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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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
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.
Molecular Weight

440.45

Formula

C22H22F2N6O2
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HW201877 Related Classifications

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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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