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MedKoo Cat#: 561109 | Name: Desidustat
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Description:

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

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

Chemical Structure

Desidustat
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: 332.31

Elemental Analysis: C, 57.83; H, 4.85; N, 8.43; O, 28.89

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 weeks
100mg USD 750.00 2 weeks
200mg USD 1,250.00 2 weeks
500mg USD 1,950.00 2 weeks
1g USD 3,450.00 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
More Info
Product Data
Product Data
Instruction
View handling instruction
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/
Solvent mg/mL mM
Solubility
DMSO 8.0 24.07
Ethanol 2.0 6.02
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 332.31 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.
1: Dhillon S. Desidustat: First Approval. Drugs. 2022 Jul;82(11):1207-1212. doi: 10.1007/s40265-022-01744-w. PMID: 35834123; PMCID: PMC9281218. 2: Joharapurkar AA, Patel VJ, Kshirsagar SG, Patel MS, Savsani HH, Kajavadara C, Valani D, Jain MR. Prolyl hydroxylase inhibitor desidustat improves anemia in erythropoietin hyporesponsive state. Curr Res Pharmacol Drug Discov. 2022 Apr 30;3:100102. doi: 10.1016/j.crphar.2022.100102. PMID: 35570856; PMCID: PMC9096675. 3: Gang S, Khetan P, Varade D, Chinta VR, Mavani S, Gupta U, Reddy SVK, Rajanna S, Jeloka T, Ruhela V, Kansagra K, Kanani P, Bhatt J, Zala K; Study Investigator Group. Desidustat in Anemia due to Dialysis-Dependent Chronic Kidney Disease: A Phase 3 Study (DREAM-D). Am J Nephrol. 2022;53(5):343-351. doi: 10.1159/000523949. Epub 2022 Apr 22. PMID: 35462369; PMCID: PMC9254304. 4: Agrawal D, Varade D, Shah H, Nazar A, Krishnan J, Shukla V, Ramakrishna C, Bandara Galahitiyawa MC, Mavani SB, Rajanna S, Jikki P, De Silva S, Ruhela V, Koradia P, Kansagra K, Kanani P, Sharma N, Zala K, Parmar D; Study Investigator Group. Desidustat in Anemia due to Non-Dialysis-Dependent Chronic Kidney Disease: A Phase 3 Study (DREAM-ND). Am J Nephrol. 2022;53(5):352-360. doi: 10.1159/000523961. Epub 2022 Apr 22. PMID: 35462372. 5: Zheng Q, Yang H, Sun L, Wei R, Fu X, Wang Y, Huang Y, Liu YN, Liu WJ. Efficacy and safety of HIF prolyl-hydroxylase inhibitor vs epoetin and darbepoetin for anemia in chronic kidney disease patients not undergoing dialysis: A network meta-analysis. Pharmacol Res. 2020 Sep;159:105020. doi: 10.1016/j.phrs.2020.105020. Epub 2020 Jun 16. PMID: 32561478. 6: Patel H, Modi N, Chaudhari J, Patel P, Giri P, Patel H, Pandya V, Desai R, Jain M. Nonclinical Pharmacokinetic Evaluation of Desidustat: a Novel Prolyl Hydroxylase Inhibitor for the Treatment of Anemia. Eur J Drug Metab Pharmacokinet. 2022 Sep;47(5):725-740. doi: 10.1007/s13318-022-00788-3. Epub 2022 Jul 26. PMID: 35881329. 7: 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 Sep;82(6):852-860. doi: 10.1002/ddr.21792. Epub 2021 Jan 22. PMID: 33480036. 8: Chen H, Cheng Q, Wang J, Zhao X, Zhu S. Long-term efficacy and safety of hypoxia-inducible factor prolyl hydroxylase inhibitors in anaemia of chronic kidney disease: A meta-analysis including 13,146 patients. J Clin Pharm Ther. 2021 Aug;46(4):999-1009. doi: 10.1111/jcpt.13385. Epub 2021 Feb 21. PMID: 33615523. 