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SR59230A hydrochloride

Cat. No. M13899
SR59230A hydrochloride Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

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 361.91
Formula
CAS Number 1135278-41-9
Purity >99%
Solubility DMSO 150 mg/mL
Water 2.5 mg/mL
Storage 2-8°C, dry, sealed
References

[1] Serge A Y Afeli, et al. Functional BK channels facilitate the β3-adrenoceptor agonist-mediated relaxation of nerve-evoked contractions in rat urinary bladder smooth muscle isolated strips

[2] Subhashree Parida, et al. Molecular and functional characteristics of β3-adrenoceptors in late pregnant mouse uterus: a comparison with β2-adrenoceptors

[3] Sotiria Bexis, et al. Role of alpha 1- and beta 3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse

[4] Khaled Al Zubair, et al. Relaxations to beta-adrenoceptor subtype selective agonists in wild-type and NOS-3-KO mouse mesenteric arteries

[5] C Tonello, et al. SR59230A blocks beta3-adrenoceptor-linked modulation of upcoupling protein-1 and leptin in rat brown adipocytes

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