SR-59230A oxalate

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.

Product information

CAS Number: 174689-39-5

Molecular Weight: 415.48

Formula: C23H29NO6

Synonym:

SR-59230A

SR-59230A oxalate

SR 59230A

SR59230A

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

Smiles: CCC1=CC=CC=C1OC[C@@H](O)CN[C@H]1CCCC2=CC=CC=C21.OC(=O)C(O)=O

InChiKey: XTBQNQMNFXNGLR-MKSBGGEFSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.
2. 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.