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534359 TRPM3 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.

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Sinonimi: ±-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

Primary Target: TRPM3
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534359
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CAS #Empirical Formula
1031496-06-6C₂₁H₂₁N₃O₂

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5343590001
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      Description
      OverviewA 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 Number534359
      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
      DescriptionTRPM3 Agonist, CIM0216
      References
      ReferencesHeld, K., et al. 2015. Proc. Natl. Acad. Sci. USA. 112, E1363.
      Product Information
      CAS number1031496-06-6
      FormWhite to light yellow solid
      Hill FormulaC₂₁H₂₁N₃O₂
      Chemical formulaC₂₁H₂₁N₃O₂
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetTRPM3
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Numero di catalogo GTIN
      5343590001 04054839059247