HW201877
Based on 1 Customer Validation
HW201877 is a potent and orally active 15-prostaglandin dehydrogenase (15-PGDH) inhibitor with an IC50 of 3.6 nM. HW201877 demonstrates robust cellular efficacy in elevating PGE2 levels in A549 cells and exhibits remarkable efficacy in animal models of tissue injury and fibrosis. HW201877 can be used for the study of inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF) and Crohn’s disease (CD).
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- Pureté: 99.00%
- CAS No.: 2927452-83-1
- Formule: C22H22F2N6O2
- Masse moléculaire:440.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
HW201877 exhibits exceptional liver microsomal stability in various species (human, rat, dog, mouse) and inhibitory effects on seven major cytochrome P450 isoforms (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4), with all IC50 values exceeding 150 μM[1].
HW201877 demonstrates superior pharmacological efficacy by inducing a 4.8-fold elevation of PEG2 levels relative to that of its counterpart[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | CL | Vz | AUC0-t | F | Cmax |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 0.5 mg/kg | i.v. | 11.1 h | 0.14 L/h/kg | 1.1 L/kg | 6831 ng·h/mL | / | / |
| Dog[1] | 1 mg/kg | p.o. | 11.1 h | / | / | 12665 ng·h/mL | 97 % | 913 ng/mL |
| Mice[1] | 10 mg/kg | p.o. | 2.1 h | / | / | 33173 ng·h/mL | 97 % | 4480 ng/mL |
| Mice[1] | 3 mg/kg | i.v. | 1.9 h | 0.42 L/h/kg | 1.1 L/kg | 8544 ng·h/mL | / | / |
| Rat[1] | 10 mg/kg | p.o. | 3.1 h | / | / | 17999 ng·h/mL | 82 % | 1637 ng/mL |
| Rat[1] | 3 mg/kg | i.v. | 2.9 h | 0.46 L/h/kg | 1.9 L/kg | 6619 ng·h/mL | / | / |
HW201877 (2.5-5 mg/kg, p.o., twice a day for 10 days) significantly mitigates DSS (HY-116282C)-induced pathological manifestations in mice ulcerative colitis model[1].
HW201877 (0.6-2.4 mg/kg, p.o., twice a day for 10 days) exhibits good therapeutic efficacy against CD-like pathology in rat Crohn’s disease model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin (HY-108345)-induced pulmonary fibrosis model established in male rats[1]
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Dosage:0.5, 1 and 2 mg/kg
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Administration:Oral administration (p.o.), twice a day for 21 days
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Result:Demonstrated marked reductions in pulmonary fibrosis scores.
Observed no significant differences in body weight changes.
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Animal Model:DSS-induced ulcerative colitis model established in female mice[1]
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Dosage:2.5 and 5 mg/kg
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Administration:Oral administration (p.o.), twice a day for 10 days
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Result:Reduced disease activity index (DAI) scores encompassing diarrhea, rectal bleeding, and weight loss and amelioration of colon shortening.
Significantly decreased the colon weight-to-length ratio.
Reduced tissue damage scores by 69.2% (both doses) and inflammatory cell infiltration by 54.2% (2.5 mg/kg) and 58.3% (5.0 mg/kg).
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Animal Model:Trinitro-benzene sulfonic acid (TNBS)-induced CD model established in male rats[1]
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Dosage:0.6, 1.2 and 2.4 mg/kg
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Administration:Oral administration (p.o.), twice a day for 10 days
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Result:Dose-dependently alleviated TNBS-induced weight loss.
Reduced DAI scores and attenuated colon shortening with a 55.7% decrease in the colon weight-to-length ratio at 2.4 mg/kg.
Included significant reductions in colon ulceration, crypt abscesses, and enhanced mucosal regeneration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2927452-83-1
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Appearance Solid
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Masse moléculaire 440.45
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Formule C22H22F2N6O2
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Color Off-white to light yellow
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SMILES
O=C1N2C=CC(N3C[C@H]4C[C@H]4C5=CC(C(N6CCC(F)(CC6)F)=O)=CN=C35)=CC2=NN1C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (113.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (5.68 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 (5.68 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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.2704 mL | 11.3520 mL | 22.7041 mL | 56.7601 mL |
| 5 mM | 0.4541 mL | 2.2704 mL | 4.5408 mL | 11.3520 mL | |
| 10 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL | 5.6760 mL | |
| 15 mM | 0.1514 mL | 0.7568 mL | 1.5136 mL | 3.7840 mL | |
| 20 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8380 mL | |
| 25 mM | 0.0908 mL | 0.4541 mL | 0.9082 mL | 2.2704 mL | |
| 30 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8920 mL | |
| 40 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
| 50 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1352 mL | |
| 60 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL | |
| 80 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL |
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