AMG-517 is a potent, selective TRPV1 antagonist that inhibits Capsaicin, Proton, and thermal activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM, and 1.3 nM, respectively.

 

Brand: BCM

 

Target: TRPV1（capsaicin）:0.62 nM, TRPV1（heat activation）:1.3 nM, TRPV1（proton）:0.76 nM

 

In Vitro: AMG 517 inhibits CAP- (500 nM), acid- (pH 5.0), or heat-(45 °C) induced 45Ca2+ influx into human TRPV1-expressing CHO Cells with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. AMG 517 blocks capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells similarly. AMG 517 inhibits native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 nM. AMG 517 is a competitive antagonist of both rat and human TRPV1 with dissociation constant (Kb) values of 4.2 and 6.2 nM, respectively. AMG 517 is a highly selective TRPV1 antagonist. The IC50 value for AMG 517 is >20 μM against 2-APB-activated TRPV2 and TRPV3, 4-αPDD-activated TRPV4, allyl isothiocyanate-activated TRPA1, and icilin-activated TRPM8 in cell-based assays that measure agonist-induced increases in intracellular calcium in CHO cells recombinantly expressing the appropriate TRP channel.

 

Melting Point: 227℃

 

pKa: 10.19±0.70(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

Isomeric SMILES: CC(=O)NC1=NC2=C(C=CC=C2S1)OC3=NC=NC(=C3)C4=CC=C(C=C4)C(F)(F)F  

 

InChIKey: YUTIXVXZQIQWGY-UHFFFAOYSA-N  

 

InChI: InChI=1S/C20H13F3N4O2S/c1-11(28)26-19-27-18-15(3-2-4-16(18)30-19)29-17-9-14(24-10-25-17)12-5-7-13(8-6-12)20(21,22)23/h2-10H,1H3,(H,26,27,28)

 

Attribute
[Chem Name]	N-[4-[6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl]oxy-1,3-benzothiazol-2-yl]acetamide
[Synonym]	AMG-517; AMG 517
[CAS No.]	659730-32-2
[MDL No.]	MFCD14584859
[Formula]	C20H13F3N4O2S
[Molecular]	430.4
[Form]	Solid powder
[Storage]	Sealed in dry. Store in freezer, under -20°C

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