Art. -Nr.: HY-108449

Acoltremon

(Synonyms: WS-12; AR-15512; AVX-012)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research.

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Reinheit: 99.13%
CAS. Nr.: 68489-09-8
Formel: C₁₈H₂₇NO₂
Molecular Weight:289.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Acoltremon Chemical Structure

CAS. Nr.: 68489-09-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

TRPM8

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	40 nM Compound: WS-12	Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay	[PMID: 24080460]

In Vitro

Acoltremon (10 μM) shows TRPM8 agonism in tests on heterologously expressed TRP ion channels^[1].
Acoltremon (1 or 10 μM; 0-250 s) shows highly potent and specific TRPM8 channel agonist in DRG neurons^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

HEK293T cells
Concentration:

10 μM
Incubation Time:
Result:

Activated mouse TRPM8 (mTRPM8), but neither activated nor inhibited mTRPA1.

Cell Viability Assay^[1]

Cell Line:

Cultured mouse DRG neurons
Concentration:

1 or 10 μM
Incubation Time:

0-250 s
Result:

Showed approximately 10% to 14% of cultured wild-type neurons responsive to WS-12.

In Vivo

Acoltremon (intraperitoneal injection; 10 mg/kg; once) shows analgesic effect by selective TRPM8 activation in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Trpm8^–/– mice and mice injected with Capsaicin^[1]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection; 10 mg/kg; once
Result:

Produced an obvious analgesic effect, and this effect abolished in Trpm8^–/– mice.
Showed no change falling latencies in mice in the rotarod test.
Reduced Capsaicin-induced nocifensive behavior.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 68489-09-8
Appearance Solid
Molecular Weight 289.41
Formel C₁₈H₂₇NO₂
Color White to off-white
SMILES

O=C([C@H]1[C@H](C(C)C)CC[C@@H](C)C1)NC2=CC=C(OC)C=C2
Synonyms

WS-12; AR-15512; AVX-012
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Cell Calcium

Activation of TRPM8 promotes K+ secretion in rat epididymal epithelium. [Abstract]

2026 Mar:134:103117. PMID: 41539212
J Cardiovasc Transl Res

TMAO Impairs Mouse Aortic Vasodilation by Inhibiting TRPV4 Channels in Endothelial Cells. [Abstract]

2024 Dec;17(6):1415-1426. PMID: 38980653

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (69.11 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

3.4553 mL

17.2765 mL

34.5531 mL

5 mM

0.6911 mL

3.4553 mL

6.9106 mL

10 mM

0.3455 mL

1.7277 mL

3.4553 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 90% Corn Oil

Solubility: ≥ 2 mg/mL (6.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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 (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 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]. Beck B, et al. Prospects for prostate cancer imaging and therapy using high-affinity TRPM8 activators. Cell Calcium. 2007 Mar;41(3):285-94. [Content Brief]

[2]. Ma S, et al. Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels. Pak J Pharm Sci. 2008 Oct;21(4):370-8. [Content Brief]

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4553 mL	17.2765 mL	34.5531 mL	86.3826 mL
	5 mM	0.6911 mL	3.4553 mL	6.9106 mL	17.2765 mL
	10 mM	0.3455 mL	1.7277 mL	3.4553 mL	8.6383 mL
	15 mM	0.2304 mL	1.1518 mL	2.3035 mL	5.7588 mL
	20 mM	0.1728 mL	0.8638 mL	1.7277 mL	4.3191 mL
	25 mM	0.1382 mL	0.6911 mL	1.3821 mL	3.4553 mL
	30 mM	0.1152 mL	0.5759 mL	1.1518 mL	2.8794 mL
	40 mM	0.0864 mL	0.4319 mL	0.8638 mL	2.1596 mL
	50 mM	0.0691 mL	0.3455 mL	0.6911 mL	1.7277 mL
	60 mM	0.0576 mL	0.2879 mL	0.5759 mL	1.4397 mL

Acoltremon

2 Cited Publications

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Acoltremon

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

FDA Approved & Pharmacopeial Drug Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Flavors and Fragrances Compound Library

Publications Citing Use of MedChemExpress (MCE) Acoltremon

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Acoltremon

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

FDA Approved & Pharmacopeial Drug Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Flavors and Fragrances Compound Library

Publications Citing Use of MedChemExpress (MCE) Acoltremon

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Acoltremon Related Classifications

HY-108449 Related Classifications