| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
MDR-652 is a novel and 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. agonist discovered to be a strong topical analgesic.
| ln Vivo |
MDR-652 (0.5 and 5 mg/kg) demonstrated a drop in body temperature that was dose-dependent, corroborating the idea that in intact animals, MDR-652 exhibits TRPV1 agonism [1]. MDR-652 (5–10 mg/kg; intraperitoneal and subcutaneous injection) exhibits 100% maximum potential effect (MPE) in blocking neuropathic pain [1]. Good local pharmacokinetic properties are possessed by MDR-652 [1]. It doesn't seem that MDR-652 is harmful. The LD50 of MDR-652 given intraperitoneally (i.p.) and topically (po) exceeded 200 and 2000 mg/kg, respectively, in single-dose toxicity investigations [1].
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| Animal Protocol |
Animal/Disease Models: ICR mice [1]
Doses: 0.5 and 5 mg/kg Route of Administration: intraperitonealadministration; 7 hrs (hrs (hours)) Experimental Results: Body temperature diminished in a dose-dependent manner. Animal/Disease Models: Rat spinal nerve ligation (SNL) model [1] Doses: 1, 2, 5, 10 mg/kg Route of Administration: intraperitonealand subcutaneous injection; 24-hour Experimental Results: intraperitonealadministration demonstrated excellent dosage Dependent analgesic properties, ED50 is 0.5-2 mg/kg. subcutaneous injection also demonstrated excellent analgesic effects, with maximal effects occurring 30 minutes after administration. |
| References |
| Molecular Formula |
C22H23CLFN3O2S
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|---|---|
| Molecular Weight |
447.9533
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| Exact Mass |
447.118
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| Elemental Analysis |
C, 58.99; H, 5.18; Cl, 7.91; F, 4.24; N, 9.38; O, 7.14; S, 7.16
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| CAS # |
1933528-96-1
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| Related CAS # |
1933528-96-1;
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| PubChem CID |
121364823
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
579
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HKMPJRGWSUCANB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23ClFN3O2S/c1-22(2,3)20-27-19(13-5-4-6-15(23)9-13)18(30-20)11-25-21(29)26-16-8-7-14(12-28)17(24)10-16/h4-10,28H,11-12H2,1-3H3,(H2,25,26,29)
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| Chemical Name |
1-((2-(tert-butyl)-4-(3-chlorophenyl)thiazol-5-yl)methyl)-3-(3-fluoro-4-(hydroxymethyl)phenyl)urea
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| Synonyms |
MDR-652 MDR652 MDR 652
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~558.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (13.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (13.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2324 mL | 11.1620 mL | 22.3239 mL | |
| 5 mM | 0.4465 mL | 2.2324 mL | 4.4648 mL | |
| 10 mM | 0.2232 mL | 1.1162 mL | 2.2324 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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