1082058-99-8

1082058-99-8 structure

Name: TUG-424
Chemical Name: 3-[4-[2-(2-methylphenyl)ethynyl]phenyl]propanoic acid
CAS Number: 1082058-99-8
Molecular Formula: C₁₈H₁₆O₂
Molecular Weight: 264.318
Catalog: Signaling Pathways GPCR/G Protein GPR40
Create Date: 2016-05-15 21:14:09
Modify Date: 2024-01-07 19:43:45
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity[1].

Name	3-[4-[2-(2-methylphenyl)ethynyl]phenyl]propanoic acid
Synonyms	3-{4-[(2-Methylphenyl)ethynyl]phenyl}propanoic acid 3-(4-(o-Tolylethynyl)phenyl)propanoic acid TUG-424 Benzenepropanoic acid, 4-[2-(2-methylphenyl)ethynyl]-

Description	TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> GPR40 Research Areas >> Metabolic Disease
Target	EC50: 32 nM (FFA1/GPR40)[1]
In Vitro	Increasing concentrations (100 nM to 10 µM) of TUG-424 enhances glucose-stimulated insulin secretion significantly already at 100 nM and with a maximal effect at 3 µM. The approximately 2-fold stimulation of secretion by TUG-424 in the presence of 12 mM glucose is comparable to that induced by palmitate in the presence of the same glucose concentration. Basal insulin secretion at 2.8 mM glucose is slightly but significantly reduces by TUG-424[1].
References	[1]. Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II DiabetesJ. Med. Chem., 2008, 51 (22), pp 7061-7064 [2]. Christiansen E, et al. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem. 2008 Nov 27;51(22):7061-4.

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H319-H410
Precautionary Statements	P273-P305 + P351 + P338-P501
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
RIDADR	UN 3077 9 / PGIII