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

Hodoodo CAT#: H317133

CAS#: 808118-40-3 (free)

Description: Roxadustat, also known as ASP1517 and FG-4592, is an HIF α prolyl hydroxylase inhibitor in a cell-free assay. It stabilizes HIF-2 and induces EPO production and stimulates erythropoiesis. Roxadustat transiently and moderately increased endogenous erythropoietin and reduced hepcidin.

Chemical Structure

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Roxadustat
CAS# 808118-40-3 (free)
Instruction

Theoretical Analysis

Hodoodo Cat#: H317133
Name: Roxadustat
CAS#: 808118-40-3 (free)
Chemical Formula: C19H16N2O5
Exact Mass: 352.11
Molecular Weight: 352.350
Elemental Analysis: C, 64.77; H, 4.58; N, 7.95; O, 22.70

Price and Availability

Size Price Availability Quantity
25mg USD 110 Ready to ship
50mg USD 180 Ready to ship
100mg USD 300 Ready to ship
200mg USD 500 Ready to ship
500mg USD 1050 Ready to ship
1g USD 1950 Ready to ship
2g USD 3450 Ready to ship
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Related CAS #: 2043026-13-5 (d5-labeled)   808118-40-3 (free)   1537180-01-0 (HCl)   1537180-03-2 (mesylate)   1537179-94-4 (sodium)   1537179-95-5 (potassium)    

Synonym: ASP1517; ASP 1517; ASP-1517; FG-4592; FG 4592; FG4592; Roxadustat.

IUPAC/Chemical Name: (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine

InChi Key: YOZBGTLTNGAVFU-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)

SMILES Code: O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O

Appearance: White to off- white 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, not in water

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:

Biological target: Roxadustat is a hypoxia-inducible factor prolyl-hydroxylase inhibitor (HIF-PHI).
In vitro activity: The in vitro effects of roxadustat on cobalt chloride (CoCl2)-stimulated pulmonary fibrosis were investigated with L929 mouse fibroblasts. The proliferation of L929 cells was inhibited and the production of collagen I, collagen III, prolyl hydroxylase domain protein 2 (PHD2), HIF-1α, α-smooth muscle actin (α-SMA), connective tissue growth factor (CTGF), transforming growth factor-β1 (TGF-β1) and p-Smad3 were reduced relative to that in the CoCl2 after roxadustat treatment. Reference: Toxicol Lett. 2020 Oct 1;331:112-121. https://www.sciencedirect.com/science/article/abs/pii/S0378427420302745?via%3Dihub
In vivo activity: The effects of roxadustat on an in vivo pulmonary fibrosismice model induced with bleomycin (BLM; intraperitoneal injection, 50 mg/kg twice a week for 4 continuous weeks) were investigated. Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1α, α-SMA, CTGF, TGF-β1 and p-Smad3/Smad3. Reference: Toxicol Lett. 2020 Oct 1;331:112-121. https://www.sciencedirect.com/science/article/abs/pii/S0378427420302745?via%3Dihub

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 66.7 189.22
DMF 50.0 141.90
Ethanol 0.1 0.28

Preparing Stock Solutions

The following data is based on the product molecular weight 352.35 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. Zhu Y, Wang Y, Jia Y, Xu J, Chai Y. Roxadustat promotes angiogenesis through HIF-1α/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats. Wound Repair Regen. 2019 Jul;27(4):324-334. doi: 10.1111/wrr.12708. Epub 2019 Feb 28. PMID: 30817065. 2. Huang H, Wang X, Zhang X, Wang H, Jiang W. Roxadustat attenuates experimental pulmonary fibrosis in vitro and in vivo. Toxicol Lett. 2020 Oct 1;331:112-121. doi: 10.1016/j.toxlet.2020.06.009. Epub 2020 Jun 10. PMID: 32534005.
In vitro protocol: 1. Zhu Y, Wang Y, Jia Y, Xu J, Chai Y. Roxadustat promotes angiogenesis through HIF-1α/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats. Wound Repair Regen. 2019 Jul;27(4):324-334. doi: 10.1111/wrr.12708. Epub 2019 Feb 28. PMID: 30817065. 2. Huang H, Wang X, Zhang X, Wang H, Jiang W. Roxadustat attenuates experimental pulmonary fibrosis in vitro and in vivo. Toxicol Lett. 2020 Oct 1;331:112-121. doi: 10.1016/j.toxlet.2020.06.009. Epub 2020 Jun 10. PMID: 32534005.
In vivo protocol: 1. Zhu Y, Wang Y, Jia Y, Xu J, Chai Y. Roxadustat promotes angiogenesis through HIF-1α/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats. Wound Repair Regen. 2019 Jul;27(4):324-334. doi: 10.1111/wrr.12708. Epub 2019 Feb 28. PMID: 30817065. 2. Huang H, Wang X, Zhang X, Wang H, Jiang W. Roxadustat attenuates experimental pulmonary fibrosis in vitro and in vivo. Toxicol Lett. 2020 Oct 1;331:112-121. doi: 10.1016/j.toxlet.2020.06.009. Epub 2020 Jun 10. PMID: 32534005.

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1: Besarab A, Provenzano R, Hertel J, Zabaneh R, Klaus SJ, Lee T, Leong R, Hemmerich S, Yu KH, Neff TB. Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients. Nephrol Dial Transplant. 2015 Oct;30(10):1665-73. doi: 10.1093/ndt/gfv302. Epub 2015 Aug 3. PubMed PMID: 26238121; PubMed Central PMCID: PMC4569392.

2: Forristal CE, Levesque JP. Targeting the hypoxia-sensing pathway in clinical hematology. Stem Cells Transl Med. 2014 Feb;3(2):135-40. doi: 10.5966/sctm.2013-0134. Epub 2013 Dec 26. PubMed PMID: 24371328; PubMed Central PMCID: PMC3925058.

3: Bouchie A. First-in-class anemia drug takes aim at Amgen's dominion. Nat Biotechnol. 2013 Nov;31(11):948-9. doi: 10.1038/nbt1113-948b. PubMed PMID: 24213751.

4: Flight MH. Deal watch: AstraZeneca bets on FibroGen's anaemia drug. Nat Rev Drug Discov. 2013 Oct;12(10):730. doi: 10.1038/nrd4135. PubMed PMID: 24080688.

5: Beuck S, Schänzer W, Thevis M. Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis. Drug Test Anal. 2012 Nov;4(11):830-45. doi: 10.1002/dta.390. Epub 2012 Feb 24. Review. PubMed PMID: 22362605.

6: Cases A. The latest advances in kidney diseases and related disorders. Drug News Perspect. 2007 Dec;20(10):647-54. PubMed PMID: 18301799.