5.34359

TRPM3 Agonist, CIM0216

• Synonyme(s) : TRPM3 Agonist, CIM0216, ±-2-(3,4-Dihydroquinolin-1(2H)-yl)-N-(5-methylisoxazol-3-yl)-2-phenylacetamide, Transient Receptor Potential Cation Channel subfamily M member 3 Agonist, CIM-0216
• Formule empirique (notation de Hill): C₂₁H₂₁N₃O₂
• Numéro CAS: 1031496-06-6
• Poids moléculaire : 347.41
• Code UNSPSC : 51111800
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white to light yellow
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

A cell-permeable isoxazolyl-phenylacetamide based compound that acts as a potent, reversible, temperature-dependent and selective activator of both human and murine TRPM3 currents (EC₅₀ = 770 nM for elevating [Ca²⁺]_i levels in HEK293-TRPM3 cells; maximal activation within ~100 s) in a dose-dependent & membrane-delimited manner. Poorly activates human TRPM1, TRPM2, TRPM4, TRPM5, TRPM6, TRPM7, TRPM8 and TRPV1. At higher concentrations, blocks hTRPM2, hTRPM5 & hTRPM8 (by 17%, 34% & 61%, respectively, at 10 µM). Elicits the opening of both the central calcium-conducting pore and the alternative cation permeation pathway. Causes nocifensive behavior in mice (2.5 nmol, intradermal), induces pain, and stimulates the release of CGRP from skin nerve terminals and insulin from pancreatic islets. Shown to display greater efficacy than the canonical TRPM3 agonist, pregnenolone sulfate.

A cell-permeable isoxazolyl-phenylacetamide based compound that acts as a potent, reversible, temperature-dependent and selective activator of both human and murine TRPM3 currents (EC₅₀ = 770 nM for elevating [Ca²⁺]_i levels in HEK293-TRPM3 cells; maximal activation within ~100 s) in a dose-dependent & membrane-delimited manner. Poorly activates human TRPM1, TRPM2, TRPM4, TRPM5, TRPM6, TRPM7, TRPM8 and TRPV1. At higher concentrations, blocks hTRPM2, hTRPM5 & hTRPM8 (by 17%, 34% & 61%, respectively, at 10 µM). Elicits the opening of both the central calcium-conducting pore and the alternative cation permeation pathway. Causes nocifensive behavior in mice (2.5 nmol, intradermal), induces pain, and stimulates the release of CGRP from skin nerve terminals and insulin from pancreatic islets. Shown to display greater efficacy than the canonical TRPM3 agonist, pregnenolone sulfate.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
TRPM3

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

Held, K., et al. 2015. Proc. Natl. Acad. Sci. USA.112, E1363.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable