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MedKoo Cat#: 326692 | Name: Avosentan
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Description:

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

Avosentan, also known as SPP301, R-639, and RO 67-0565, is an endothelin receptor antagonist. Avosentan ameliorates nephropathy and atherosclerosis in diabetic apolipoprotein E knockout mice. Avosentan is protective in hypertensive nephropathy at doses not causing fluid retention. Avosentan reduces albuminuria when added to standard treatment in people with type 2 diabetes and overt nephropathy but induces significant fluid overload and congestive heart failure.

Chemical Structure

Avosentan
Avosentan
CAS#290815-26-8

Theoretical Analysis

MedKoo Cat#: 326692

Name: Avosentan

CAS#: 290815-26-8

Chemical Formula: C23H21N5O5S

Exact Mass: 479.1263

Molecular Weight: 479.51

Elemental Analysis: C, 57.61; H, 4.41; N, 14.61; O, 16.68; S, 6.69

Price and Availability

Size Price Availability Quantity
5mg USD 300.00 2 Weeks
10mg USD 550.00 2 Weeks
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Related CAS #
No Data
Synonym
SPP301; SPP301; SPP301; RO 67-0565; RO-67-0565; RO67-0565; R-639; Avosentan
IUPAC/Chemical Name
5-methylpyridine-2-sulfonic acid (6-methoxy-5-(2-methoxyphenoxy)-2-(pyridin-4-yl)pyrimidin-4-yl)amide
InChi Key
YBWLTKFZAOSWSM-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H21N5O5S/c1-15-8-9-19(25-14-15)34(29,30)28-22-20(33-18-7-5-4-6-17(18)31-2)23(32-3)27-21(26-22)16-10-12-24-13-11-16/h4-14H,1-3H3,(H,26,27,28)
SMILES Code
O=S(C1=NC=C(C)C=C1)(NC2=NC(C3=CC=NC=C3)=NC(OC)=C2OC4=CC=CC=C4OC)=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, 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

