SR 59230A HCl

Alias: SR 59230A; SR-59230A; SR59230A; SR 59230A HCl; SR59230A HCl
Cat No.:V15215 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.
SR 59230A HCl Chemical Structure CAS No.: 1135278-41-9
Product category: Adenosine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
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Other Forms of SR 59230A HCl:

  • SR-59230A oxalate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
β adrenergic receptor
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].
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].
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

[1]. Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes. Mol Pharmacol. 1996 Jan;49(1):7-14.

[2]. Involvement of β3-adrenergic receptors in the control of food intake in rats.Braz J Med Biol Res. 2011 Nov;44(11):1141-7.

[3]. β3-adrenoreceptor blockade reduces tumor growth and increases neuronal differentiation in neuroblastoma via SK2/S1P2 modulation.Oncogene. 2020 Jan;39(2):368-384.

[4]. Role of alpha 1- and beta 3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse. Br J Pharmacol. 2009 Sep;158(1):259-66.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H28CLNO2
Molecular Weight
361.91
Exact Mass
361.18
Elemental Analysis
C, 69.69; H, 7.80; Cl, 9.80; N, 3.87; O, 8.84
CAS #
1135278-41-9
Related CAS #
SR59230A; 174689-39-5
Appearance
Solid powder
SMILES
CCC1=CC=CC=C1OC[C@H](CN[C@H]2CCCC3=CC=CC=C23)O.Cl
InChi Key
SHUCXUIOEAAJJL-MKSBGGEFSA-N
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
Chemical Name
(2S)-1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]propan-2-ol;hydrochloride
Synonyms
SR 59230A; SR-59230A; SR59230A; SR 59230A HCl; SR59230A HCl
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 Data
Solubility (In Vitro)
DMSO: ~250 mg/mL (~690.8 mM)
H2O: ~2.5 mg/mL (~6.9 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • 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.
  • 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.
  • 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.
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