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

SR59230A hydrochloride 

Cat. No.: HY-103200
Handling Instructions

SR59230A hydrochloride 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 hydrochloride Chemical Structure

SR59230A hydrochloride Chemical Structure

CAS No. : 1135278-41-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
25 mg USD 330 In-stock
Estimated Time of Arrival: December 31
50 mg USD 550 In-stock
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100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

SR59230A hydrochloride 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

361.91

Formula

C₂₁H₂₈ClNO₂

CAS No.

1135278-41-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (690.78 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*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 (5.75 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.75 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.75 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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Product Name:
SR59230A hydrochloride
Cat. No.:
HY-103200
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