9: Patel H, Momin T, Kansagra K, Patel H, Shah C, Barot A, Bhavsar J, Zala K, Parmar D. A Food-Effect Study to Evaluate the Oral Bioavailability of Desidustat. Clin Pharmacol Drug Dev. 2023 Apr;12(4):356-362. doi: 10.1002/cpdd.1206. Epub 2022 Dec 2. PMID: 36458679. 10: Parmar DV, Kansagra KA, Patel JC, Joshi SN, Sharma NS, Shelat AD, Patel NB, Nakrani VB, Shaikh FA, Patel HV; on behalf of the ZYAN1 Trial Investigators. Outcomes of Desidustat Treatment in People with Anemia and Chronic Kidney Disease: A Phase 2 Study. Am J Nephrol. 2019;49(6):470-478. doi: 10.1159/000500232. Epub 2019 May 21. PMID: 31112954. 11: Philip M, Karakka Kal AK, Subhahar MB, Karatt TK, Mathew B, Perwad Z. In vitro studies of hypoxia inducible factor-prolyl hydroxylase inhibitors daprodustat, desidustat, and vadadustat for equine doping control. Drug Test Anal. 2022 Feb;14(2):317-348. doi: 10.1002/dta.3188. Epub 2021 Nov 25. PMID: 34714596. 12: Sharma S, Jain S. A Novel Spectrophotometric Method Development for Quantification of Desidustat in Bulk and Pharmaceutical Dosage Form. Drug Metab Bioanal Lett. 2023 Aug 28. doi: 10.2174/2949681016666230828150206. Epub ahead of print. PMID: 37642003. 13: Yang J, Xing J, Zhu X, Xie X, Wang L, Zhang X. Effects of hypoxia-inducible factor-prolyl hydroxylase inhibitors vs. erythropoiesis-stimulating agents on iron metabolism in non-dialysis-dependent anemic patients with CKD: A network meta-analysis. Front Endocrinol (Lausanne). 2023 Mar 16;14:1131516. doi: 10.3389/fendo.2023.1131516. PMID: 37008953; PMCID: PMC10060950. 14: 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. 15: Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR. Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. J Med Chem. 2018 Aug 23;61(16):6964-6982. doi: 10.1021/acs.jmedchem.7b01686. Epub 2018 May 9. PMID: 29712435. 16: Mazzarino M, Perretti I, Stacchini C, Comunità F, de la Torre X, Botrè F. UPLC-MS-Based Procedures to Detect Prolyl-Hydroxylase Inhibitors of HIF in Urine. J Anal Toxicol. 2021 Feb 13;45(2):184-194. doi: 10.1093/jat/bkaa055. PMID: 32435795. 17: Janssens LK, Stove CP. Sensing an Oxygen Sensor: Development and Application of Activity-Based Assays Directly Monitoring HIF Heterodimerization. Anal Chem. 2021 Nov 2;93(43):14462-14470. doi: 10.1021/acs.analchem.1c02923. Epub 2021 Oct 22. PMID: 34677954. 18: Chandrasekaran J, Balasubramaniam J. A computational evaluation of FDA medicines' ability to inhibit hypoxia-inducible factor prolyl hydroxylase-2 (PHD-2) for acute respiratory distress syndrome. Struct Chem. 2022;33(5):1391-1407. doi: 10.1007/s11224-022-02012-z. Epub 2022 Jul 9. PMID: 35855326; PMCID: PMC9282623. 19: Chen D, Niu Y, Liu F, Yang Y, Wang X, Li P, Chen X. Safety of HIF prolyl hydroxylase inhibitors for anemia in dialysis patients: a systematic review and network meta-analysis. Front Pharmacol. 2023 May 24;14:1163908. doi: 10.3389/fphar.2023.1163908. PMID: 37292157; PMCID: PMC10244523. 20: Patel H, Soni K, Trivedi R, Heading H, Geue J, Kansagra K, Gupta RJ, Pandya VB, Srinivas NR, Patel PR, Desai RC. A sensitive assay for ZYAN1 in human whole blood and urine utilizing positive LC-MS/MS electrospray ionization. Bioanalysis. 2017 May;9(9):719-732. doi: 10.4155/bio-2017-0014. Epub 2017 May 10. PMID: 28488896.