SR-59230A oxalate


Catalog No. size PriceQuantity
M7124-2 2mg solid $84
M7124-10 10mg solid $328

Description

Cas:174689-39-5 (oxalate)

Product Information

SR-59230A is a potent and selective β3 adrenoceptor antagonist (IC50 values are 40, 408 and 648 nM for β3, β1 and β2 receptors respectively). SR-59230A was subsequently shown to also act at α1 adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies. SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism

 

Chemical Formula: C23H29NO6

 

Molecular Weight: 415.486

 

Elemental Analysis: C, 66.49; H, 7.04; N, 3.37; O, 23.10

 

Synonym:

 

SR-59230A oxalate

SR-59230A

SR 59230A

SR59230A

 

Chemical Name: 1-(2-Ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol oxalate

 

InChi Key: 

XTBQNQMNFXNGLR-MKSBGGEFSA-N

 

InChi Code: InChI=1S/C21H27NO2.C2H2O4/c1-2-16-8-4-6-13-21(16)24-15-18(23)14-22-20-12-7-10-17-9-3-5-11-19(17)20;3-1(4)2(5)6/h3-6,8-9,11,13,18,20,22-23H,2,7,10,12,14-15H2,1H3;(H,3,4)(H,5,6)/t18-,20-;/m0./s1

 

Smiles Code:

O[C@@H](CN[C@H]1CCCC2=C1C=CC=C2)COC3=CC=CC=C3CC.O=C(O)C(O)=O.

 

 

Technical Data:

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: 2934.99.9001

 

In Vitro

SR59230A (100 nM-50 μM; 24 hours) is able to reduce cell viability in a dose-dependent manner in Neuro-2A, BE(2)C and SK-N-BE(2) NB cell lines.

 

In Vivo

MDMA (20 mg/kg) produces a slowly developing hyperthermia, reaching a maximum increase of 1.8°C at 130 min post injection. SR59230A (0.5 mg/kg) produces a small but significant attenuation of the slowly developing hyperthermia to MDMA. SR59230A (5 mg/kg) reveals a significant and marked early hypothermic reaction to MDMA.

 

 

References

 

  1. Jing JN, Li FL, Wang X, Wan X, Zhao QQ, Cui XL. [SR 59230A on the expression of MicroRNAs in myocardium of heart failure rats]. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2017 May 8;33(5):456-460. Chinese. doi: 10.12047/j.cjap.5561.2017.109. PMID: 29926593.

 

  1. Kulzer M, Seyler C, Welke F, Scherer D, Xynogalos P, Scholz EP, Thomas D, Becker R, Karle CA, Katus HA, Zitron E. Inhibition of cardiac Kir2.1-2.3 channels by beta3 adrenoreceptor antagonist SR 59230A. Biochem Biophys Res Commun. 2012 Jul 27;424(2):315-20. doi: 10.1016/j.bbrc.2012.06.114. Epub 2012 Jun 27. PMID: 22749993.

 

  1. Pettersson US, Henriksnäs J, Jansson L. Reversal of high pancreatic islet and white adipose tissue blood flow in type 2 diabetic GK rats by administration of the beta3-adrenoceptor inhibitor SR-59230A. Am J Physiol Endocrinol Metab. 2009 Aug;297(2):E490-4. doi: 10.1152/ajpendo.00140.2009. Epub 2009 Jun 2. PMID: 19491297.

 

  1. Leblais V, Pourageaud F, Ivorra MD, Guibert C, Marthan R, Muller B. Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A, on the contraction of rat intrapulmonary artery. J Pharmacol Exp Ther. 2004 Apr;309(1):137-45. doi: 10.1124/jpet.103.061192. Epub 2004 Jan 12. PMID: 14718590.

 

  1. MacDonald A, Watt K. Characterisation of the atypical beta-adrenoceptor in rabbit isolated jejunum using BRL 37344, cyanopindolol and SR 59230A. J Auton Pharmacol. 1999 Apr;19(2):91-5. doi: 10.1046/j.1365-2680.1999.00121.x. PMID: 10466941.

 

Products are for research use only. Not for human use.

 

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