1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. SR59230A

SR59230A 

Cat. No.: HY-100672 Purity: >98.0%
Handling Instructions

SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

For research use only. We do not sell to patients.

SR59230A Chemical Structure

SR59230A Chemical Structure

CAS No. : 174689-39-5

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Based on 1 publication(s) in Google Scholar

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Description

SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].

IC50 & Target

IC50: 40 nM (β3 receptor), 408 nM ((β1 receptor), 648 nM (β2 receptor)[2]

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[3].

Cell Viability Assay[3]

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).
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[4].

Animal Model: Male C-57BL6J wild-type mice (22-35 g)[4]
Dosage: 0.5 or 5 mg/kg
Administration: Injected s.c.; administered 30 min prior to the injection s.c. of MDMA (20 mg/kg).
Result: Modulated the actions of MDMA on temperature involve α1-adrenoceptor antagonism.
Molecular Weight

415.48

Formula

C₂₃H₂₉NO₆

CAS No.

174689-39-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (75.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

SR59230AAdrenergic ReceptorBeta Receptorhyperthermiahypothermiaα1adrenoceptorβ3adrenergicreceptorInhibitorinhibitorinhibit

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SR59230A
Cat. No.:
HY-100672
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