| Bioactivity | 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]. |
| Invitro | 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: |
| Name | AMG8379 |
| CAS | 1642112-31-9 |
| Formula | C25H16ClF2N3O5S |
| Molar Mass | 543.93 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kornecook TJ, et al. Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7. J Pharmacol Exp Ther. 2017 Jul;362(1):146-160. |
AMG8379
CAS: 1642112-31-9 F: C25H16ClF2N3O5S W: 543.93
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with
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