WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H593046
CAS#: 178738-96-0 (sodium)
Description: Atrasentan, also known as ABT-627, is a orally available ETA receptor antagonist with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.
Hodoodo Cat#: H593046
Name: Atrasentan sodium
CAS#: 178738-96-0 (sodium)
Chemical Formula: C29H37N2NaO6
Exact Mass: 510.27
Molecular Weight: 532.610
Elemental Analysis: C, 65.40; H, 7.00; N, 5.26; Na, 4.32; O, 18.02
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 195733-43-8 (HCl) 173937-91-2 (free base) 178738-96-0 (sodium) 195704-72-4 (free base)
Synonym: Atrasentan sodium; Atrasentan; (+) A 127722; A 127722; ABT627; ABT 627; ABT-627; NSC720763; A147627; Abbott 147627; US brand name: Xinlay;
IUPAC/Chemical Name: sodium (2R,3R,4S)-4-(benzo[d][1,3]dioxol-5-yl)-1-(2-(dibutylamino)-2-oxoethyl)-2-(4-methoxyphenyl)pyrrolidine-3-carboxylate
InChi Key: JQWVNUYJUQFYPN-SQMFDTLJSA-M
InChi Code: InChI=1S/C29H38N2O6.Na/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20;/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34);/q;+1/p-1/t23-,27-,28+;/m1./s1
SMILES Code: O=C(O[Na])[C@H]1[C@@H](N(C[C@@H]1C2=CC=C3OCOC3=C2)CC(N(CCCC)CCCC)=O)C4=CC=C(C=C4)OC
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: >3 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: 2934.99.03.00
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 532.61 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Unger JM, Griffin K, Donaldson GW, Baranowski KM, Good MJ, Reburiano E, Hussain M, Monk PJ, Van Veldhuizen PJ, Carducci MA, Higano CS, Lara PN, Tangen CM, Quinn DI, Wade JL, Iii, Vogelzang NJ, Thompson IM, Jr, Moinpour CM. Patient-reported outcomes for patients with metastatic castration-resistant prostate cancer receiving docetaxel and Atrasentan versus docetaxel and placebo in a randomized phase III clinical trial (SWOG S0421). J Patient Rep Outcomes. 2018 Jun 13;2:27. doi: 10.1186/s41687-018-0054-5. eCollection 2017. PubMed PMID: 29951640; PubMed Central PMCID: PMC5997724.
2: Spires D, Poudel B, Shields CA, Pennington A, Fizer B, Taylor L, McPherson KC, Cornelius DC, Williams JM. Prevention of the progression of renal injury in diabetic rodent models with pre-existing renal disease with chronic endothelin A receptor blockade. Am J Physiol Renal Physiol. 2018 May 30. doi: 10.1152/ajprenal.00182.2018. [Epub ahead of print] PubMed PMID: 29846112.
3: Wang Y, Zhang H, Shen W, He P, Zhou Z. Effectiveness and tolerability of targeted drugs for the treatment of metastatic castration-resistant prostate cancer: a network meta-analysis of randomized controlled trials. J Cancer Res Clin Oncol. 2018 Sep;144(9):1751-1768. doi: 10.1007/s00432-018-2664-y. Epub 2018 May 24. Review. PubMed PMID: 29797220.
4: Burnier M. Update on Endothelin Receptor Antagonists in Hypertension. Curr Hypertens Rep. 2018 May 19;20(6):51. doi: 10.1007/s11906-018-0848-0. Review. PubMed PMID: 29779164.
5: Panchapakesan U, Pollock C. Drug repurposing in kidney disease. Kidney Int. 2018 Jul;94(1):40-48. doi: 10.1016/j.kint.2017.12.026. Epub 2018 Apr 6. Review. PubMed PMID: 29628139.
6: Kang WL, Xu GS. Corrigendum: Atrasentan increased the expression of klotho by mediating miR-199b-5p and prevented renal tubular injury in diabetic nephropathy. Sci Rep. 2018 Apr 6;8:46965. doi: 10.1038/srep46965. PubMed PMID: 29623952; PubMed Central PMCID: PMC5887050.
7: Heerspink HJL, Andress DL, Bakris G, Brennan JJ, Correa-Rotter R, Hou FF, Kitzman DW, Kohan D, Makino H, McMurray J, Perkovic V, Tobe S, Wigderson M, Yi T, Parving HH, de Zeeuw D. Baseline characteristics and enrichment results from the SONAR trial. Diabetes Obes Metab. 2018 Aug;20(8):1829-1835. doi: 10.1111/dom.13315. Epub 2018 May 1. PubMed PMID: 29604160; PubMed Central PMCID: PMC6055730.
8: Koomen JV, Stevens J, Mostafa NM, Parving HH, de Zeeuw D, Heerspink HJL. Determining the optimal dose of atrasentan by evaluating the exposure-response relationships of albuminuria and bodyweight. Diabetes Obes Metab. 2018 Aug;20(8):2019-2022. doi: 10.1111/dom.13312. Epub 2018 May 1. PubMed PMID: 29603851; PubMed Central PMCID: PMC6055665.
9: Heerspink HJL, Andress DL, Bakris G, Brennan JJ, Correa-Rotter R, Dey J, Hou FF, Kitzman DW, Kohan D, Makino H, McMurray J, Perkovic V, Tobe S, Wigderson M, Parving HH, de Zeeuw D. Rationale and protocol of the Study Of diabetic Nephropathy with AtRasentan (SONAR) trial: A clinical trial design novel to diabetic nephropathy. Diabetes Obes Metab. 2018 Jun;20(6):1369-1376. doi: 10.1111/dom.13245. Epub 2018 Mar 9. PubMed PMID: 29405626; PubMed Central PMCID: PMC5969254.
