Desidustat
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561109

CAS#: 1616690-16-4

Description: Desidustat, also known as ZYan1, is an antianaemic drug candidate.


Chemical Structure

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Desidustat
CAS# 1616690-16-4

Theoretical Analysis

MedKoo Cat#: 561109
Name: Desidustat
CAS#: 1616690-16-4
Chemical Formula: C16H16N2O6
Exact Mass: 332.1008
Molecular Weight: 332.312
Elemental Analysis: C, 57.83; H, 4.85; N, 8.43; O, 28.89

Price and Availability

Size Price Availability Quantity
50.0mg USD 450.0 2 weeks
100.0mg USD 750.0 2 weeks
200.0mg USD 1250.0 2 weeks
500.0mg USD 1950.0 2 weeks
1.0g USD 3450.0 2 weeks
2.0g USD 4850.0 2 weeks
5.0g USD 7650.0 2 weeks
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Synonym: Desidustat, ZYan1; ZYan-1; ZYan 1;

IUPAC/Chemical Name: N-[1-(cyclopropylmethoxy)-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl]glycine

InChi Key: IKRKQQLJYBAPQT-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(O)CNC(C1=C(O)C2=C(N(OCC3CC3)C1=O)C=CC=C2)=O

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Product Data:

Biological target: Desidustat is an inhibitor of HIF hydroxylase extracted from patent WO 2014102818 A1, compound example 2.
In vitro activity: TBD
In vivo activity: In this study, the effect of desidustat on the inflammatory and fibrotic changes was investigated in preclinical models of acute and chronic kidney injury. Acute kidney injury was induced in male Sprague Dawley rats by ischemia-reperfusion, in which effect of desidustat (15 mg/kg, PO) was estimated. In a separate experiment, male C57 mice were treated with adenine for 14 days to induce CKD. These mice were treated with desidustat (15 mg/kg, PO, alternate day) treatment for 14 days, with adenine continued. Desidustat prevented elevation of serum creatinine, urea, IL-1β, IL-6, and kidney injury molecule-1 (KIM-1), and elevated the erythropoietin levels in rats that were subjected to acute kidney injury. Mice treated with adenine developed CKD and anemia, and desidustat treatment caused improvement in serum creatinine, urea, and also improved hemoglobin and reduced hepatic and serum hepcidin. A significant reduction in IL-1β, IL-6, myeloperoxidase (MPO) and oxidative stress was observed by desidustat treatment. Desidustat treatment also reduced renal fibrosis as observed by histological analysis and hydroxyproline content. Desidustat treatment reduced the renal fibrosis and inflammation along with a reduction in anemia in preclinical models of kidney injury, which may translate to protective effects in CKD patients. Reference: Drug Dev Res. 2021 Jan 22. https://pubmed.ncbi.nlm.nih.gov/33480036/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.0 24.07
Ethanol 2.0 6.02

Preparing Stock Solutions

The following data is based on the product molecular weight 332.312 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Jain M, Joharapurkar A, Patel V, Kshirsagar S, Sutariya B, Patel M, Patel H, Patel PR. Pharmacological inhibition of prolyl hydroxylase protects against inflammation-induced anemia via efficient erythropoiesis and hepcidin downregulation. Eur J Pharmacol. 2019 Jan 15;843:113-120. doi: 10.1016/j.ejphar.2018.11.023. Epub 2018 Nov 17. PMID: 30458168. 2. Joharapurkar AA, Patel VJ, Kshirsagar SG, Patel MS, Savsani HH, Jain MR. Prolyl hydroxylase inhibitor desidustat protects against acute and chronic kidney injury by reducing inflammatory cytokines and oxidative stress. Drug Dev Res. 2021 Jan 22. doi: 10.1002/ddr.21792. Epub ahead of print. PMID: 33480036.
In vitro protocol: TBD
In vivo protocol: 1. Jain M, Joharapurkar A, Patel V, Kshirsagar S, Sutariya B, Patel M, Patel H, Patel PR. Pharmacological inhibition of prolyl hydroxylase protects against inflammation-induced anemia via efficient erythropoiesis and hepcidin downregulation. Eur J Pharmacol. 2019 Jan 15;843:113-120. doi: 10.1016/j.ejphar.2018.11.023. Epub 2018 Nov 17. PMID: 30458168. 2. Joharapurkar AA, Patel VJ, Kshirsagar SG, Patel MS, Savsani HH, Jain MR. Prolyl hydroxylase inhibitor desidustat protects against acute and chronic kidney injury by reducing inflammatory cytokines and oxidative stress. Drug Dev Res. 2021 Jan 22. doi: 10.1002/ddr.21792. Epub ahead of print. PMID: 33480036.

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