Acoltremon
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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- Purity: 99.13%
- CAS No.: 68489-09-8
- 화학식: C18H27NO2
- 분자량:289.41
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Acoltremon
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Biological Activity
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TRPM8 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
40 nM
Compound: WS-12
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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
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[PMID: 24080460] |
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.
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Cell Line:HEK293T cells
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Concentration:10 μM
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Incubation Time:
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Result:Activated mouse TRPM8 (mTRPM8), but neither activated nor inhibited mTRPA1.
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Cell Line:Cultured mouse DRG neurons
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Concentration:1 or 10 μM
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Incubation Time:0-250 s
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Result:Showed approximately 10% to 14% of cultured wild-type neurons responsive to WS-12.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Trpm8–/– mice and mice injected with Capsaicin[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; 10 mg/kg; once
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 68489-09-8
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Appearance Solid
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분자량 289.41
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화학식 C18H27NO2
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Color White to off-white
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SMILES
O=C([C@H]1[C@H](C(C)C)CC[C@@H](C)C1)NC2=CC=C(OC)C=C2
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Synonyms
WS-12; AR-15512; AVX-012
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
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Most Recent
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Cell Calcium
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
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
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 |
Acoltremon Related Classifications
HY-108449 Related Classifications
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