10: Coelho SC, Berillo O, Caillon A, Ouerd S, Fraulob-Aquino JC, Barhoumi T, Offermanns S, Paradis P, Schiffrin EL. Three-Month Endothelial Human Endothelin-1 Overexpression Causes Blood Pressure Elevation and Vascular and Kidney Injury. Hypertension. 2018 Jan;71(1):208-216. doi: 10.1161/HYPERTENSIONAHA.117.09925. Epub 2017 Nov 13. PubMed PMID: 29133362.
11: Webb DJ, Coll B, Heerspink HJL, Andress D, Pritchett Y, Brennan JJ, Houser M, Correa-Rotter R, Kohan D, Makino H, Perkovic V, Remuzzi G, Tobe SW, Toto R, Busch R, Pergola P, Parving HH, de Zeeuw D. Longitudinal Assessment of the Effect of Atrasentan on Thoracic Bioimpedance in Diabetic Nephropathy: A Randomized, Double-Blind, Placebo-Controlled Trial. Drugs R D. 2017 Sep;17(3):441-448. doi: 10.1007/s40268-017-0201-0. PubMed PMID: 28831752; PubMed Central PMCID: PMC5629141.
12: Lin CW, Mostafa NM, L Andress D, J Brennan J, Klein CE, Awni WM. Relationship Between Atrasentan Concentrations and Urinary Albumin to Creatinine Ratio in Western and Japanese Patients With Diabetic Nephropathy. Clin Ther. 2018 Feb;40(2):242-251. doi: 10.1016/j.clinthera.2017.07.011. Epub 2017 Jul 27. PubMed PMID: 28756065.
13: Sonpavde G, Pond GR, Plets M, Tangen CM, Hussain MHA, Lara PN Jr, Goldkorn A, Garzotto MG, Mack PC, Higano CS, Vogelzang NJ, Thompson IM Jr, Twardowski PW, Van Veldhuizen PJ Jr, Agarwal N, Carducci MA, Monk JP, Quinn DI. Validation of the Association of RECIST Changes With Survival in Men With Metastatic Castration-Resistant Prostate Cancer Treated on SWOG Study S0421. Clin Genitourin Cancer. 2017 Dec;15(6):635-641. doi: 10.1016/j.clgc.2017.05.014. Epub 2017 May 10. PubMed PMID: 28579151; PubMed Central PMCID: PMC5734863.
14: Gibbens J, Morris R, Bowles T, Spencer SK, Wallace K. Dysregulation of the Fas/FasL system in an experimental animal model of HELLP syndrome. Pregnancy Hypertens. 2017 Apr;8:26-30. doi: 10.1016/j.preghy.2017.02.004. Epub 2017 Feb 24. PubMed PMID: 28501275; PubMed Central PMCID: PMC5433259.
15: Egido J, Rojas-Rivera J, Mas S, Ruiz-Ortega M, Sanz AB, Gonzalez Parra E, Gomez-Guerrero C. Atrasentan for the treatment of diabetic nephropathy. Expert Opin Investig Drugs. 2017 Jun;26(6):741-750. doi: 10.1080/13543784.2017.1325872. Review. PubMed PMID: 28468519.
16: Sedláková L, Čertíková Chábová V, Doleželová Š, Škaroupková P, Kopkan L, Husková Z, Červenková L, Kikerlová S, Vaněčková I, Sadowski J, Kompanowska-Jezierska E, Kujal P, Kramer HJ, Červenka L. Renin-angiotensin system blockade alone or combined with ET(A) receptor blockade: effects on the course of chronic kidney disease in 5/6 nephrectomized Ren-2 transgenic hypertensive rats. Clin Exp Hypertens. 2017;39(2):183-195. doi: 10.1080/10641963.2016.1235184. Epub 2017 Mar 1. PubMed PMID: 28287881.
17: Pena MJ, de Zeeuw D, Andress D, Brennan JJ, Correa-Rotter R, Coll B, Kohan DE, Makino H, Perkovic V, Remuzzi G, Tobe SW, Toto R, Parving HH, Sharma S, Corringham T, Sharma K, Heerspink HJL. The effects of atrasentan on urinary metabolites in patients with type 2 diabetes and nephropathy. Diabetes Obes Metab. 2017 May;19(5):749-753. doi: 10.1111/dom.12864. Epub 2017 Feb 22. PubMed PMID: 28019071.
18: Larivière R, Gauthier-Bastien A, Ung RV, St-Hilaire J, Mac-Way F, Richard DE, Agharazii M. Endothelin type A receptor blockade reduces vascular calcification and inflammation in rats with chronic kidney disease. J Hypertens. 2017 Feb;35(2):376-384. doi: 10.1097/HJH.0000000000001161. PubMed PMID: 28005706.
19: Petrykiv SI, de Zeeuw D, Persson F, Rossing P, Gansevoort RT, Laverman GD, Heerspink HJL. Variability in response to albuminuria-lowering drugs: true or random? Br J Clin Pharmacol. 2017 Jun;83(6):1197-1204. doi: 10.1111/bcp.13217. Epub 2017 Feb 1. PubMed PMID: 28002889; PubMed Central PMCID: PMC5427237.
20: Lee TM, Chang NC, Lin SZ. Inhibition of infarction-induced sympathetic innervation with endothelin receptor antagonism via a PI3K/GSK-3β-dependent pathway. Lab Invest. 2017 Mar;97(3):243-255. doi: 10.1038/labinvest.2016.138. Epub 2016 Dec 19. PubMed PMID: 27991911.
