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PD173212

Catalog No. T16448   CAS 217171-01-2

PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol/kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.

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PD173212 Chemical Structure
PD173212, CAS 217171-01-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
2 mg In stock $ 64.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
25 mg In stock $ 333.00
50 mg In stock $ 497.00
100 mg In stock $ 693.00
500 mg In stock $ 1,450.00
1 mL * 10 mM (in DMSO) In stock $ 162.00
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Purity: 99.54%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol/kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.
Targets&IC50 VSCC:36 nM
In vitro PD 173212 blocked recombinant B-class (N-type) Ca+2 channels with a IC50 of 74 nM (N = 2), and blocked Na+ channels by 8% at 1 μM (N = 4), and blocked K+ channels by 10% at 1 μM (N = 4) in superior cervical ganglion neurons. PD 173212 effectively blocks recombinant B-class (N-type) calcium channel currents 78±7.8% (IC50: 74 nM), by whole-cell voltage-clamp techniques[1].
In vivo This study evaluated the effect of acute administration of the selective N-type Cav2.2 blocker PD17321238 in their visceral pain model. The test (VMR assessment) was performed on day 14 after DNBS injection. PD173212 (0.0017-1.7 μmol·kg−1, i.p.) dose-dependently reduced the visceral hypersensitivity induced by DNBS. The compound started to be effective at a dose of 0.017 μmol·kg−1 and completely relieved abdominal pain when administered at a ten-fold higher dose[2]. In the audiogenic seizure model, PD173212 (30 mg/kg, i.v.) displays moderate efficacy in preventing tonic seizures[1].
Molecular Weight 599.85
Formula C38H53N3O3
CAS No. 217171-01-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (150.0 mM)

TargetMolReferences and Literature

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. 2. Lucarini E, et al. Acute visceral pain relief mediated by A3AR agonists in rats: involvement of N-type voltage-gated calcium channels. Pain. 2020 Sep 1;161(9):2179-2190.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Neuronal Signaling Compound Library Bioactive Compound Library

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Keywords

PD173212 217171-01-2 Membrane transporter/Ion channel Metabolism Calcium Channel PD 173212 PD-173212 inhibitor inhibit

 

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