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

HW201877 是一种强效且口服有效的 15-前列腺素脱氢酶 (15-PGDH) 抑制剂，其 IC50 值为 3.6 nM。HW201877 能在 A549 细胞中极大程度上提升 PEG2 水平，并在组织损伤和纤维化的动物模型中显示出显著的疗效。HW201877 可用于炎症性肠病 (IBD)、特发性肺纤维化 (IPF) 和克罗恩病 (CD) 的研究。

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HW201877

HW201877 Chemical Structure

CAS No. : 2927452-83-1

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HW201877 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

HW 201877 在不同种属 (人、大鼠、犬、小鼠) 中表现出较好的肝微粒体稳定性，和 7 种主要细胞色素 P450 亚型 (CYP 1A2、2B6、2C8、2C9、2C19、2D6 和 3A) 的抑制作用，其 IC50 值均超过 150 μM[1]。
HW 201877 诱导 PEG2 水平相对于其对应物升高 4.8 倍，证明了其较好的药理学疗效[1]。

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

HW201877 相关抗体:
体内研究
(In Vivo)

HW201877 (0.5-2 mg/kg, p.o., 1 天 2 次, 持续 21 天) 能有效减缓大鼠肺纤维化模型的病情进展[1]。
HW201877 (2.5-5 mg/kg, p.o., 1 天 2 次, 持续 10 天) 能显著减轻 DSS (HY-116282C) 引发的小鼠溃疡性结肠炎模型的病理表现[1]。
HW201877 (2.5-5 mg/kg, p.o., 1 天 2 次, 持续 10 天) 对大鼠克罗恩病模型中的病理表现具有良好的治疗效果[1]。

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.
分子量

440.45

Formula

C22H22F2N6O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HW201877 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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