Roxadustat-d5 | CAS#2043026-13-5 | Roxadustat internal standard

MedKoo Cat#: 464788 | Name: Roxadustat-d5

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Description:

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

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS.

Chemical Structure

Roxadustat-d5

CAS#2043026-13-5 (d5-labeled)

Theoretical Analysis

MedKoo Cat#: 464788

Name: Roxadustat-d5

CAS#: 2043026-13-5 (d5-labeled)

Chemical Formula: C19H11D5N2O5

Exact Mass: 357.1373

Molecular Weight: 357.38

Elemental Analysis: C, 63.86; H, 5.92; N, 7.84; O, 22.38

Price and Availability

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1mg	USD 750.00	2 Weeks

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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

Roxadustat-d5; Roxadustat d5;

IUPAC/Chemical Name

(4-hydroxy-1-methyl-7-(phenoxy-d5)isoquinoline-3-carbonyl)glycine

InChi Key

YOZBGTLTNGAVFU-VIQYUKPQSA-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)/i2D,3D,4D,5D,6D

SMILES Code

CC1=NC(C(NCC(O)=O)=O)=C(C2=C1C=C(C=C2)OC3=C(C([2H])=C(C([2H])=C3[2H])[2H])[2H])O

Appearance

Solid powder

Purity

>99% (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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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:

Roxadustat-d5 is deuterium labeled Roxadustat. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells.

In vitro activity:

This study investigated the effect of HIF-1α stabilizer roxadustat on the disruption of tight junction proteins induced by Hcy and CKD and the underlying mechanism. The results indicate that roxadustat attenuated the disruption of epithelial TJPs induced by Hcy in Caco2 cells. Reference: Front Med (Lausanne). 2022 Apr 13;9:850966. https://pubmed.ncbi.nlm.nih.gov/35492370/

In vivo activity:

This study investigated the effects of FG-4592 pretreatment on survival and second choke vessels of multi-territory perforator flaps in rats. They found that pretreatment with roxadustat may improve initial flap survival and dilate the second choke zone vessels in a multi-territory perforator flap. Reference: Open Med (Wars). 2023 Jul 31;18(1):20230762. https://pubmed.ncbi.nlm.nih.gov/37554150/

	Solvent	mg/mL	mM
Solubility
	DMSO	10.0	27.98

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 357.38 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.

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. 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. 2. Qu N, Chen L, Liang S, Wei M, Sun L, He Q, Xue J, Wang M, Shi K, Jiang H, Liu H. Roxadustat Attenuates the Disruption of Epithelial Tight Junction in Caco2 Cells and a Rat Model of CKD Through MicroRNA-223. Front Med (Lausanne). 2022 Apr 13;9:850966. doi: 10.3389/fmed.2022.850966. PMID: 35492370; PMCID: PMC9043115. 3. Tao X, Pan X, Rui Y, Xue M. Effects of pharmacological delay with roxadustat on multi-territory perforator flap survival in rats. Open Med (Wars). 2023 Jul 31;18(1):20230762. doi: 10.1515/med-2023-0762. PMID: 37554150; PMCID: PMC10404892. 4. Chen J, Lin X, Yao C, Bingwa LA, Wang H, Lin Z, Jin K, Zhuge Q, Yang S. Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats. CNS Neurosci Ther. 2022 Oct;28(10):1519-1531. doi: 10.1111/cns.13890. Epub 2022 Jun 13. PMID: 35695696; PMCID: PMC9437235.

In vitro protocol:

In vivo protocol:

1. Tao X, Pan X, Rui Y, Xue M. Effects of pharmacological delay with roxadustat on multi-territory perforator flap survival in rats. Open Med (Wars). 2023 Jul 31;18(1):20230762. doi: 10.1515/med-2023-0762. PMID: 37554150; PMCID: PMC10404892. 2. Chen J, Lin X, Yao C, Bingwa LA, Wang H, Lin Z, Jin K, Zhuge Q, Yang S. Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats. CNS Neurosci Ther. 2022 Oct;28(10):1519-1531. doi: 10.1111/cns.13890. Epub 2022 Jun 13. PMID: 35695696; PMCID: PMC9437235.

1: Wu R, Peng Y. Roxadustat on anti-erythropoietin antibody-related pure red cell aplasia in the patient with end-stage renal disease. Semin Dial. 2021 Jun 15. doi: 10.1111/sdi.12991. Epub ahead of print. PMID: 34128578. 2: Zhang L, Hou J, Li J, Su SS, Xue S. Roxadustat for the treatment of anemia in patients with chronic kidney diseases: a meta-analysis. Aging (Albany NY). 2021 Jun 11;13. doi: 10.18632/aging.203143. Epub ahead of print. PMID: 34115611. 3: Barratt J, Andric B, Tataradze A, Schömig M, Reusch M, Valluri U, Mariat C. Roxadustat for the treatment of anaemia in chronic kidney disease patients not on dialysis: a phase 3, randomised, open-label, active-controlled study (DOLOMITES). Nephrol Dial Transplant. 2021 Jun 2:gfab191. doi: 10.1093/ndt/gfab191. Epub ahead of print. PMID: 34077510. 4: Ikenoue T, Furumatsu Y, Kitamura T. Transfusion-dependent anaemia treatment using continuous erythropoietin receptor activator (epoetin β pegol) and roxadustat after darbepoetin treatment failure in low-risk myelodysplastic syndrome: a case report. Oxf Med Case Reports. 2021 May 24;2021(5):omab026. doi: 10.1093/omcr/omab026. PMID: 34055362; PMCID: PMC8143669. 5: Fei M, Wen XQ, Yu ZL, Kang T, Wu WH, Ou ST. Roxadustat as treatment for a blood transfusion-dependent maintenance hemodialysis patient: A case report and review of literature. World J Clin Cases. 2021 May 26;9(15):3680-3688. doi: 10.12998/wjcc.v9.i15.3680. PMID: 34046470; PMCID: PMC8130086. 6: De Backer J, Maric D, Bosman M, Dewilde S, Hoogewijs D. A reliable set of reference genes to normalize oxygen-dependent cytoglobin gene expression levels in melanoma. Sci Rep. 2021 May 25;11(1):10879. doi: 10.1038/s41598-021-90284-6. PMID: 34035373; PMCID: PMC8149659. 7: Zhou Y, Chen XX, Zhang YF, Lou JZ, Yuan HB. Roxadustat for dialysis patients with erythropoietin hypo-responsiveness: a single-center, prospective investigation. Intern Emerg Med. 2021 May 22. doi: 10.1007/s11739-021-02738-4. Epub ahead of print. PMID: 34021853. 8: Miao AF, Liang JX, Yao L, Han JL, Zhou LJ. Hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) protects against renal ischemia/reperfusion injury by inhibiting inflammation. Ren Fail. 2021 Dec;43(1):803-810. doi: 10.1080/0886022X.2021.1915801. PMID: 33966598; PMCID: PMC8118507. 9: Wang H, Huang K, Wang C, Chen C, Fang H, Cao J. Effectiveness and safety of roxadustat in the treatment of anemia of kidney disease: a systematic review and meta-analysis. Ann Palliat Med. 2021 Apr;10(4):4736-4746. doi: 10.21037/apm-21-456. PMID: 33966423. 10: Groenendaal-van de Meent D, Kerbusch V, Barroso-Fernandez B, den Adel M, van Dijk J, Golor G, Schaddelee M. Effect of the Phosphate Binders Sevelamer Carbonate and Calcium Acetate on the Pharmacokinetics of Roxadustat After Concomitant or Time-Separated Administration in Healthy Individuals. Clin Ther. 2021 May 4:S0149-2918(21)00160-0. doi: 10.1016/j.clinthera.2021.03.025. Epub ahead of print. PMID: 33962762. 11: Tokuyama A, Kadoya H, Obata A, Obata T, Sasaki T, Kashihara N. Roxadustat and thyroid-stimulating hormone suppression. Clin Kidney J. 2021 Jan 20;14(5):1472-1474. doi: 10.1093/ckj/sfab007. PMID: 33959275; PMCID: PMC8087136. 