therapeutic area

Analgesic

Biological target category

Voltage gated sodium channels

TECHNICAL INFORMATION

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

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

Chemical Formula: C20H15ClF3N3O2

SMILES: FC(F)(F)COc1ncccc1CNC(=O)c1cncc(c1)-c1ccc(Cl)cc1

CAS Number: 1026822-49-0

Molecular Weight: 421.800

Purity: >95%

Appearance: white powder

Solubility: DMSO

STORAGE AND HANDLING

Storage: Store at +20°C

Stability: Stable under normal condition.

Shipping Conditions: Shipped at room temperature.

USE PROTOCOL

Soluble in DMSO. If precipitate is observed, vortex for 5 minutes.

REFERENCES

1. Kort M. E. et al. Subtype-selective Nav1.8 sodium channel blockers: Identification of potent, orally active nicotinamide derivatives Bioorg. Med. Chem. Lett. 2010, 20, 6812. DOI: 10.1016/j.bmcl.2010.08.121

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