1. Metabolic Enzyme/Protease
  2. 15-PGDH
  3. 15-PGDH-IN-1

15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration.

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

15-PGDH-IN-1 Chemical Structure

15-PGDH-IN-1 Chemical Structure

CAS No. : 2241676-74-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 254 In-stock
Solution
10 mM * 1 mL in DMSO USD 254 In-stock
Solid
1 mg USD 65 In-stock
5 mg USD 290 In-stock
10 mg USD 550 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration[1].

IC50 & Target

IC50: 3 nM (15-PGDH)[1]

In Vitro

15-PGDH-IN-1 (compound 49) has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM[1].
15-PGDH-IN-1 (4, 20, 100, 500, 2500 nM) induces PGE2 in A549 cells at 20 nM[1].

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

In Vivo

15-PGDH-IN-1 (compound 49) (5, 10, 20, 40 mg/kg; IV, IP, PO) shows potent inhibition of 15-PGDH, good oral bioavailability, and protective activity in mouse models of ulcerative colitis and recovery from bone marrow transplantation[1].

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

Animal Model: CD1 Mice (female)[1]
Dosage: 5, 10 mg/kg
Administration: IV, IP, PO
Result: Showed a low Cmax value when dosed orally versus IP, but the AUC was only reduced by half and had good oral bioavailability (63%).
Animal Model: C57Bl/6 mice[1]
Dosage: 5, 20, 40 mg/kg
Administration: IP, Oral
Result: Showed elevation of PGE2 levels in colon and lung inhibited 15-PGDH enzymatic activity in the colon.
Animal Model: DSS model[1]
Dosage: 10, 40 mg/kg
Administration: IP (10 mg/kg BID) or PO (40 mg/kg BID)
Result: Showed protection in the mouse DSS model of ulcerative colitis.
Molecular Weight

398.46

Formula

C24H22N4O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN1C=CC2=CC(C3=CN=C4C=CC(C(N5CCCCC5)=O)=CC4=N3)=CC=C2C1=O

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 : 100 mg/mL (250.97 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 2.5097 mL 12.5483 mL 25.0966 mL
5 mM 0.5019 mL 2.5097 mL 5.0193 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. 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
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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

×
Volume (start)

V1

=
Concentration (final)

C2

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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: 2.5 mg/mL (6.27 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.27 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, 6 months; -20°C, 1 month. 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 2.5097 mL 12.5483 mL 25.0966 mL 62.7416 mL
5 mM 0.5019 mL 2.5097 mL 5.0193 mL 12.5483 mL
10 mM 0.2510 mL 1.2548 mL 2.5097 mL 6.2742 mL
15 mM 0.1673 mL 0.8366 mL 1.6731 mL 4.1828 mL
20 mM 0.1255 mL 0.6274 mL 1.2548 mL 3.1371 mL
25 mM 0.1004 mL 0.5019 mL 1.0039 mL 2.5097 mL
30 mM 0.0837 mL 0.4183 mL 0.8366 mL 2.0914 mL
40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5685 mL
50 mM 0.0502 mL 0.2510 mL 0.5019 mL 1.2548 mL
60 mM 0.0418 mL 0.2091 mL 0.4183 mL 1.0457 mL
80 mM 0.0314 mL 0.1569 mL 0.3137 mL 0.7843 mL
100 mM 0.0251 mL 0.1255 mL 0.2510 mL 0.6274 mL
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15-PGDH-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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Product Name:
15-PGDH-IN-1
Cat. No.:
HY-151807
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