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MK-8617

Catalog No. T4106Cas No. 1187990-87-9
Alias MK8617

MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).

MK-8617

MK-8617

Purity: 100%
Catalog No. T4106Alias MK8617Cas No. 1187990-87-9
MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
2 mg$40In Stock
5 mg$64In Stock
10 mg$89In Stock
25 mg$172In Stock
50 mg$327In Stock
100 mg$486In Stock
200 mg$693In Stock
500 mg$1,090In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
Targets&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.
AliasMK8617
Chemical Properties
Molecular Weight443.45
FormulaC24H21N5O4
Cas No.1187990-87-9
Storage & Solubility Information
StoragePowder: -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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