TRPM3 Agonist; CIM0216 1PC X 25MG

Biochem/physiol Actions

Reversible: yes

Primary TargetTRPM3

Cell permeable: yes

General description

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.

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)