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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
SR 59230A HCl is a potent, brain penetrant and selective β3 adrenoceptor antagonist with IC50 values of 40, 408 and 648 nM for β3, β1 and β2 receptors respectively. In animal studies, SR-59230A was 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.
Targets |
β adrenergic receptor
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ln Vitro |
SR59230A hydrochloride (100 nM–50 μM; 24 hours) decreases the cell viability of Neuro-2A, BE (2) C, and SK-N-BE (2) NB cell lines in a quantitatively dependent manner[3].
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ln Vivo |
MDMA (20 mg/kg) caused hyperthermia that developed gradually and peaked at 130 minutes after injection, with a temperature increase of 1.8°C. MDMA's slowly developing hyperthermia was significantly but slightly attenuated when SR59230A hydrochloride (0.5 mg/kg) was administered. A notable early hypothermic response to MDMA was shown by SR59230A hydrochloride (5 mg/kg) [4].
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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 |
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Molecular Formula |
C21H28CLNO2
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Molecular Weight |
361.91
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Exact Mass |
361.18
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Elemental Analysis |
C, 69.69; H, 7.80; Cl, 9.80; N, 3.87; O, 8.84
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CAS # |
1135278-41-9
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Related CAS # |
SR59230A; 174689-39-5
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Appearance |
Solid powder
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SMILES |
CCC1=CC=CC=C1OC[C@H](CN[C@H]2CCCC3=CC=CC=C23)O.Cl
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InChi Key |
SHUCXUIOEAAJJL-MKSBGGEFSA-N
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InChi Code |
InChI=1S/C21H27NO2.ClH/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;/h3-6,8-9,11,13,18,20,22-23H,2,7,10,12,14-15H2,1H3;1H/t18-,20-;/m0./s1
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Chemical Name |
(2S)-1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]propan-2-ol;hydrochloride
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Synonyms |
SR 59230A; SR-59230A; SR59230A; SR 59230A HCl; SR59230A HCl
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
DMSO: ~250 mg/mL (~690.8 mM)
H2O: ~2.5 mg/mL (~6.9 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7631 mL | 13.8156 mL | 27.6312 mL | |
5 mM | 0.5526 mL | 2.7631 mL | 5.5262 mL | |
10 mM | 0.2763 mL | 1.3816 mL | 2.7631 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> |
Binding curves showing the displacement by SR59230A of [3H]-prazosin binding to α1A-adrenoceptor ligand binding sites of rat submandibular gland and α1B-adrenoceptor ligand binding sites of rat spleen. Br J Pharmacol . 2009 Sep;158(1):259-66. td> |