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

MDR-652 

Cat. No.: HY-136363 Purity: 98.17%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 220 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
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100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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[1]

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].

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.

1933528-96-1

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (558.10 mM; Need ultrasonic)

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
10 mM 0.2232 mL 1.1162 mL 2.2324 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

MDR-652MDR652MDR 652TRP ChannelTransient receptor potential channelsTRPV1ligandhTRPV1analgesicactivityneuropathicpainInhibitorinhibitorinhibit

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MDR-652
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