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.

Product information

CAS Number: 1262132-81-9

Molecular Weight: 340.33

Formula: C17H16N4O4

Chemical Name: N-[7-hydroxy-5-(2-phenylethyl)[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl]glycine

Smiles: OC(=O)CNC(=O)C1C2=NC=NN2C(CCC2C=CC=CC=2)=CC=1O

InChiKey: NALAUGMPMIVAOW-UHFFFAOYSA-N

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/h1-5,8,10,22H,6-7,9H2,(H,18,25)(H,23,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 68 mg/mL (199.81 mM) Ethanol 2.5 mg/mL (7.35 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

References:

1. Yosuke Ogoshi, et al. ACS Med Chem Lett. 2017 Nov 20;8(12):1

Products are for research use only. Not for human use.