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Solabegron

Cat. No. M11289
Solabegron Structure
Synonym:

GW 427353

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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Solabegron (GW 427353) is a selective agonist of β3 adrenergic receptor (β3-AR). The EC50 value of Solabegron was 22 nM in Chinese hamster ovarian cells. It can be used to study overactive bladder and irritable bowel syndrome.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 410.89
Formula C23H23ClN2O3
CAS Number 252920-94-8
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage 4°C , protect from light , dry , sealed
References

[1] Ikko Nureki, et al. Biochem Biophys Res Commun. Cryo-EM structures of the β 3 adrenergic receptor bound to solabegron and isoproterenol

[2] Pamela Ellsworth, et al. Expert Opin Investig Drugs. Solabegron: a potential future addition to the β-3 adrenoceptor agonist armamentarium for the management of overactive bladder

[3] Eliot H Ohlstein, et al. Eur Urol. A multicenter, double-blind, randomized, placebo-controlled trial of the β3-adrenoceptor agonist solabegron for overactive bladder

[4] April B M Grudell, et al. Am J Physiol Gastrointest Liver Physiol. Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and somatostatin levels in health

[5] Alexandra Hicks, et al. J Pharmacol Exp Ther. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog

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