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| Targets |
TRPM3 (Transient Receptor Potential cation channel subfamily M member 3). CIM-0216 is a synthetic TRPM3 ligand that acts as a potent and selective agonist of TRPM3. It exhibits selectivity for TRPM3 over TRPM1, TRPM2, and TRPM4-8. The compound activates the TRPM3 channel, leading to cation influx and cellular depolarization.
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| 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].
In vitro, CIM-0216 selectively activates TRPM3 in stably transfected HEK293 cells. Its potency and apparent affinity greatly exceed that of the canonical TRPM3 agonist. The compound exhibits selectivity for TRPM3 over TRPM1, TRPM2, and TRPM4-8. Its activity has been characterized in various calcium imaging and electrophysiological assays. |
| ln Vivo |
In vivo activity of CIM-0216 is not extensively documented. As a TRPM3 activator, it may have effects on pain perception, insulin secretion, and other TRPM3-mediated physiological processes. However, detailed in vivo studies in animal models are limited. The compound is primarily used as a research tool to study TRPM3 function.
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| Enzyme Assay |
In vitro TRPM3 activation assays for CIM-0216 involve measuring calcium influx in cells expressing TRPM3. HEK293 cells stably transfected with TRPM3 are treated with CIM-0216 at varying concentrations (typically 0.1-100 µM), and intracellular calcium levels are measured using fluorescent indicators such as Fura-2 or Fluo-4. EC50 values are determined from dose-response curves. Electrophysiological recordings using patch-clamp techniques can also be performed.
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| Cell Assay |
Cellular assays for CIM-0216 involve culturing HEK293 cells expressing TRPM3 or other TRPM channels. Cells are treated with CIM-0216 at varying concentrations, and calcium influx is measured using fluorescent indicators. Selectivity for TRPM3 over other TRPM channels is assessed by comparing activity in cells expressing different TRPM subtypes. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo animal studies for CIM-0216 are not extensively documented. When performed, they typically involve administration in rodent models to study TRPM3-mediated effects on pain, thermoregulation, or insulin secretion. The compound is typically administered via injection. Dosing regimens vary depending on the study objectives.
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| ADME/Pharmacokinetics |
CIM-0216 has a molecular weight of 347.41 g/mol and a molecular formula of C21H21N3O2. Its chemical name is ±-2-(3,4-dihydroquinolin-1(2H)-yl)-N-(5-methylisoxazol-3-yl)-2-phenylacetamide. The compound is soluble in DMSO and should be stored at -20°C protected from light. It is available with a purity of ≥99%. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
CIM-0216 is generally considered safe for research use at appropriate concentrations. Comprehensive toxicological data are limited. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
CIM-0216 is a synthetic TRPM3 activator with potency and affinity greatly exceeding that of the canonical TRPM3 agonist. It is selective for TRPM3 over TRPM1, TRPM2, and TRPM4-8. The compound is used as a research tool to study TRPM3 function. It is not approved for clinical use and is available for research purposes only.
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| Molecular Formula |
C21H21N3O2
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| Molecular Weight |
347.410344839096
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| Exact Mass |
347.163
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| CAS # |
1031496-06-6
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| PubChem CID |
42887770
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
608.7±55.0 °C at 760 mmHg
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| Flash Point |
321.9±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
3.18
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
480
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KSEXDSJYVSEVGF-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
2-(3,4-dihydro-2H-quinolin-1-yl)-N-(5-methyl-1,2-oxazol-3-yl)-2-phenylacetamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~35 mg/mL (~100.75 mM)
Ethanol : ~17 mg/mL (~48.93 mM) |
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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