2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. MR-L2

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.

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

MR-L2 Chemical Structure

MR-L2 Chemical Structure

CAS No. : 2374703-19-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 750 In-stock
50 mg USD 2250 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

MR-L2 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM[1].

IC50 & Target

PDE4

 

In Vitro

MR-L2 (0.3-10 μM; 1 h) significantly suppresses cAMP elevation and cysts formation in MDCK cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MR-L2 Related Antibodies

Cell Viability Assay[1]

Cell Line: Madin-Darby Canine Kidney (MDCK) cell line
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 1 hour
Result: Suppressed cAMP elevation but not enhanced cAMP excretion in MDCK cells. Suppressed cysts formation in MDCK cells with an EC50 value of 1.2 µM. Suppressed the number of cysts formation in 3D culture for both unstimulated and vasopressin-treated culture condition while showed no effect on cell viability.
Molecular Weight

441.71

Formula

C19H16Cl3FN4O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

ClC1=C(F)C=C(C2=NN(CC(NCC3=CC(Cl)=CC(Cl)=C3)=O)C(CC)=N2)C=C1
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 : 83.33 mg/mL (188.65 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 2.2639 mL 11.3196 mL 22.6393 mL
5 mM 0.4528 mL 2.2639 mL 4.5279 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
=
Concentration
×
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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Purity: 99.23%

COA (248 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
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 2.2639 mL 11.3196 mL 22.6393 mL 56.5982 mL
5 mM 0.4528 mL 2.2639 mL 4.5279 mL 11.3196 mL
10 mM 0.2264 mL 1.1320 mL 2.2639 mL 5.6598 mL
15 mM 0.1509 mL 0.7546 mL 1.5093 mL 3.7732 mL
20 mM 0.1132 mL 0.5660 mL 1.1320 mL 2.8299 mL
25 mM 0.0906 mL 0.4528 mL 0.9056 mL 2.2639 mL
30 mM 0.0755 mL 0.3773 mL 0.7546 mL 1.8866 mL
40 mM 0.0566 mL 0.2830 mL 0.5660 mL 1.4150 mL
50 mM 0.0453 mL 0.2264 mL 0.4528 mL 1.1320 mL
60 mM 0.0377 mL 0.1887 mL 0.3773 mL 0.9433 mL
80 mM 0.0283 mL 0.1415 mL 0.2830 mL 0.7075 mL
100 mM 0.0226 mL 0.1132 mL 0.2264 mL 0.5660 mL
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MR-L2 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:

MR-L22374703-19-0Phosphodiesterase (PDE)reversiblenoncompetitiveallostericlong-isoformMDCKcAMPPKAcystADPKDtriazoleInhibitorinhibitorinhibit

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