MK-8617 - 98%, high purity , CAS No.1187990-87-9

  • ≥98%
Item Number
M414011
Grouped product items
SKUSizeAvailabilityPrice Qty
M414011-5mg
5mg
In stock
$78.90
M414011-10mg
10mg
In stock
$107.90
M414011-25mg
25mg
In stock
$206.90
M414011-50mg
50mg
In stock
$404.90
M414011-100mg
100mg
In stock
$741.90

HIF Modulators

Basic Description

SynonymsFT-0710163 | UNII-39RRC0G27V | DS-19919 | N-(bis(4-methoxyphenyl)methyl)-6-oxo-2-(pyridazin-3-yl)-1,6-dihydropyrimidine-5-carboxamide | CCG-269164 | BDBM50563889 | SCHEMBL24575031 | 39RRC0G27V | BCP25371 | N-[bis(4-methoxyphenyl)methyl]-6-oxo-2-pyridazin-
Specifications & Purity≥98%
Biochemical and Physiological MechanismsMK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

Information

MK-8617 is an pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1 , 2 , 3 with IC50s of 1.0, 1.0 and 14 nM, respectively.


Targets

PHD1 (Cell-free assay); PHD2 (Cell-free assay); PHD3 (Cell-free assay) 1 nM; 1 nM; 14 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.


In vivo

Tritiated MK-8617 exhibits minimal metabolic turnover in liver microsomes (+NADPH) from rat, dog, and monkey (<10% turover) but significant turnover in human liver microsomes (34% turnover) after 60 min (10 μM compound, 1 mg/mL microsomal protein). In terms of its pharmacokinetic profile, MK-8617 shows good oral bioavailability across species (36−71%), with low clearance and volume of distribution. The compound still has a relatively long elimination half-life across preclinical species. In mice (C57Bl/6), single doses of 5 and 15 mpk po (n = 3) causes increases in circulating reticulocytes measured on both 3 and 4 days postcompound challenge. In rat (Sprague−Dawley), a single dose titration of 1.5, 5, and 15 mpk po (n = 5) causes a large increase in serum erythropoietin(EPO) levels of 1.7-, 8-, and 204-fold relative to vehicle, respectively. Increases in circulating reticulocytes are observed at 5 and 15 mg/kg 3 days after challenge and, with the 15 mg dose, at 4 days after challenge.

Product Properties

ALogP3.149
HBD Count2
Rotatable Bond7

Associated Targets(Human)

EGLN1 Tclin Egl nine homolog 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGLN3 Tclin Egl nine homolog 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGLN2 Tclin Egl nine homolog 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EGLN2 Tclin Hypoxia-inducible factor prolyl hydroxylase 1 (404 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EGLN1 Tclin Egl nine homolog 1 (1702 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[bis(4-methoxyphenyl)methyl]-6-oxo-2-pyridazin-3-yl-1H-pyrimidine-5-carboxamide
INCHI InChI=1S/C24H21N5O4/c1-32-17-9-5-15(6-10-17)21(16-7-11-18(33-2)12-8-16)27-23(30)19-14-25-22(28-24(19)31)20-4-3-13-26-29-20/h3-14,21H,1-2H3,(H,27,30)(H,25,28,31)
InChi Key WXLPERVDMILVIF-UHFFFAOYSA-N
Canonical SMILES COC1=CC=C(C=C1)C(C2=CC=C(C=C2)OC)NC(=O)C3=CN=C(NC3=O)C4=NN=CC=C4
Isomeric SMILES COC1=CC=C(C=C1)C(C2=CC=C(C=C2)OC)NC(=O)C3=CN=C(NC3=O)C4=NN=CC=C4
PubChem CID 44230662
Molecular Weight 443.45

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot NumberCertificate TypeDateItem
C2308805Certificate of AnalysisNov 21, 2022 M414011
C2308806Certificate of AnalysisNov 21, 2022 M414011
C2308807Certificate of AnalysisNov 21, 2022 M414011
C2308896Certificate of AnalysisNov 21, 2022 M414011
C2308920Certificate of AnalysisNov 21, 2022 M414011

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 10 mg/mL warmed with 50ºC Water: bath (22.55 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility20
DMSO(mM) Max Solubility45.10091329
Water(mg / mL) Max Solubility<1

Related Documents

Solution Calculators