JTZ-951( JTZ 951 | JTZ951 | Enarodustat )

Catalog No. M11090 CAS No. 1262132-81-9

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

JTZ-951
Note

Research use only, not for human use.
Brief Description

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
Description

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2; increases EPO release from Hep3B cells with EC50 of 5.7 uM, increases hemoglobin levels in rats.Anemia Phase 2 Clinical(In Vitro):Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat exhibits neither CYP (IC50 > 100 μM; CYP3A4/5, CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2C8, CYP2B6) nor hERG (IC50 > 100 μM) inhibition.(In Vivo):Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats.
In Vitro

Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat exhibits neither CYP (IC50 > 100 μM; CYP3A4/5, CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2C8, CYP2B6) nor hERG (IC50 > 100 μM) inhibition.
In Vivo

Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats.
Synonyms

JTZ 951 | JTZ951 | Enarodustat
Pathway

Angiogenesis
Target

HIF/HIF Prolyl-hydroxylase
Recptor

HIF/HIF Prolyl-hydroxylase
Research Area

Other Indications
Indication

Anemia

CAS Number

1262132-81-9
Formula Weight

340.339
Molecular Formula

C17H16N4O4
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 83.33 mg/mL (244.85 mM)
SMILES

O=C(O)CNC(C1=C(O)C=C(CCC2=CC=CC=C2)N3C1=NC=N3)=O
Chemical Name

(7-hydroxy-5-phenethyl-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)glycine

1. Yosuke Ogoshi, et al. ACS Med. Chem. Lett., 2017, 8 (12), pp 1320-1325.

Calculator

molnova catalog