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cim0216

Catalog No. T9263 CAS 1031496-06-6

Synonyms: N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide

CIM0216 is a synthetic TRPM3 activator whose potency and apparent affinity greatly exceeds that of the canonical TRPM3 agonist.

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cim0216, CAS 1031496-06-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 84.00
10 mg	In stock	$ 148.00
25 mg	In stock	$ 313.00
50 mg	In stock	$ 490.00
100 mg	In stock	$ 738.00
500 mg	In stock	$ 1,530.00
1 mL * 10 mM (in DMSO)	In stock	$ 93.00

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Purity: 99.6%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

CIM0216 is a synthetic TRPM3 activator whose potency and apparent affinity greatly exceeds that of the canonical TRPM3 agonist.

In vitro

CIM0216 Selectively Activates TRPM3 in Stably Transfected HEK293 Cells.A diverse small-molecule library was screened for compounds that modulate TRPM3-mediated Ca2+ responses in HEK293 cells stably expressing murine TRPM3 (HEK-TRPM3 cells), as described previously[1].In HEK-TRPM3 cells, CIM0216 elicited a dose-dependent Ca2+ response [negative logarithm of the EC50 value (pEC50) = 0.77 ± 0.1 μM], which was not observed in nontransfected HEK293 cells . The endogenous TRPM3 activator pregnenolone sulfate (PS) also elicited a dose-dependent Ca2+ response, typified by a smaller Ca2+ influx and a fivefold lower potency (pEC50 = 3.0 ± 0.1 μM; n = 2) compared with CIM0216 . In the presence of 40 μM PS, the dose dependency of CIM0216 shifted to a lower concentration in HEK-TRPM3 cells (pEC50 = 42 ± 0.6 nM CIM0216 in the presence of PS). Single-cell FURA2-ratiometric Ca2+ imaging revealed a robust increase in intracellular Ca2+ concentration (1,145 ± 26 nM; n = 603 from at least three independent measurements) on stimulation with 1 μM CIM0216 in all HEK-TRPM3 cells. These responses were not observed in nontransfected HEK cells (n = 166) or in the absence of extracellular Ca2+.

Synonyms	N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide
Molecular Weight	347.41
Formula	C21H21N3O2
CAS No.	1031496-06-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (86.35 mM), Sonication and heating are recommended.

Ethanol: 17 mg/mL (48.93 mM), Sonication and heating are recommended.

References and Literature

1. Vriens J , Owsianik G , Hofmann T , et al. TRPM3 is a nociceptor channel involved in the detection of noxious heat.[J]. Neuron, 2011, 70(3):482-494.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Bioactive Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Ion Channel Inhibitor Library

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Related compounds with same targets

WS-12 TC-I2000 AMG 517 α-Spinasterol EIPA SB-705498 SN 2 PF-4840154

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

cim0216 1031496-06-6 Membrane transporter/Ion channel TRP/TRPV Channel N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide cim-0216 inflammation inhibit TRP Channel Transient receptor potential channels sensory nerve neurogenic TRPM3 Inhibitor CIM 0216 inhibitor

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