A selective β3-AR agonist (EC50 = 3.5 nM in rat colon); minimally active against β1-ARs in rat uterus (EC50 = 499 nM) and inactive against β2-ARs in guinea pig trachea and atrium (EC50s = >10

SR 58611A (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
121524-09-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

SR 58611A is a selective β3-adrenergic receptor agonist (β3-AR; EC50 = 3.5 nM in rat colon).{38085} Its activity cannot be blocked by the β1- and β2-AR antagonists CGP 20712A and ICI 118551 (Item No. 15591), respectively. SR 58611A is minimally active against β1-ARs in rat uterus (EC50 = 499 nM) and inactive against β2-ARs in guinea pig trachea and atrium (EC50s = >10,000 and >30,000 nM, respectively). SR 58611A activates brown fat metabolism through activation of adenylyl cyclase activity and glycerol release in brown adipocytes (EC50s = 20 and 11 nM, respectively).{38086} It also reduces hypothermia produced by apomorphine (Item No. 16094) and reserpine (Item No. 16474) and potentiates toxicity produced by yohimbine (Item No. 19869) in mice.{38087} SR 58611A (0.6 to 2 mg/kg/day) also reduces the number of escape failures in a learned helplessness model of antidepressant-like activity in rats without changes in locomotor activity typically seen with β2-AR agonists.  

 

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SKU: 11954 - 1 mg Category:

Description

A selective β3-AR agonist (EC50 = 3.5 nM in rat colon); minimally active against β1-ARs in rat uterus (EC50 = 499 nM) and inactive against β2-ARs in guinea pig trachea and atrium (EC50s = >10,000 and >30,000 nM, respectively); activates brown fat metabolism through activation of adenylyl cyclase activity and glycerol release in brown adipocytes (EC50s = 20 and 11 nM, respectively); reduces hypothermia produced by apomorphine and reserpine; potentiates toxicity produced by yohimbine; reduces number of escape failures in a learned helplessness model of antidepressant-like activity in rats ,

Formal name: [[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydro-2-naphthalenyl]oxy]-acetic acid, ethyl ester, monohydrochloride

Synonyms:  Amibegron

Molecular weight: 440.4

CAS: 121524-09-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area

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