2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. MDR-652

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.

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

MDR-652 Chemical Structure

MDR-652 Chemical Structure

CAS No. : 1933528-96-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

MDR-652 Related Antibodies

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Description

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[1].

IC50 & Target

hTRPV1

11.4 nM (Ki)

rTRPV1

23.8 nM (Ki)

hTRPV1

5.05 nM (EC50)

rTRPV1

93 nM (EC50)

In Vivo

MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal[1].
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.
Molecular Weight

447.95

Formula

C22H23ClFN3O2S
CAS No.
Appearance

Solid

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
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 : 250 mg/mL (558.10 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 2.2324 mL 11.1620 mL 22.3239 mL
5 mM 0.4465 mL 2.2324 mL 4.4648 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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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    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 6.25 mg/mL (13.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 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 (62.5 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 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
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MDR-652 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:

MDR-6521933528-96-1MDR652MDR 652TRP ChannelTransient receptor potential channelsTRPV1ligandhTRPV1analgesicactivityneuropathicpainInhibitorinhibitorinhibit

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