217171-01-2

217171-01-2 structure

Name: PD 173212
Chemical Name: (2S)-N-[(2S)-1-(tert-butylamino)-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-2-[(4-tert-butylphenyl)methyl-methylamino]-4-methylpentanamide
CAS Number: 217171-01-2
Molecular Formula: C₃₈H₅₃N₃O₃
Molecular Weight: 599.84600
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
Create Date: 2017-10-19 13:41:35
Modify Date: 2024-01-15 00:13:19
PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.

Name	(2S)-N-[(2S)-1-(tert-butylamino)-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-2-[(4-tert-butylphenyl)methyl-methylamino]-4-methylpentanamide
Synonyms	PD173212

Description	PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Neurological Disease
Target	IC50: 36 nM (VSCC)[1]
In Vitro	PD173212 (PD 173212, 300 nM) potently blocks recombinant B-class (N-type) calcium channel currents 78±7.8%, with an IC50 of 74 nM, by whole-cell voltage-clamp techniques. PD 173212 possesses selectivity for non L-type Ca2+ channels versus neuronal Na+, K+, and L-type Ca2+ channels[1].
In Vivo	PD173212 (30 mg/kg, i.v.) shows moderate efficacy in preventing tonic seizures in the audiogenic seizure model[1].
References	[1]. Hu LY, et al. Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2151-6.