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

MedKoo CAT#: 522560

CAS#: 244081-42-3

Description: Rafabegron, also known as AJ-9677; TAK 677; AD 9677, is a potent and selective beta3-adrenoceptor agonist. Rafabegron is a potential treatment of non-insulin dependent diabetes and obesity. Rafabegron has a high relaxant potency on the rat, monkey and human detrusor smooth muscle, and it may have the potential to treat overactive bladder.

Price and Availability




Rafabegron is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 522560
Name: Rafabegron
CAS#: 244081-42-3
Chemical Formula: C21H23ClN2O4
Exact Mass: 402.1346
Molecular Weight: 402.875
Elemental Analysis: C, 62.61; H, 5.75; Cl, 8.80; N, 6.95; O, 15.88

Synonym: TAK 677; TAK-677; TAK677; AD-9677; AD9677; AD 9677; AJ-9677; AJ-9677; AJ-9677; Rafabegron.

IUPAC/Chemical Name: 2-((3-((R)-2-(((R)-2-(3-chlorophenyl)-2-hydroxyethyl)amino)propyl)-1H-indol-7-yl)oxy)acetic acid


InChi Code: InChI=1S/C21H23ClN2O4/c1-13(23-11-18(25)14-4-2-5-16(22)9-14)8-15-10-24-21-17(15)6-3-7-19(21)28-12-20(26)27/h2-7,9-10,13,18,23-25H,8,11-12H2,1H3,(H,26,27)/t13-,18+/m1/s1


Technical Data

Solid powder

>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).

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).

Harmonized System Code:


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2: Kullmann FA, Downs TR, Artim DE, Limberg BJ, Shah M, Contract D, de Groat WC, Rosenbaum JS. Urothelial beta-3 adrenergic receptors in the rat bladder. Neurourol Urodyn. 2011 Jan;30(1):144-50. doi: 10.1002/nau.20965. PubMed PMID: 21046653; PubMed Central PMCID: PMC3395322.

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4: Kullmann FA, Limberg BJ, Artim DE, Shah M, Downs TR, Contract D, Wos J, Rosenbaum JS, de Groat WC. Effects of beta3-adrenergic receptor activation on rat urinary bladder hyperactivity induced by ovariectomy. J Pharmacol Exp Ther. 2009 Sep;330(3):704-17. doi: 10.1124/jpet.109.155010. Epub 2009 Jun 10. PubMed PMID: 19515967; PubMed Central PMCID: PMC2729793.

5: Otsuka A, Shinbo H, Hasebe K, Matsumoto R, Ozono S. Effects of a novel beta(3)-adrenoceptor agonist, AJ-9677, on relaxation of the detrusor muscle: an in vitro study. Int J Urol. 2008 Dec;15(12):1072-6. doi: 10.1111/j.1442-2042.2008.02165.x. PubMed PMID: 19120515.

6: Omachi A, Matsushita Y, Kimura K, Saito M. Role of uncoupling protein 1 in the anti-obesity effect of beta3-adrenergic agonist in the dog. Res Vet Sci. 2008 Oct;85(2):214-9. doi: 10.1016/j.rvsc.2007.11.003. Epub 2008 Apr 11. PubMed PMID: 18406437.

7: Omachi A, Ishioka K, Uozumi A, Kamikawa A, Toda C, Kimura K, Saito M. Beta3-adrenoceptor agonist AJ-9677 reduces body fat in obese beagles. Res Vet Sci. 2007 Aug;83(1):5-11. Epub 2006 Nov 30. PubMed PMID: 17140615.

8: Redman LM, de Jonge L, Fang X, Gamlin B, Recker D, Greenway FL, Smith SR, Ravussin E. Lack of an effect of a novel beta3-adrenoceptor agonist, TAK-677, on energy metabolism in obese individuals: a double-blind, placebo-controlled randomized study. J Clin Endocrinol Metab. 2007 Feb;92(2):527-31. Epub 2006 Nov 21. PubMed PMID: 17118998.

9: Sugimoto T, Ogawa W, Kasuga M, Yokoyama Y. Chronic effects of AJ-9677 on energy expenditure and energy source utilization in rats. Eur J Pharmacol. 2005 Sep 5;519(1-2):135-45. PubMed PMID: 16111677.

10: Harada H, Hirokawa Y, Suzuki K, Hiyama Y, Oue M, Kawashima H, Kato H, Yoshida N, Furutani Y, Kato S. Discovery of a novel and potent human and rat beta3-adrenergic receptor agonist, [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]ac etic acid. Chem Pharm Bull (Tokyo). 2005 Feb;53(2):184-98. PubMed PMID: 15684518.

11: Francke S. TAK-677 (Dainippon/Takeda). Curr Opin Investig Drugs. 2002 Nov;3(11):1624-8. Review. PubMed PMID: 12476963.

12: Sakura H. [Beta 3 adrenergic receptor agonist]. Nihon Rinsho. 2002 Oct;60 Suppl 10:712-8. Review. Japanese. PubMed PMID: 12430307.

13: Noda M. [Tailor-made medicine for diabetes]. Nihon Rinsho. 2002 Jan;60(1):149-53. Review. Japanese. PubMed PMID: 11808326.

14: Sakura H, Togashi M, Iwamoto Y. [beta 3-adrenergic receptor agonists as anti-obese and anti-diabetic drugs]. Nihon Rinsho. 2002 Jan;60(1):123-9. Review. Japanese. PubMed PMID: 11808322.

15: Kato H, Ohue M, Kato K, Nomura A, Toyosawa K, Furutani Y, Kimura S, Kadowaki T. Mechanism of amelioration of insulin resistance by beta3-adrenoceptor agonist AJ-9677 in the KK-Ay/Ta diabetic obese mouse model. Diabetes. 2001 Jan;50(1):113-22. PubMed PMID: 11147775.