PD 173212

An N-type calcium channel blocker

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10mg

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货号: ajci7598
CAS: 217171-01-2
别名: N-[[4-叔丁基苯基]甲基]-N-甲基-L-亮氨酰-N-叔丁基-O-苄基-L-酪氨酰胺
分子式: C38H53N3O3
分子量: 599.85
纯度: >98%
溶解度: DMSO: 100 mM,Ethanol: 100 mM
储存: Store at -20°C
库存: 现货

Background

PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.

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].

PD173212 (30 mg/kg, i.v.) shows moderate efficacy in preventing tonic seizures in the audiogenic seizure model[1].

参考文献:
[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.