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Merck

5.34359

TRPM3 Agonist, CIM0216

Sinónimos:

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

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Fórmula empírica (notación de Hill):
C21H21N3O2
Número CAS:
Peso molecular:
347.41
MDL number:
NACRES:
NA.77
UNSPSC Code:
51111800
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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assay

≥97% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white to light yellow

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
TRPM3
Reversible: yes

Packaging

Packaged under inert gas

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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