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534359
Sigma-AldrichTRPM3 Agonist, CIM0216 - CAS 1031496-06-6 - Calbiochem
Highly efficacious TRPM3 Agonist that opens both the central Ca2+-conducting pore and the alternative cation permeation pathway. Causes nocifensive behavior in mice.
More>>Highly efficacious TRPM3 Agonist that opens both the central Ca2+-conducting pore and the alternative cation permeation pathway. Causes nocifensive behavior in mice. Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
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.
Catalogue Number
534359
Brand Family
Calbiochem®
Synonyms
±-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
Description
TRPM3 Agonist, CIM0216
References
References
Held, K., et al. 2015. Proc. Natl. Acad. Sci. USA.112, E1363.
TRPM3 Agonist, CIM0216 - CAS 1031496-06-6 - Calbiochem Certificates of Analysis
Title
Lot Number
534359
References
Reference overview
Held, K., et al. 2015. Proc. Natl. Acad. Sci. USA.112, E1363.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
18-October-2024 JSW
Synonyms
±-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
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.
Form
White to light yellow solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1031496-06-6
Chemical formula
C₂₁H₂₁N₃O₂
Purity
≥97% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light +2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Held, K., et al. 2015. Proc. Natl. Acad. Sci. USA.112, E1363.