Enarodustat (JTZ-951) - 10mM in DMSO, high purity , CAS No.1262132-81-9

Item Number
E421099
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E421099-1ml
1ml
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$241.90

HIF Inhibitors

Basic Description

SynonymsC17H16N4O4 | CS-0031647 | Glycine, N-((7-hydroxy-5-(2-phenylethyl)(1,2,4)triazolo(1,5-a)pyridin-8-yl)carbonyl)- | JSK7TUA223 | UNII-JSK7TUA223 | Enarodustat (JTZ-951) | JTZ 951 | HY-109057 | BJ162590 | DB14985 | EX-A4798 | MS-25187 | 2-(7-Hydroxy-5-phenet
Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsEnarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Information

Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia.

Targets

PHD2 (Cell-free assay); EPO release from Hep3B cells (Cell-based assay) 0.22 μM; 5.7 μM(EC50)

In vitro

Enarodustat (JTZ-951) inhibits PHD2 with IC50 of 0.22 μM and the EPO release from Hep3B cells with EC50 of 5.7 μM.

In vivo

JTZ-951 (compound 14), with a 5-phenethyl substituent on the triazolopyridine group, increases hemoglobin levels with daily oral dosing in rats. JTZ-951 is rapidly absorbed after oral administration and disappears shortly thereafter, which can be advantageous in terms of safety. JTZ-951 is selected as a clinical candidate.

Cell Research(from reference)

Cell lines:Hep3B cells 

Incubation Time:24 h 

Product Properties

ALogP1.511
HBD Count2
Rotatable Bond6

Associated Targets(Human)

EGLN1 Tclin Egl nine homolog 1 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 2-[[7-oxo-5-(2-phenylethyl)-3H-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl]amino]acetic acid
INCHI InChI=1S/C17H16N4O4/c22-13-8-12(7-6-11-4-2-1-3-5-11)21-16(19-10-20-21)15(13)17(25)18-9-14(23)24/h1-5,8,10H,6-7,9H2,(H,18,25)(H,19,20)(H,23,24)
InChi Key FJYRBJKWDXVHHO-UHFFFAOYSA-N
Canonical SMILES C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O
Isomeric SMILES C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O
PubChem CID 50899324
Molecular Weight 340.33

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

DMSO(mg / mL) Max Solubility68
DMSO(mM) Max Solubility199.806070578556
Water(mg / mL) Max Solubility<1

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