2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. Acoltremon

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

Cat. No.: HY-108449 Purity: 99.90%
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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.

For research use only. We do not sell to patients.

Acoltremon Chemical Structure

Acoltremon Chemical Structure

CAS No. : 68489-09-8

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Based on 1 publication(s) in Google Scholar

Acoltremon Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Acoltremon

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TRPC TRPM TRPV TRPA TRPML

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Description

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[1][2].

IC50 & Target[1]

TRPM8

 

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.

Acoltremon Related Antibodies

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
Molecular Weight

289.41

Formula

C18H27NO2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4553 mL 17.2765 mL 34.5531 mL
5 mM 0.6911 mL 3.4553 mL 6.9106 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Acoltremon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Acoltremon68489-09-8WS-12 AR-15512 AVX-012WS12WS 12AR15512AR 15512AR-15512AVX012AVX 012AVX-012TRP ChannelTransient receptor potential channelsanalgesic effectchronic neuropathic painHEK293Tcultured mouse DRG neuronsInhibitorinhibitorinhibit

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