15-PGDH-IN-1
Based on 1 Customer Validation
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.
- Purity: 98.35%
- CAS No.: 2241676-74-2
- Formula: C24H22N4O2
- Molecular Weight:398.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 3 nM (15-PGDH)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 Mice (female)[1]
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Dosage:5, 10 mg/kg
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Administration:IV, IP, PO
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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%).
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Animal Model:C57Bl/6 mice[1]
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Dosage:5, 20, 40 mg/kg
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Administration:IP, Oral
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Result:Showed elevation of PGE2 levels in colon and lung inhibited 15-PGDH enzymatic activity in the colon.
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Animal Model:DSS model[1]
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Dosage:10, 40 mg/kg
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Administration:IP (10 mg/kg BID) or PO (40 mg/kg BID)
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Result:Showed protection in the mouse DSS model of ulcerative colitis.
Chemical Information
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CAS No. 2241676-74-2
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Appearance Solid
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Molecular Weight 398.46
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Formula C24H22N4O2
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Color Light yellow to yellow
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SMILES
CN1C=CC2=CC(C3=CN=C4C=CC(C(N5CCCCC5)=O)=CC4=N3)=CC=C2C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (250.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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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, 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 |