12: Ugawa T, Ashizaki M, Murata A, Majikawa Y. [Roxadustat (Evrenzo® tablet), a therapeutic drug for renal anemia: pharmacological characteristics and clinical evidence in Japan]. Nihon Yakurigaku Zasshi. 2021;156(3):187-197. Japanese. doi: 10.1254/fpj.21001. PMID: 33952849. 13: Gaihre B, Liu X, Li L, Lee Miller Ii A, Camilleri ET, Li Y, Waletzki B, Lu L. Bifunctional hydrogel for potential vascularized bone tissue regeneration. Mater Sci Eng C Mater Biol Appl. 2021 May;124:112075. doi: 10.1016/j.msec.2021.112075. Epub 2021 Mar 24. PMID: 33947567. 14: van Kuijk K, Demandt JAF, Perales-Patón J, Theelen TL, Kuppe C, Marsch E, de Bruijn J, Jin H, Gijbels MJ, Matic L, Mees BME, Reutelingsperger CPM, Hedin U, Biessen EAL, Carmeliet P, Baker AH, Kramann RK, Schurgers LJ, Saez-Rodriguez J, Sluimer JC. DEFICIENCY OF MYELOID PHD PROTEINS AGGRAVATES ATHEROGENESIS VIA MACROPHAGE APOPTOSIS AND PARACRINE FIBROTIC SIGNALING: Atherogenic effects of myeloid PHD knockdown. Cardiovasc Res. 2021 Apr 26:cvab152. doi: 10.1093/cvr/cvab152. Epub ahead of print. PMID: 33913468. 15: Burmakin M, Fasching A, Kobayashi H, Urrutia AA, Damdimopoulos A, Palm F, Haase VH. Pharmacological HIF-PHD inhibition reduces renovascular resistance and increases glomerular filtration by stimulating nitric oxide generation. Acta Physiol (Oxf). 2021 Apr 26:e13668. doi: 10.1111/apha.13668. Epub ahead of print. PMID: 33900001. 16: Huang LT, Chou HC, Chen CM. Roxadustat attenuates hyperoxia-induced lung injury by upregulating proangiogenic factors in newborn mice. Pediatr Neonatol. 2021 Mar 24:S1875-9572(21)00054-1. doi: 10.1016/j.pedneo.2021.03.012. Epub ahead of print. PMID: 33865748. 17: Cai KD, Zhu BX, Lin HX, Luo Q. Successful application of roxadustat in the treatment of patients with anti-erythropoietin antibody-mediated renal anaemia: a case report and literature review. J Int Med Res. 2021 Apr;49(4):3000605211005984. doi: 10.1177/03000605211005984. PMID: 33853432; PMCID: PMC8054214. 18: Wing PAC, Keeley TP, Zhuang X, Lee JY, Prange-Barczynska M, Tsukuda S, Morgan SB, Harding AC, Argles ILA, Kurlekar S, Noerenberg M, Thompson CP, Huang KA, Balfe P, Watashi K, Castello A, Hinks TSC, James W, Ratcliffe PJ, Davis I, Hodson EJ, Bishop T, McKeating JA. Hypoxic and pharmacological activation of HIF inhibits SARS-CoV-2 infection of lung epithelial cells. Cell Rep. 2021 Apr 20;35(3):109020. doi: 10.1016/j.celrep.2021.109020. Epub 2021 Apr 5. PMID: 33852916; PMCID: PMC8020087. 19: Eleftheriadis T, Pissas G, Liakopoulos V, Stefanidis I. On the Increased Event Rate of Urinary Tract Infection and Pneumonia in CKD Patients Treated with Roxadustat for Anemia. J Am Soc Nephrol. 2021 Jun 1;32(6):1537. doi: 10.1681/ASN.2021020204. Epub 2021 Apr 13. PMID: 33849917. 20: van Vliet T, Varela-Eirin M, Wang B, Borghesan M, Brandenburg SM, Franzin R, Evangelou K, Seelen M, Gorgoulis V, Demaria M. Physiological hypoxia restrains the senescence-associated secretory phenotype via AMPK-mediated mTOR suppression. Mol Cell. 2021 May 6;81(9):2041-2052.e6. doi: 10.1016/j.molcel.2021.03.018. Epub 2021 Apr 5. PMID: 33823141.