Name | MK-8617 |
Description | MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM). |
In vitro | In vitro, MK-8617 hasn't markedly inhibitory for CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6 (IC50>60 μM), and is a moderate reversible inhibitor of CYP2C8 (IC50: 1.6 μM). MK-8617 (10 μM) is inactive against a general panel of 171 radioligand binding and enzymatic assays. |
In vivo | In liver microsomes (+NADPH) from rat, dog, and monkey, tritiated MK-8617 exhibits minimal metabolic turnover (<10%), but the significant turnover (34%) in HLMs after 60 min (10 μM compound, 1 mg/mL microsomal protein). MK-8617 has good oral bioavailability across species (36?71%), with low clearance and volume of distribution. Increases in circulating reticulocytes are observed at 5 and 15 mg/kg 3 days after challenge and at the 15 mg/kg 4 days after challenge. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 1 mg/ml, Sonication is recommended.
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Keywords | MK 8617 | HIF-PH | inhibit | Hypoxia-inducible factors | MK-8617 | HIFs | Inhibitor | HIF/HIF Prolyl-Hydroxylase |
Inhibitors Related | Deferoxamine Mesylate | Hydralazine hydrochloride | 1,4-DPCA | DMOG | Chlorogenic Acid | Roxadustat | Glucosamine | Hydroxycitric acid tripotassium hydrate | Glucosamine hydrochloride | Minocycline hydrochloride | Oltipraz | Glucosamine sulfate |
Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |