JAMI1001A

JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.

Product information

CAS Number: 1001019-46-0

Molecular Weight: 402.39

Formula: C16H17F3N4O3S

Chemical Name: 2-{2-[4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetamido}-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide

Smiles: NC(=O)C1=C(NC(=O)CN2C=C(CO)C(=N2)C(F)(F)F)SC2CCCCC=21

InChiKey: ZGRBZBGNPZBNLW-UHFFFAOYSA-N

InChi: InChI=1S/C16H17F3N4O3S/c17-16(18,19)13-8(7-24)5-23(22-13)6-11(25)21-15-12(14(20)26)9-3-1-2-4-10(9)27-15/h5,24H,1-4,6-7H2,(H2,20,26)(H,21,25)

Technical Data

Appearance: Solid Power

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

Solubility: Soluble in DMSO

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:

JAMI1001A binds in the solvent accessible allosteric pocket that lies at the interface between AMPA receptor ligand-binding core dimers. JAMI1001A efficaciously blocks channel desensitization and slows deactivation of the flip and flop isoforms of AMPA receptor GluA2. A simple kinetic model suggests that JAMI1001A independently modulates both the protein rearrangements necessary for channel desensitization and its recovery from the desensitized state, and the protein rearrangements necessary for channel deactivation (closed-cleft stability or channel gating).

References:

1. Harms JE, Benveniste M, Maclean JK, Partin KM, Jamieson C. Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy. Neuropharmacology. 2013 Jan;64:45-52.

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