Elismetrep
Based on 1 Customer Validation
Elismetrep (MT-8554) is a TRPM8 channel antagonist and neuroprotective agent. Elismetrep is used for research on pain, menopause-related vasomotor symptoms, and diabetic peripheral neuropathy.
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- Purity: 99.59%
- CAS No.: 1400699-64-0
- 화학식: C27H21F3N2O5S
- 분자량:542.53
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Help & FAQs
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Biological Activity
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TRPM8 |
Elismetrep exerts neuroprotective effects and is used in studies of menopausal-related vasomotor symptoms and diabetic peripheral neuropathy[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1400699-64-0
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Appearance Solid
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분자량 542.53
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화학식 C27H21F3N2O5S
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Color Off-white to light yellow
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SMILES
O=C(C1=CC=C(S(=O)(N(CC2=CC=C(C=C2)OC(F)(F)F)C3=C(C4CC4)C5=CC=CC=C5C=N3)=O)C=C1)O
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Synonyms
MT-8554
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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 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (184.32 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, 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.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.61 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Conklin M, et al. Neurokinin receptor antagonists as potential non-hormonal treatments for vasomotor symptoms of menopause. Therapeutic advances in reproductive health. 2023;17:26334941231177611. [Content Brief]
[2]. Weyer AD, et al. Development of TRPM8 Antagonists to Treat Chronic Pain and Migraine. Pharmaceuticals (Basel, Switzerland). 2017 Mar 30;10(2):37. [Content Brief]
[3]. Genazzani AR, et al. Oral investigational drugs currently in phase I or phase II for the amelioration of menopausal symptoms. Expert opinion on investigational drugs. 2019 Mar;28(3):235-247. [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, 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 |
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| DMSO | 1 mM | 1.8432 mL | 9.2161 mL | 18.4322 mL | 46.0804 mL |
| 5 mM | 0.3686 mL | 1.8432 mL | 3.6864 mL | 9.2161 mL | |
| 10 mM | 0.1843 mL | 0.9216 mL | 1.8432 mL | 4.6080 mL | |
| 15 mM | 0.1229 mL | 0.6144 mL | 1.2288 mL | 3.0720 mL | |
| 20 mM | 0.0922 mL | 0.4608 mL | 0.9216 mL | 2.3040 mL | |
| 25 mM | 0.0737 mL | 0.3686 mL | 0.7373 mL | 1.8432 mL | |
| 30 mM | 0.0614 mL | 0.3072 mL | 0.6144 mL | 1.5360 mL | |
| 40 mM | 0.0461 mL | 0.2304 mL | 0.4608 mL | 1.1520 mL | |
| 50 mM | 0.0369 mL | 0.1843 mL | 0.3686 mL | 0.9216 mL | |
| 60 mM | 0.0307 mL | 0.1536 mL | 0.3072 mL | 0.7680 mL | |
| 80 mM | 0.0230 mL | 0.1152 mL | 0.2304 mL | 0.5760 mL | |
| 100 mM | 0.0184 mL | 0.0922 mL | 0.1843 mL | 0.4608 mL |
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