Art. -Nr.: HY-136363

MDR-652

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MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The K_is 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.

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Reinheit: 98.08%
CAS. Nr.: 1933528-96-1
Formel: C₂₂H₂₃ClFN₃O₂S
Molecular Weight:447.95

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MDR-652 Chemical Structure

CAS. Nr.: 1933528-96-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

hTRPV1

11.4 nM (Ki)

rTRPV1

23.8 nM (Ki)

hTRPV1

5.05 nM (EC₅₀)

rTRPV1

93 nM (EC₅₀)

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

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.

Chemical Information

CAS. Nr. 1933528-96-1
Appearance Solid
Molecular Weight 447.95
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jihyae Ann, et al. Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic. J Med Chem. 2020 Jan 9;63(1):418-424. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MDR-652

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MDR-652 Related Classifications

HY-136363 Related Classifications