Drug intelligence / Profile preview

CL-316,243

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

CL-316,243 is a **highly potent and selective agonist of the β3-adrenergic receptor** (β3-AR), characterized by an EC50 of approximately 3 nM and >10,000-fold selectivity over β1 and β2 adrenergic receptors[14][16][5][2]. As a **small molecule** used exclusively in research, it is not approved for clinical use. The drug increases brown adipose tissue thermogenesis and metabolic rate, reduces blood insulin and glucose levels, and induces energy expenditure and weight loss in animal models. It also induces muscle hypertrophy and increases skeletal muscle strength in rodents, effects mediated via mTOR and NOS signaling[1][6]. Its anti-obesity effects are mediated through selective β3-AR activation, leading to remodeling of adipose tissue and upregulation of UCP1 in brown and beige adipocytes[4][6][13][9]. CL-316,243 has also been used in studies examining combined anti-obesity therapies and glucose homeostasis.

Other names
CL 316243 disodium saltCL316243 disodium saltCL-316243 disodium saltdisodium;5-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,3-dicarboxylatedisodium (R,R)-5-(2-((2-(3-chlorophenyl)-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxole-2,3-dicarboxylateCL 316243 (free acid)Cl-316243 Free diacidCl316243 Free diacidCl 316243 Free diacid
02

Targets

ADRB3 (β3)

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