1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. AMG8379

AMG8379 

目录号: HY-108425
产品使用指南

AMG8379 是一种有效的、口服的、选择性的、电压门控钠通道 NaV1.7 拮抗剂, 对人和小鼠 NaV1.7 的 IC50 值分别为 8.5 和 18.6 nM。AMG8379 能可逆地阻断背根神经节 (DRG) 神经元内源性河豚毒素 (TTX) 敏感钠通道, IC50为 3.1 nM。

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AMG8379 Chemical Structure

AMG8379 Chemical Structure

CAS No. : 1642112-31-9

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Description

AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM[1].

In Vitro

AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons[1].
The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM[1].

In Vivo

AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior[1].

Animal Model: CD-1 male mice[1]
Dosage: 30 or 100 mg/kg body weight
Administration: Oral
Result: Showed a dose-dependent reduction in overall nociceptive behavior.
Molecular Weight

543.93

Formula

C₂₅H₁₆ClF₂N₃O₅S

CAS No.

1642112-31-9

SMILES

O=S(NC1=NOC=C1)(C2=CC(C=CC(N3C4=C(OC)C=C(C(F)=C4)C5=CC(Cl)=CC(F)=C5)=O)=C3C=C2)=O.[S]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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× = ×
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Keywords:

AMG8379AMG 8379AMG-8379Sodium ChannelNa channelsNa+ channelsselectiveoraldorsalrootgangliasulfonamideC-fibernociceptivepainitchInhibitorinhibitorinhibit

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AMG8379
目录号:
HY-108425
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