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

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.

For research use only. We do not sell to patients.

PHD2-IN-1 Chemical Structure

PHD2-IN-1 Chemical Structure

CAS No. : 2768219-28-7

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PHD2-IN-1 Related Antibodies

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Description

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].

In Vitro

PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 hours) stabilizes HIF-α and increases the expression of the erythropoietin (EPO) gene[1].

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

PHD2-IN-1 Related Antibodies

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.
In Vivo

PHD2-IN-1 (Compound 22) (10,20,50 mg/kg, p.o., once daily for three days) stimulates erythropoiesis and increase reticulocytes in a dose-dependent manner in C57BL/6 mice[1].
PHD2-IN-1 (50,100,200 mg/kg for i.p., once daily for 14 days) has no significant toxic reactions in ICR mice[1].
PHD2-IN-1 (1 mg/kg for i.p., 10 mg/kg for p.o.) shows 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[1].
Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice [1]

MedChemExpress (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.
Molecular Weight

446.88

Formula

C21H23ClN4O5
CAS No.
SMILES

ClC1=CC=C(NCC(N2CCC(C3=CN=C(C(NCC(O)=O)=O)C(O)=C3)CC2)=O)C=C1
Shipping

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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PHD2-IN-1 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:

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

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