Art. -Nr.: HY-108461

TRPM8-IN-1

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TRPM8-IN-1 (example 14) is an inhibitor of transient receptor potential melastatin-8 (TRPM8) channels, IC₅₀<5 μM.

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Reinheit: 99.44%
CAS. Nr.: 1159996-20-9
Formel: C₂₃H₁₈F₄N₂O
Molecular Weight:414.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TRPM8-IN-1 Chemical Structure

CAS. Nr.: 1159996-20-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

TRPM8-IN-1 (example 14) is an inhibitor of transient receptor potential melastatin-8 (TRPM8) channels, IC₅₀<5 μM^[1].

IC₅₀ & Target^[1]

TRPM8

<5 μM (IC₅₀)

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	53 nM Compound: 68	Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin induction by flash luminometry Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin induction by flash luminometry	[PMID: 22329507]

Chemical Information

CAS. Nr. 1159996-20-9
Appearance Solid
Molecular Weight 414.40
Formel C₂₃H₁₈F₄N₂O
Color White to off-white
SMILES

O=C(N1C(C2=CC=C(C(F)(F)F)C=C2)C3=C(C=CC=C3)CC1)NC4=CC=C(F)C=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (241.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4131 mL

12.0656 mL

24.1313 mL

5 mM

0.4826 mL

2.4131 mL

4.8263 mL

10 mM

0.2413 mL

1.2066 mL

2.4131 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Norman, et al. Preparation of substituted dihydroisoquinoline derivatives for use as TRP-M8 receptor ligands. World Intellectual Property Organization, WO2009073203 A1. 2009-06-11.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4131 mL	12.0656 mL	24.1313 mL	60.3282 mL
	5 mM	0.4826 mL	2.4131 mL	4.8263 mL	12.0656 mL
	10 mM	0.2413 mL	1.2066 mL	2.4131 mL	6.0328 mL
	15 mM	0.1609 mL	0.8044 mL	1.6088 mL	4.0219 mL
	20 mM	0.1207 mL	0.6033 mL	1.2066 mL	3.0164 mL
	25 mM	0.0965 mL	0.4826 mL	0.9653 mL	2.4131 mL
	30 mM	0.0804 mL	0.4022 mL	0.8044 mL	2.0109 mL
	40 mM	0.0603 mL	0.3016 mL	0.6033 mL	1.5082 mL
	50 mM	0.0483 mL	0.2413 mL	0.4826 mL	1.2066 mL
	60 mM	0.0402 mL	0.2011 mL	0.4022 mL	1.0055 mL
	80 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7541 mL
	100 mM	0.0241 mL	0.1207 mL	0.2413 mL	0.6033 mL

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TRPM8-IN-1

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TRPM8-IN-1

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TRPM8-IN-1 Related Classifications

HY-108461 Related Classifications