MDR-652
Based on 1 Customer Validation
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.08%
- No. CAS: 1933528-96-1
- Fòrmula: C22H23ClFN3O2S
- Peso molecular:447.95
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Mechanoreceptors Compound Library
HY-L095
-
Targeted Diversity Library
HY-L099
-
Heterocyclic Compound Library
HY-L138
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Activators Library
HY-L159
-
Ion Channel Compound Library
HY-L166
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
|
hTRPV1 11.4 nM (Ki) |
rTRPV1 23.8 nM (Ki) |
hTRPV1 5.05 nM (EC50) |
rTRPV1 93 nM (EC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
5.05 nM
Compound: 4; MDR-652
|
Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
|
[PMID: 31702924] |
| CHO | EC50 |
93 nM
Compound: 4; MDR-652
|
Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
|
[PMID: 31702924] |
MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) [1].
MDR-652 has a promising topical pharmacokinetic profile[1].
MDR-652 has no significant toxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:ICR mouse[1]
-
Dosage:0.5 and 5 mg/kg
-
Administration:Administered intraperitoneally; 7 hours
-
Result:Decreased body temperature in a dose-dependent manner.
-
Animal Model:Rats with spinal nerve ligation (SNL) model[1]
-
Dosage:1, 2, 5, and 10 mg/kg
-
Administration:Administered intraperitoneally and subcutaneously; 24 hours
-
Result:The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED50 of 0.5-2 mg/kg.
The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.
Chemical Information
-
No. CAS 1933528-96-1
-
Appearance Solid
-
Peso molecular 447.95
-
Fòrmula C22H23ClFN3O2S
-
Color Off-white to light yellow
-
SMILES
O=C(NC1=CC=C(CO)C(F)=C1)NCC2=C(C3=CC=CC(Cl)=C3)N=C(C(C)(C)C)S2
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 250 mg/mL (558.10 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (13.95 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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:
-
-
-
-
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
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.
Pureza y Documentación
-
Ficha de datos (274 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2324 mL | 11.1620 mL | 22.3239 mL | 55.8098 mL |
| 5 mM | 0.4465 mL | 2.2324 mL | 4.4648 mL | 11.1620 mL | |
| 10 mM | 0.2232 mL | 1.1162 mL | 2.2324 mL | 5.5810 mL | |
| 15 mM | 0.1488 mL | 0.7441 mL | 1.4883 mL | 3.7207 mL | |
| 20 mM | 0.1116 mL | 0.5581 mL | 1.1162 mL | 2.7905 mL | |
| 25 mM | 0.0893 mL | 0.4465 mL | 0.8930 mL | 2.2324 mL | |
| 30 mM | 0.0744 mL | 0.3721 mL | 0.7441 mL | 1.8603 mL | |
| 40 mM | 0.0558 mL | 0.2790 mL | 0.5581 mL | 1.3952 mL | |
| 50 mM | 0.0446 mL | 0.2232 mL | 0.4465 mL | 1.1162 mL | |
| 60 mM | 0.0372 mL | 0.1860 mL | 0.3721 mL | 0.9302 mL | |
| 80 mM | 0.0279 mL | 0.1395 mL | 0.2790 mL | 0.6976 mL | |
| 100 mM | 0.0223 mL | 0.1116 mL | 0.2232 mL | 0.5581 mL |
MDR-652 Related Classifications
HY-136363 Related Classifications
Powered by Bioz