TUG-469

Names

[ CAS No. ]:
1236109-67-3

[ Name ]:
TUG-469

[Synonym ]:
3-(4-{[(2'-Methyl-3-biphenylyl)methyl]amino}phenyl)propanoic acid
Benzenepropanoic acid, 4-[[(2'-methyl[1,1'-biphenyl]-3-yl)methyl]amino]-

Biological Activity

[Description]:

TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPR40
Research Areas >> Metabolic Disease

[In Vitro]

TUG-469 (0-10 μM) shows efficacy to hFFA1 with an pEC50 value of 7.73[1]. TUG-469 (10 μM) increases the insulin secretion under 10 mM glucose stimulation[1]. TUG-469 (0-100 μM) is >200-fold selective for FFA1 over FFA4 with EC50 values of 19 nM and 4.4 μM for FFA1 and FFA4, respectively[2]. TUG-469 (5 μM; 30 min) leds a significantly increases insulin secretion of INS-1 cells with the presence of high glucose concentration (16.7 mM)[2].

[In Vivo]

TUG-469 (5 mg/kg; i.p.; 60 and 90 min after glucose administration) affects blood glucose level[2]. Animal Model: Male NZO mice with glucose administration[2] Dosage: 5 mg/kg Administration: Intraperitoneal injection; 5 mg/kg; 60 and 90 min after glucose administration Result: Reduced the blood glucose level.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
532.7±38.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H23NO2

[ Molecular Weight ]:
345.434

[ Flash Point ]:
275.9±26.8 °C

[ Exact Mass ]:
345.172882

[ LogP ]:
4.97

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.634

[ Storage condition ]:
-20°C


Related Compounds