WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319599
CAS#: 451470-34-1 (HCl)
Description: Solabegron, also known as GW-427,353, is a selective agonist for the β3 adrenergic receptor. It is being developed for the treatment of overactive bladder and irritable bowel syndrome. It has been shown to produce visceral analgesia by releasing somatostatin from adipocytes. Solabegron decreases excitability of human enteric neurons via release of somatostatin. Solabegron evokes bladder relaxation and increases micturition reflex threshold in the dog.
Hodoodo Cat#: H319599
Name: Solabegron HCl
CAS#: 451470-34-1 (HCl)
Chemical Formula: C23H24Cl2N2O3
Exact Mass: 446.12
Molecular Weight: 447.356
Elemental Analysis: C, 61.75; H, 5.41; Cl, 15.85; N, 6.26; O, 10.73
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
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Note: Price will be listed if it is available in the future.
Related CAS #: 252920-94-8 (free base)
Synonym: GW-427353; GW 427353; GW427353; GW-427,353; GW 427,353; GW427,353; Solabegron; Solabegron HC1; Solabegron hydrochloride.
IUPAC/Chemical Name: (R)-3'-((2-((2-(3-chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)-[1,1'-biphenyl]-3-carboxylic acid hydrochloride
InChi Key: PMXCGBVBIRYFPR-FTBISJDPSA-N
InChi Code: InChI=1S/C23H23ClN2O3.ClH/c24-20-8-2-6-18(13-20)22(27)15-25-10-11-26-21-9-3-5-17(14-21)16-4-1-7-19(12-16)23(28)29;/h1-9,12-14,22,25-27H,10-11,15H2,(H,28,29);1H/t22-;/m0./s1
SMILES Code: O=C(C1=CC(C2=CC=CC(NCCNC[C@@H](C3=CC=CC(Cl)=C3)O)=C2)=CC=C1)O.[H]Cl
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:
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The following data is based on the product molecular weight 447.36 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: Rosa GM, Ferrero S, Nitti VW, Wagg A, Saleem T, Chapple CR. Cardiovascular Safety of β(3)-adrenoceptor Agonists for the Treatment of Patients with Overactive Bladder Syndrome. Eur Urol. 2015 Sep 28. pii: S0302-2838(15)00864-7. doi: 10.1016/j.eururo.2015.09.007. [Epub ahead of print] Review. PubMed PMID: 26422675.
2: Thiagamoorthy G, Giarenis I, Cardozo L. Early investigational β3 adreno-receptor agonists for the management of the overactive bladder syndrome. Expert Opin Investig Drugs. 2015;24(10):1299-306. doi: 10.1517/13543784.2015.1076390. Epub 2015 Aug 14. PubMed PMID: 26292923.
3: Hertzberg R, Monreal Santiago G, Moberg C. Synthesis of the β3-adrenergic receptor agonist solabegron and analogous N-(2-ethylamino)-β-amino alcohols from O-acylated cyanohydrins - expanding the scope of minor enantiomer recycling. J Org Chem. 2015 Mar 6;80(5):2937-41. doi: 10.1021/acs.joc.5b00322. Epub 2015 Feb 24. PubMed PMID: 25689345.
4: Ellsworth P, Fantasia J. Solabegron: a potential future addition to the β-3 adrenoceptor agonist armamentarium for the management of overactive bladder. Expert Opin Investig Drugs. 2015 Mar;24(3):413-9. doi: 10.1517/13543784.2015.1001836. Epub 2015 Jan 5. Review. PubMed PMID: 25557359.
5: Andersson KE, Martin N, Nitti V. Selective β₃-adrenoceptor agonists for the treatment of overactive bladder. J Urol. 2013 Oct;190(4):1173-80. doi: 10.1016/j.juro.2013.02.104. Epub 2013 Feb 28. Review. PubMed PMID: 23458471.
6: Igawa Y, Michel MC. Pharmacological profile of β3-adrenoceptor agonists in clinical development for the treatment of overactive bladder syndrome. Naunyn Schmiedebergs Arch Pharmacol. 2013 Mar;386(3):177-83. doi: 10.1007/s00210-012-0824-1. Epub 2012 Dec 21. PubMed PMID: 23263450.
7: Chapple CR. β3-agonist therapy: a new advance in the management of overactive bladder? Eur Urol. 2012 Nov;62(5):841-2. doi: 10.1016/j.eururo.2012.08.006. Epub 2012 Aug 13. PubMed PMID: 22901985.
8: Ohlstein EH, von Keitz A, Michel MC. A multicenter, double-blind, randomized, placebo-controlled trial of the β3-adrenoceptor agonist solabegron for overactive bladder. Eur Urol. 2012 Nov;62(5):834-40. doi: 10.1016/j.eururo.2012.05.053. Epub 2012 Jun 5. PubMed PMID: 22695239.
9: Ellsworth P. Treatment of overactive bladder symptoms beyond antimuscarinics: current and future therapies. Postgrad Med. 2012 May;124(3):16-27. doi: 10.3810/pgm.2012.05.2544. Review. PubMed PMID: 22691895.
10: Tasler S, Baumgartner R, Behr-Roussel D, Oger-Roussel S, Gorny D, Giuliano F, Ney P. An aryloxypropanolamine hβ3-adrenoceptor agonist as bladder smooth muscle relaxant. Eur J Pharm Sci. 2012 Aug 15;46(5):381-7. doi: 10.1016/j.ejps.2012.03.001. Epub 2012 Mar 10. PubMed PMID: 22430195.
11: Sahi S, Tewatia P, Malik BK. Modeling and simulation studies of human β3 adrenergic receptor and its interactions with agonists. Curr Comput Aided Drug Des. 2012 Dec 1;8(4):283-95. PubMed PMID: 22242799.
12: Schemann M, Hafsi N, Michel K, Kober OI, Wollmann J, Li Q, Zeller F, Langer R, Lee K, Cellek S. The beta3-adrenoceptor agonist GW427353 (Solabegron) decreases excitability of human enteric neurons via release of somatostatin. Gastroenterology. 2010 Jan;138(1):266-74. doi: 10.1053/j.gastro.2009.09.046. Epub 2009 Sep 25. PubMed PMID: 19786030.
13: Tyagi P, Thomas CA, Yoshimura N, Chancellor MB. Investigations into the presence of functional Beta1, Beta2 and Beta3-adrenoceptors in urothelium and detrusor of human bladder. Int Braz J Urol. 2009 Jan-Feb;35(1):76-83. PubMed PMID: 19254402.
14: Grudell AB, Camilleri M, Jensen KL, Foxx-Orenstein AE, Burton DD, Ryks MD, Baxter KL, Cox DS, Dukes GE, Kelleher DL, Zinsmeister AR. Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and somatostatin levels in health. Am J Physiol Gastrointest Liver Physiol. 2008 May;294(5):G1114-9. doi: 10.1152/ajpgi.00051.2008. Epub 2008 Mar 27. PubMed PMID: 18372395.
15: Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. J Pharmacol Exp Ther. 2007 Oct;323(1):202-9. Epub 2007 Jul 12. PubMed PMID: 17626794.
