详情描述
Desidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis.
Product information
CAS Number: 1616690-16-4
Molecular Weight: 332.31
Formula: C16H16N2O6
Synonym:
ZYAN1
ZYAN1-1001
Chemical Name: N-[1-(cyclopropylmethoxy)-4-hydroxy-2-oxo- 1,2-dihydroquinoline-3-carbonyl]glycine
Smiles: OC(=O)CNC(=O)C1C(=O)N(OCC2CC2)C2=CC=CC=C2C=1O
InChiKey: IKRKQQLJYBAPQT-UHFFFAOYSA-N
InChi: InChI=1S/C16H16N2O6/c19-12(20)7-17-15(22)13-14(21)10-3-1-2-4-11(10)18(16(13)23)24-8-9-5-6-9/h1-4,9,21H,5-8H2,(H,17,22)(H,19,20)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO 10 mg/mL (30.09 mM) Ethanol 2 mg/mL (6.02 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 Vivo:
In BALB/c mice, a single dose treatment of desidustat attenuates the effect of lipopolysaccharide (LPS) - or turpentine oil-induced inflammation and increased serum erythropoietin (EPO), iron, and reticulocyte count, and decreases serum hepcidin levels. In turpentine oil-induced anemia in BALB/c mice, repeated dose desidustat treatment increases hemoglobin, RBC and hematocrit in a dose related manner. In female Lewis rats, treatment with desidustat markedly reduces PGPS-induced anemia and increases hemoglobin, red blood cell (RBC) and white blood cell (WBC) count, hematocrit, serum iron and spleen iron.
References:
- Deven V Parmar, et al. Am J Nephrol. 2019;49(6):470-478.
- Mukul Jain, et al. Eur J Pharmacol. 2019 Jan 15;843:113-120.
Products are for research use only. Not for human use.