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SR-58611A

Cat. No. M8433
SR-58611A Structure
Synonym:

SR 58611A

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Biological Activity

SR58611A is a potent, specific b3 adrenergic receptor agonist. The EC50 for reduction of β3-mediated spontaneous motility in rat distal colon sections is 3.5 nM. Minimal anti-depressant efficacious doses for SR58611A are 0.1-0.3 mpk in rodent models.

Chemical Information
Molecular Weight 440.36
Formula C22H26ClNO4 · HCl
CAS Number 121524-09-2
Solubility (25°C) DMSO: 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] No authors listed. Drugs R D. SR 58611A: SR 58611

[2] C A Williams, et al. Sustained improvement in glucose homeostasis in lean and obese mice following chronic administration of the beta 3 agonist SR 58611A

[3] E Nisoli, et al. SR 58611A: a novel thermogenic beta-adrenoceptor agonist

[4] F De Ponti, et al. Inhibitory effects of SR 58611A on canine colonic motility: evidence for a role of beta 3-adrenoceptors

[5] J Simiand, et al. Antidepressant profile in rodents of SR 58611A, a new selective agonist for atypical beta-adrenoceptors

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