1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PDE12-IN-1

PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity.

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

PDE12-IN-1 Chemical Structure

PDE12-IN-1 Chemical Structure

CAS No. : 2259620-80-7

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1 mg USD 582 In-stock
5 mg USD 1280 In-stock
10 mg USD 2050 In-stock
25 mg USD 4050 In-stock
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Description

PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity[1].

IC50 & Target[1]

PDE12

9.1 (pIC50)

In Vitro

PDE12-IN-1 inhibits the EMCV-induced cytopathic effect in HeLa Ohio cells with a pIC50 of 6.7. PDE12-IN-1 inhibits HeLa Ohio cell proliferation in the absence of EMCV infection with a pIC50 of 5.7. PDE12-IN-1 inhibits the proliferation of both HeLa and HeLaΔPDE12 cells with a pIC50 of 5.7. PDE12-IN-1 inhibits HRV infection with a pIC50 of 6.9[1].

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

Molecular Weight

616.48

Formula

C31H27BrFN5O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

N#CC1=CC2=C(C=C1)C(C3=NC4=CC(Br)=C(C(N5[C@H](CO)[C@@H](C6=CC=C(F)C=C6)OCC5)=O)C=C4N3C)=CN2CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 90 mg/mL (145.99 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 1.6221 mL 8.1106 mL 16.2211 mL
5 mM 0.3244 mL 1.6221 mL 3.2442 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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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: ≥ 4.75 mg/mL (7.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.75 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 (47.5 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.5 mg/mL (7.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6221 mL 8.1106 mL 16.2211 mL 40.5528 mL
5 mM 0.3244 mL 1.6221 mL 3.2442 mL 8.1106 mL
10 mM 0.1622 mL 0.8111 mL 1.6221 mL 4.0553 mL
15 mM 0.1081 mL 0.5407 mL 1.0814 mL 2.7035 mL
20 mM 0.0811 mL 0.4055 mL 0.8111 mL 2.0276 mL
25 mM 0.0649 mL 0.3244 mL 0.6488 mL 1.6221 mL
30 mM 0.0541 mL 0.2704 mL 0.5407 mL 1.3518 mL
40 mM 0.0406 mL 0.2028 mL 0.4055 mL 1.0138 mL
50 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8111 mL
60 mM 0.0270 mL 0.1352 mL 0.2704 mL 0.6759 mL
80 mM 0.0203 mL 0.1014 mL 0.2028 mL 0.5069 mL
100 mM 0.0162 mL 0.0811 mL 0.1622 mL 0.4055 mL
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PDE12-IN-1 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.

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PDE12-IN-1
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