5.34359

TRPM3 Agonist, CIM0216

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₂₁H₂₁N₃O₂
• Numero CAS: 1031496-06-6
• Peso molecolare: 347.41
• Numero MDL: MFCD00045972
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white to light yellow
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
TRPM3

Reversible: yes

Confezionamento

Packaged under inert gas

Altre note

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

Note legali

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

Esclusione di responsabilità

Toxicity: Standard Handling (A)

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable