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.
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- CAS No.: 2768219-28-7
- 화학식: C21H23ClN4O5
- 분자량:446.88
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보관:
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Biological Activity
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Chemical Information
- 순도&문서
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Help & FAQs
Biological Activity
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.
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Cell Line:Hep3B cells
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Concentration:0,5,20,50 μM
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Incubation Time:12 hours
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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.
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]
| 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 | / |
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