Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
説明 | MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM). |
ターゲット&IC50 | PHD3:14 nM, PHD1:1 nM, PHD2:1 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. |
別名 | MK8617 |
分子量 | 443.45 |
分子式 | C24H21N5O4 |
CAS No. | 1187990-87-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16 mg/mL (36.1 mM)
You can also refer to dose conversion for different animals. 詳細
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MK-8617 1187990-87-9 Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase MK 8617 HIF-PH inhibit Hypoxia-inducible factors MK8617 HIFs Inhibitor inhibitor