CIM0216 is a synthetic TRPM3 ligand and a potent and specific TRPM3 agonist. CIM0216 is more selective for TRPM3 than TRPM1, TRPM2, and TRPM4-8. CIM0216 causes pain and evokes neuropeptide release from sensory nerve terminals in a TRPM3-dependent manner. CIM0216 is a potent tool for studying the physiological functions of TRPM3 and can be used for related research on neurogenic inflammation.

Physicochemical Properties

Molecular Formula	C21H21N3O2
Molecular Weight	347.410344839096
Exact Mass	347.163
CAS #	1031496-06-6
PubChem CID	42887770
Appearance	White to yellow solid powder
Density	1.3±0.1 g/cm3
Boiling Point	608.7±55.0 °C at 760 mmHg
Flash Point	321.9±31.5 °C
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.646
LogP	3.18
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	4
Heavy Atom Count	26
Complexity	480
Defined Atom Stereocenter Count	0
InChi Key	KSEXDSJYVSEVGF-UHFFFAOYSA-N
InChi Code	InChI=1S/C21H21N3O2/c1-15-14-19(23-26-15)22-21(25)20(17-9-3-2-4-10-17)24-13-7-11-16-8-5-6-12-18(16)24/h2-6,8-10,12,14,20H,7,11,13H2,1H3,(H,22,23,25)
Chemical Name	2-(3,4-dihydro-2H-quinolin-1-yl)-N-(5-methyl-1,2-oxazol-3-yl)-2-phenylacetamide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro

In HEK-TRPM3 cells, CIM0216 induced a dose-dependent Ca2+ response [pEC50=0.77±0.1 μM], which was not seen in HEK293 cells that were not transfected. In HEK-TRPM3 single-cell FURA2 ratio Ca2+ inference, CIM0216 significantly raises intracellular Ca2+ concentration (1,145±26 nM). In the absence of exogenous Ca2+ or in untransfected HEK cells, these reactions were not seen[1]. CIM0216 (10 μM) did neither stimulate or inhibit TRPM1, TRPM4, TRPM6, or TRPM7 currents. However, it did cause a slight foaming effect when TRPM2 (16.6% foam) and TRPM5 (33.5% foam) were activated. The activation of the human TRPV1 and TRPM8 channels is also not affected by CIM0216 [1].

References

[1]. Activation of TRPM3 by a potent synthetic ligand reveals a role in peptide release. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):E1363-72.

Solubility Data

Solubility (In Vitro)

DMSO : ~35 mg/mL (~100.75 mM) Ethanol : ~17 mg/mL (~48.93 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.8784 mL	14.3922 mL	28.7844 mL
	5 mM	0.5757 mL	2.8784 mL	5.7569 mL
	10 mM	0.2878 mL	1.4392 mL	2.8784 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.