CIM-0216

Cat No.:V10450 Purity: ≥98%

COA Product Data Instructions for use SDS

CIM0216 is a synthetic TRPM3 ligand and a potent and specific TRPM3 agonist.

CIM-0216 Chemical Structure CAS No.: 1031496-06-6
Product category: New1

This product is for research use only, not for human use. We do not sell to patients.

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Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

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.

Biological Activity I Assay Protocols (From Reference)

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.

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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

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)

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.)

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.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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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.

Note： (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.

Biological Data

CIM0216 activates TRPM3 in HEK-TRPM3 cells. (A) Chemical structure of CIM0216. (B) [Ca2+]I was monitored using Fluo-4 AM in HEK-TRPM3 cells before and after the addition of different concentrations of PS (black), CIM0216 (blue), and PS plus CIM0216 (red). Responses were measured as peak increases in fluorescence minus basal, expressed relative to a maximum PS response, and are given as mean ± SEM. n = 2. (C) Time course of Ca2+ imaging measurements in HEK293 cells stably expressing TRPM3 (HEK-TRPM3 cells) and nontransfected (NT) HEK293 cells during application of PS (40 µM) and CIM0216 (1 µM). (D) Time course at ±80 mV of a whole-cell patch-clamp recording on HEK-TRPM3 cells treated with PS (40 µM) and CIM0216 (1 µM), (E) I–V traces corresponding to the time points indicated in D. (F) Time course at ±80 mV of a whole-cell patch-clamp recording showing the application of PS and CIM0216 on nontransfected HEK293 cells. Mean ± SEM values are shown; n = 5. (G) Time course at ±80 mV of whole-cell patch-clamp measurement on HEK-TRPM3 cells presenting the block of CIM0216-induced currents by isosakuranetin (5 µM). (H) Time course at ±80 mV of a patch-clamp recording in whole-cell configuration showing CIM0216 dose-dependent activation of TRPM3 currents in HEK-TRPM3 cells. (I) Dose–response curves of CIM0216 (blue) and PS (black) in HEK-TRPM3. n = 5. Unless indicated otherwise, standard compound concentrations were 40 µM for PS and 1 µM for CIM0216.

Reduced CIM0216 responses in TRPM3-deficient sensory neurons. (A–C) Representative traces showing typical patterns of intracellular Ca2+ in DRG and TGN from control animals Trpm3+/+ (A), Trpm3−/− (B), and Trpa1−/− (C) mice in response to PS (20 µM), CIM0216 (1 µM), MO (100 µM), capsaicin (Cap; 1 µM), and K+ (50 mM). (D) Percentage of sensory neurons derived from TRPM3+/+, TRPM3−/−, and TRPA1−/− mice responding to stimulation by PS (20 µM), CIM0216 (1 µM), MO (100 µM), and capsaicin (1 µM). (E) Percentage of sensory neurons responding to CIM0216 in preparations from TRPM3+/+, TRPM3−/−, and TRPA1−/− mice. Different colors correspond to the different subtypes of CIM0216 responders based on PS and MO sensitivity. (F) Representative traces showing typical response patterns of intracellular Ca2+ in DRG and TGN from control animals in response to CIM0216 (1 µM), MO, and high K+. At the indicated time bar, the TRPM3 blocker isosakuranetin (5 µM) was added.

Synergistic effects of heat and CIM0216 on TRPM3. (A) Typical examples of the intracellular calcium increase induced by low doses of CIM0216 (0.1 µM) applied at room temperature (22 °C) and 37 °C in HEK-TRPM3 cells. (B) Bar diagram showing average Ca2+ increases in response to CIM0216 (0.1 µM), heat stimulus (37 °C), and CIM0216 (0.1 µM) at 37 °C. The open bar illustrates the calculated summation of CIM0216 and heat response. The red bar shows the measured value of combined application of heat and CIM0216, illustrating the supra-additive effect of heat on CIM0216 stimulation. n > 42 cells from at least three independent measurements. Data are presented as mean ± SEM.