2. Metabolic Enzyme/Protease
  3. 15-PGDH
  4. HW201877

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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HW201877

HW201877 Chemical Structure

CAS No. : 2927452-83-1

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Based on 1 publication(s) in Google Scholar

HW201877 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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)[1].

In Vitro

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.

HW201877 Related Antibodies
Parmacokinetics
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 / /
In Vivo

HW201877 (0.5-2 mg/kg, p.o., twice a day for 21 days) effectively reduces the progression of pulmonary fibrosis in rats model[1].
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.

Animal Model: Bleomycin (HY-108345)-induced pulmonary fibrosis model established in male rats[1]
Dosage: 0.5, 1 and 2 mg/kg
Administration: Oral administration (p.o.), twice a day for 21 days
Result: Demonstrated marked reductions in pulmonary fibrosis scores.
Observed no significant differences in body weight changes.
Animal Model: DSS-induced ulcerative colitis model established in female mice[1]
Dosage: 2.5 and 5 mg/kg
Administration: Oral administration (p.o.), twice a day for 10 days
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).
Animal Model: Trinitro-benzene sulfonic acid (TNBS)-induced CD model established in male rats[1]
Dosage: 0.6, 1.2 and 2.4 mg/kg
Administration: Oral administration (p.o.), twice a day for 10 days
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.
Clinical Trial
Molecular Weight

440.45

Formula

C22H22F2N6O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N2C=CC(N3C[C@H]4C[C@H]4C5=CC(C(N6CCC(F)(CC6)F)=O)=CN=C35)=CC2=NN1C
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 : 50 mg/mL (113.52 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 2.2704 mL 11.3520 mL 22.7041 mL
5 mM 0.4541 mL 2.2704 mL 4.5408 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
=
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    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.
  • Protocol 2

    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.
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 2.2704 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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HW201877 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:

HW2018772927452-83-1HW 201877HW-20187715-PGDH15-Hydroxyprostaglandin dehydrogenaseProstaglandin E2Inflammatory bowel diseaseIdiopathic pulmonary fibrosisA549 cellsInhibitorinhibitorinhibit

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