2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. PHD2-IN-1

PHD2-IN-1 是一种强效的、具有口服活性的 HIF-脯氨酰羟化酶2 (PHD2) 抑制剂，IC50 为 22.53 nM，可用于贫血病研究。

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PHD2-IN-1 Chemical Structure

PHD2-IN-1 Chemical Structure

CAS No. : 2768219-28-7

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PHD2-IN-1 相关抗体

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查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research[1].

体外研究
(In Vitro)

PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 小时) 稳定 HIF-α 并增加促红细胞生成素 (EPO) 基因的表达。

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

PHD2-IN-1 相关抗体:

RT-PCR[1]

Cell Line: Hep3B cells
Concentration: 0,5,20,50 μM
Incubation Time: 12 hours
Result: Significantly stabilized HIF-1α and HIF-2α.
Upregulated the EPO mRNA level in a dose-dependently manner.
Showed no significant effects on the expression of the VEGFA gene.
体内研究
(In Vivo)

PHD2-IN-1 (Compound 22) (10,20,50 mg/kg 口服，每日一次持续三天) 在 C57BL/6 小鼠中刺激红细胞生成并以剂量依赖性方式增加网织红细胞[1]。
PHD2-IN-1 (50,100,200 mg/kg，腹腔注射, 每日一次持续三天) 对 ICR 小鼠无明显毒性反应[1]。
PHD2-IN-1 (静脉注射1 mg/kg，口服10 mg/kg) 显示在大鼠中 T1/2 为 2.29 小时 (口服) 或 3.72 小时 (静脉注射)，在小鼠中 T1/2 为 1.17 小时 (口服) 或 0.33 小时 (静脉注射)。在大鼠和小鼠中的口服生物利用度 (F%) 分别为 33.9% 和 35.3%[1]。
Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice [1]

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

Species Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) T1/2 (h) CL (mL•min-1/kg-1) VZ (mL/kg) MRT0-Ꝏ (h) F (%)
rat p.o. 10 0.08 26140 7118 7135 2.29 1417 4629 0.56 33.9
rat i.v. 1 / / 2069 2106 3.72 483 2644 1.54 /
mice p.o. 10 0.5 3036 4475 4489 1.17 2246 4532 1.67 35.3
mice i.v. 1 / / 1384 1387 0.33 721 345 0.53 /
Animal Model: C57BL/6 mice[1]
Dosage: 10,20, and 50 mg/kg
Administration: Oral gavage (p.o.), once daily for three days
Result: Increased reticulocytes in a dose-dependent manner.
The reticulocyte count/red blood cell count (RBC%) increased significantly in a dose-dependent manner.
Animal Model: SD rats and C57BL/6 mice (Pharmacokinetic assay)[1]
Dosage: 1, 10 mg/kg
Administration: Intravenous injection (i.v.)，Oral gavage (p.o.)
Result: Showed T1/2s of 2.29 h (p.o.) or 3.72 h (i.v.) in rats and 1.17 h (p.o.) or 0.33 h (i.v.) in mice. And oral bioavailability (F%) of 33.9% in rats and 35.3% in mice.
Animal Model: Subacute toxicity assessment in ICR mice[1]
Dosage: 50,100,200 mg/kg
Administration: Intraperitoneal injection (i.p.) once daily for 14 days
Result: Had no significant hepatotoxicity or nephrotoxicity reactions after administration of a high dose of 200 mg/kg, at 10 imes the efficacious dose (20mg/kg).
Observed no death or behavioral abnormalities when the mice were treated in the dose of 800 mg/kg by p.o. administration.
分子量

446.88

Formula

C21H23ClN4O5
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

PHD2-IN-1 相关分类

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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:

PHD2-IN-12768219-28-7HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHAnemiaEPOHIF-ΑProlyl Hydroxylase 2Hep3B CellsPlasma ReticulocytesInhibitorinhibitorinhibit

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目录号：
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