[CAS NO. 1187990-87-9]  MK-8617

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PRODUCTS SPECIFICATIONS [1187990-87-9]

Catalog
SLK-S8443
Brand
Selleck
CAS
1187990-87-9

DESCRIPTION [1187990-87-9]

Overview

MDLMFCD22572348
Molecular Weight443.45
Molecular FormulaC24H21N5O4
SMILESO=C(C1=CN=C(C2=NN=CC=C2)NC1=O)NC(C3=CC=C(OC)C=C3)C4=CC=C(OC)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting , , with of 1.0, 1.0 and 14 nM, respectively.

Targets

PHD1 [1]
(Cell-free assay)
PHD2 [1]
(Cell-free assay)
PHD3 [1]
(Cell-free assay)
1 nM1 nM14 nM

In vitro

MK-8617 is not a significant inhibitor of the cytochrome p450 enzymes in vitro (IC50), CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6, >60 μM, and is a moderate reversible inhibitor of CYP2C8 at 1.6 μM in vitro. MK-8617 is inactive when screened at 10 μM against a general panel of 171 radioligand binding and enzymatic assays.