Preparing Stock Solutions

The following data is based on the product molecular weight 479.51 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
1: Baltatu OC, Zaugg CE, Schumacher C, Louie P, Campos LA, Bader M. Avosentan is protective in hypertensive nephropathy at doses not causing fluid retention. Pharmacol Res. 2014 Feb;80:9-13. doi: 10.1016/j.phrs.2013.12.003. Epub 2013 Dec 22. PMID: 24368192. 2: Mann JF, Green D, Jamerson K, Ruilope LM, Kuranoff SJ, Littke T, Viberti G; ASCEND Study Group. Avosentan for overt diabetic nephropathy. J Am Soc Nephrol. 2010 Mar;21(3):527-35. doi: 10.1681/ASN.2009060593. Epub 2010 Feb 18. PMID: 20167702; PMCID: PMC2831858. 3: Wenzel RR, Littke T, Kuranoff S, Jürgens C, Bruck H, Ritz E, Philipp T, Mitchell A; SPP301 (Avosentan) Endothelin Antagonist Evaluation in Diabetic Nephropathy Study Investigators. Avosentan reduces albumin excretion in diabetics with macroalbuminuria. J Am Soc Nephrol. 2009 Mar;20(3):655-64. doi: 10.1681/ASN.2008050482. Epub 2009 Jan 14. PMID: 19144760; PMCID: PMC2653691. 4: Konieczka K, Meyer P, Schoetzau A, Neutzner A, Mozaffarieh M, Flammer J. Effect of avosentan (SPP-301) in porcine ciliary arteries. Curr Eye Res. 2011 Feb;36(2):118-24. doi: 10.3109/02713683.2010.529982. PMID: 21281066. 5: Dieterle W, Hengelage T. Absolute bioavailability and pharmacokinetics of avosentan in man. Int J Clin Pharmacol Ther. 2009 Sep;47(9):587-94. doi: 10.5414/cpp47587. PMID: 19761718. 6: Watson AM, Li J, Schumacher C, de Gasparo M, Feng B, Thomas MC, Allen TJ, Cooper ME, Jandeleit-Dahm KA. The endothelin receptor antagonist avosentan ameliorates nephropathy and atherosclerosis in diabetic apolipoprotein E knockout mice. Diabetologia. 2010 Jan;53(1):192-203. doi: 10.1007/s00125-009-1540-3. Epub 2009 Oct 28. PMID: 19862499. 7: Dieterle W, Mann J. Influence of avosentan (SPP3OI) on the pharmacokinetics of a second generation oral contraceptive containing ethinylestradiol and levonorgestrel in healthy female volunteers. Int J Clin Pharmacol Ther. 2006 Dec;44(12):668-74. doi: 10.5414/cpp44668. PMID: 17190377. 8: Smolander J, Vogt B, Maillard M, Zweiacker C, Littke T, Hengelage T, Burnier M. Dose-dependent acute and sustained renal effects of the endothelin receptor antagonist avosentan in healthy subjects. Clin Pharmacol Ther. 2009 Jun;85(6):628-34. doi: 10.1038/clpt.2009.15. Epub 2009 Mar 11. PMID: 19279566. 9: Hoekman J, Lambers Heerspink HJ, Viberti G, Green D, Mann JF, de Zeeuw D. Predictors of congestive heart failure after treatment with an endothelin receptor antagonist. Clin J Am Soc Nephrol. 2014 Mar;9(3):490-8. doi: 10.2215/CJN.07040713. Epub 2014 Jan 9. PMID: 24408122; PMCID: PMC3944766. 10: Baltatu OC, Iliescu R, Zaugg CE, Reckelhoff JF, Louie P, Schumacher C, Campos LA. Antidiuretic effects of the endothelin receptor antagonist avosentan. Front Physiol. 2012 Apr 18;3:103. doi: 10.3389/fphys.2012.00103. PMID: 22529820; PMCID: PMC3328756. 11: 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. PMID: 28468519. 12: Dieterle W, Hengelage T. Influence of food intake on the pharmacokinetics of avosentan in man. Int J Clin Pharmacol Ther. 2008 Sep;46(9):453-8. doi: 10.5414/cpp46453. PMID: 18793575. 13: Martínez-Díaz I, Martos N, Llorens-Cebrià C, Álvarez FJ, Bedard PW, Vergara A, Jacobs-Cachá C, Soler MJ. Endothelin Receptor Antagonists in Kidney Disease. Int J Mol Sci. 2023 Feb 8;24(4):3427. doi: 10.3390/ijms24043427. PMID: 36834836; PMCID: PMC9965540. 14: Kohan DE, Pollock DM. Endothelin antagonists for diabetic and non-diabetic chronic kidney disease. Br J Clin Pharmacol. 2013 Oct;76(4):573-9. doi: 10.1111/bcp.12064. PMID: 23228194; PMCID: PMC3791980. 15: Gagliardini E, Corna D, Zoja C, Sangalli F, Carrara F, Rossi M, Conti S, Rottoli D, Longaretti L, Remuzzi A, Remuzzi G, Benigni A. Unlike each drug alone, lisinopril if combined with avosentan promotes regression of renal lesions in experimental diabetes. Am J Physiol Renal Physiol. 2009 Nov;297(5):F1448-56. doi: 10.1152/ajprenal.00340.2009. Epub 2009 Aug 12. PMID: 19675181. 16: Ahmad N, Veerapalli H, Lankala CR, Castaneda EE, Aziz A, Rockferry AG, Hamid P. Endothelin Receptor Antagonists as a Potential Treatment of Diabetic Nephropathy: A Systematic Review. Cureus. 2021 Nov 7;13(11):e19325. doi: 10.7759/cureus.19325. PMID: 34909290; PMCID: PMC8653857. 17: Stefoni S, Cianciolo G, Baraldi O, Iorio M, Angelini ML. Emerging drugs for chronic kidney disease. Expert Opin Emerg Drugs. 2014 Jun;19(2):183-99. doi: 10.1517/14728214.2014.900044. Epub 2014 May 16. PMID: 24836744. 18: Zhou Y, Chi J, Huang Y, Dong B, Lv W, Wang YG. Efficacy and safety of endothelin receptor antagonists in type 2 diabetic kidney disease: A systematic review and meta-analysis of randomized controlled trials. Diabet Med. 2021 Jan;38(1):e14411. doi: 10.1111/dme.14411. Epub 2020 Oct 9. PMID: 33000477. 19: Rabelink TJ, Kohan DE. Endothelin receptor blockade in patients with diabetic nephropathy. Contrib Nephrol. 2011;172:235-242. doi: 10.1159/000328703. Epub 2011 Aug 30. PMID: 21894003. 20: Fernández Fernández B, Elewa U, Sánchez-Niño MD, Rojas-Rivera JE, Martin- Cleary C, Egido J, Ortiz A. 2012 update on diabetic kidney disease: the expanding spectrum, novel pathogenic insights and recent clinical trials. Minerva Med. 2012 Aug;103(4):219-34. PMID: 22805616.

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PC DBCO-PEG4-NHS ester

PC DBCO-PEG4-NHS ester