A778317


CAS No. : 808756-64-1

A778317,808756-64-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000290
Synonyms:A778317;1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-isoquinolin-5-ylurea
Molecular Formula:C23H25N3O
Molecular Weight:359.473
Target:TRPV1
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Appearance:Solid powder
Purity: > 98%
Cat No:I000290
Cas No:808756-64-1
Product-Name:A778317
InChI:InChI=1S/C23H25N3O/c1-23(2,3)17-8-9-18-15(13-17)7-10-21(18)26-22(27)25-20-6-4-5-16-14-24-12-11-19(16)20/h4-6,8-9,11-14,21H,7,10H2,1-3H3,(H2,25,26,27)/t21-/m1/s1
InChIKey:VPSCJCQPUGKRNC-OAQYLSRUSA-N
SMILES:O=C(NC1=CC=CC2=C1C=CN=C2)N[C@@H]3CCC4=C3C=CC(C(C)(C)C)=C4
A778317(cas 808756-64-1) is a novel, stereoselective, high-affinity antagonist that potently blocks transient receptor potential vanilloid-1 (TRPV1) receptor-mediated changes in intracellular calcium concentrations (pIC50 = 8.31 ± 0.13).
1: Bianchi BR, El Kouhen R, Chen J, Puttfarcken PS. Binding of [(3)H]A-778317 to native transient receptor potential vanilloid-1 (TRPV1) channels in rat dorsal root ganglia and spinal cord. Eur J Pharmacol. 2010 May 10;633(1-3):15-23. doi: 10.1016/j.ejphar.2010.02.004. Epub 2010 Feb 11. PubMed PMID: 20153316.
2: Bianchi BR, El Kouhen R, Neelands TR, Lee CH, Gomtsyan A, Raja SN, Vaidyanathan SN, Surber B, McDonald HA, Surowy CS, Faltynek CR, Moreland RB, Jarvis MF, Puttfarcken PS. [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J Pharmacol Exp Ther. 2007 Oct;323(1):285-93. Epub 2007 Jul 27. PubMed PMID: 17660385.
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