Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: =99.1%
SR-59230A oxalate (SR59230A) is a novel, potent, blood-brain barrier penetrating, and selective β3 adrenoceptor antagonist (IC50 values are 40, 408 and 648 nM for β3, β1 and β2 receptors respectively). SR-59230A was later demonstrated to act at high doses at α1 adrenoceptors as well. In studies on animals, it has been demonstrated to prevent the hyperthermia caused by MDMA. At elevated concentrations, SR 59230A not only prevents hyperthermia caused by MDMA but also enhances heat loss by acting as an antagonist of α1-AR.
ln Vitro |
|
|
---|---|---|
ln Vivo |
|
|
Cell Assay |
Cell Line: Three different neuroblastoma (NB) cell lines, one murine (Neuro-2A) and two human (SK-N-BE(2), BE(2)C)
Concentration: 100 nM, 1 μM, 5 μM, 10 μM, and 50 μM
Incubation Time: 24 hours
Result: Reduced cell viability in a dose-dependent manner, with significant effect at a concentration limit over 1 µM for Neuro-2A cells and 5 µM for SK-N-BE(2) and BE(2)C).
|
|
Animal Protocol |
Male C-57BL6J wild-type mice (22-35 g)
0.5 or 5 mg/kg Injected s.c.; administered 30 min prior to the injection s.c. of MDMA (20 mg/kg). |
|
References |
|
Molecular Formula |
C23H29NO6
|
---|---|
Molecular Weight |
415.4795
|
Elemental Analysis |
C, 66.49; H, 7.04; N, 3.37; O, 23.10
|
CAS # |
174689-39-5
|
Appearance |
Solid powder
|
SMILES |
O[C@@H](CN[C@H]1CCCC2=C1C=CC=C2)COC3=CC=CC=C3CC.O=C(O)C(O)=O
|
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
|
Chemical Name |
1-(2-Ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol oxalate
|
Synonyms |
SR 59230A; SR-59230A; SR59230A; SR-59230A oxalate
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~31.25 mg/mL (~75.21 mM)
|
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4069 mL | 12.0343 mL | 24.0685 mL | |
5 mM | 0.4814 mL | 2.4069 mL | 4.8137 mL | |
10 mM | 0.2407 mL | 1.2034 mL | 2.4069 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Neuroblastoma tumor growth reduction exerted by SR59230A via SK2/S1P2 signaling axis is accompanied with an increased neuronal differentiation of NB cells. Oncogene . 2020 Jan;39(2):368-384. td> |
Core body temperature recordings in conscious wild-type mice administered with vehicle, SR59230A (0.5 or 5 mg·kg−1) or prazosin (0.1 mg·kg−1) plus SR59230A (5 mg·kg−1), 30 min prior to giving MDMA (20 mg·kg−1), at room temperature. Br J Pharmacol . 2009 Sep;158(1):259-66. td> |
Effects of SR59230A (10 µmol·L−1) on contractions to phenylephrine in rat spleen (A) and contractions to noradrenaline in rat aorta (B). Br J Pharmacol . 2009 Sep;158(1):259-66. td> |