AMG8379 - CAS# 1642112-31-9


Catalog No. Size PriceQuantity
M15828-C Contact sales@xcessbio.com for quotation $100

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.

Product information

CAS Number: 1642112-31-9

Molecular Weight: 543.93

Formula: C25H16ClF2N3O5S

Chemical Name: (1R)-1-(3'-Chloro-2, 5'-difluoro-5-methoxy-4-biphenylyl)-N-3-isoxazolyl-2-oxo-1, 2-dihydro-6-quinolinesulfonamide

Smiles: COC1=CC(=C(F)C=C1N1C(=O)C=CC2=CC(=CC=C12)S(=O)(=O)NC1C=CON=1)C1C=C(F)C=C(Cl)C=1

InChiKey: HXQNEKJQBGXFAG-UHFFFAOYSA-N

InChi: InChI=1S/C25H16ClF2N3O5S/c1-35-23-12-19(15-8-16(26)11-17(27)9-15)20(28)13-22(23)31-21-4-3-18(10-14(21)2-5-25(31)32)37(33,34)30-24-6-7-36-29-24/h2-13H,1H3,(H,29,30)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

In Vivo:

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

Products are for research use only. Not for human use.

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