TUG-770
- Product Name
- TUG-770
- CAS No.
- 1402601-82-4
- Chemical Name
- TUG-770
- Synonyms
- TUG-770;CS-1047;TUG770; TUG 770;4-[2-[2-(Cyanomethyl)phenyl]ethynyl]-2-fluorobenzenepropanoic acid;3-(4-((2-(Cyanomethyl)phenyl)ethynyl)-2-fluorophenyl)propanoic acid;Benzenepropanoic acid, 4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluoro-;4-[2-[2-(Cyanomethyl)phenyl]ethynyl]-2-fluorobenzenepropanoic acid TUG-770
- CBNumber
- CB42659732
- Molecular Formula
- C19H14FNO2
- Formula Weight
- 307.32
- MOL File
- 1402601-82-4.mol
TUG-770 Property
- Boiling point:
- 523.5±50.0 °C(Predicted)
- Density
- 1.28±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥11.85 mg/mL in DMSO; ≥9.5 mg/mL in EtOH with gentle warming and ultrasonic
- form
- solid
- pka
- 4.61±0.10(Predicted)
N-Bromosuccinimide Price
- Product number
- 22131
- Product name
- TUG-770
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 22131
- Product name
- TUG-770
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 22131
- Product name
- TUG-770
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 22131
- Product name
- TUG-770
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $618
- Updated
- 2024/03/01
- Product number
- 2850DS
- Product name
- 3-(4-((2-(Cyanomethyl)phenyl)ethynyl)-2-fluorophenyl)propanoicacid
- Packaging
- 25mg
- Price
- $785
- Updated
- 2021/12/16
TUG-770 Chemical Properties,Usage,Production
Biological Activity
tug-770 is a potent free fatty acid receptor 1 (ffa1/gpr40) agonist. free fatty acid receptor 1 (ffa1 or gpr40) enhances the glucose-stimulated insulin secretion from pancreatic β-cells and attracts high interest as a new target for the treatment of type 2 diabetes.
in vitro
tug-770 showed a pronounced increase in potency on ffa1 with ec50 = 6 nm and 150-fold selectivity over ffa4. tug-770 showed a high selectivity over ffa2, ffa3, pparγ, and 54 diverse transporters, receptors, and enzymes. in the rat ins-1e cell line, tug-770 caused significantly increased insulin secretion at high glucose concentration and, as expected, no effect at low glucose concentration [1].
in vivo
pharmacokinetic studies of tug-770 in mice showed a fast oral absorption, higher plasma concentration, a longer half-life, lower clearance, and increased bioavailability. no adverse effects were seen in mice after four weeks of daily oral treatment of 20 mg/kg and acute treatment in doses up to 250 mg/kg. in vivo examination of tug-770 in an acute intraperitoneal glucose tolerance test in normal mice showed a good dose-dependent response with maximal reduction in glucose level reached at 50 mg/kg. the followed chronic oral glucose tolerance test study in dio mice showed that tug-770 was more effective than its analog. further evaluation of tug-770 in rats confirmed a significant glucose lowering effect for the high doses [1].
IC 50
6 nm
References
[1] christiansen e,hansen sv,urban c,hudson bd,wargent et,grundmann m,jenkins l,zaibi m,stocker cj,ullrich s,kostenis e,kassack mu,milligan g,cawthorne ma,ulven t. discovery of tug-770: a highly potent free fatty acid receptor 1 (ffa1/gpr40) agonist for treatment of type 2 diabetes. acs med chem lett.2013 may 9;4(5):441-445.
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