[CAS NO. 1402601-82-4] TUG-770
PRODUCTS SPECIFICATIONS [1402601-82-4]
DESCRIPTION [1402601-82-4]
Overview
| MDL | MFCD26142679 |
|---|---|
| Molecular Weight | 307.32 |
| Molecular Formula | C19H14FNO2 |
| SMILES | FC1=C(CCC(O)=O)C=CC(C#CC2=C(CC#N)C=CC=C2)=C1 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
EC50: 6 nM (Human GPR40/FFA1) [1]
In Vitro
TUG-770 (Compound 22) displays excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 shows excellent stability toward human liver microsomes (HLM), and good permeability in the Caco-2 cell assay
[1]
.
TUG-770 exhibits lower potency on the rodent orthologs (mFFA1, pEC
50
= 6.83; rFFA1, pEC
50
= 6.49)
[1]
.
In the rat INS-1E cell line, TUG-770 significantly increases insulin secretion (10.75% of total content with 10 μM 22 vs 8.74 with vehicle) at high glucose concentration (12.4 mM) and, no effect (4.14% of total content with 10 μM 22 vs 4.02 with vehicle) at low glucose concentration (2.8 mM)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TUG-770 (Compound 22; 20 mg/kg; oral administration; daily; for 28 days) treatment significantly improves glucose tolerance, and has no effect on food intake, body weight, body composition or plasma leptin concentration. TUG-770 also significantly improves the insulin sensitivity index (plasma glucose x plasma insulin) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C56B1/6 male mice (5-6 weeks of age) fed on the 60% fat diet D12492 [1] |
| Dosage: | 20 mg/kg |
| Administration: | Oral administration; daily; for 28 days |
| Result: | Significantly improved glucose tolerance. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 325.39 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2539 mL | 16.2697 mL | 32.5394 mL |
| 5 mM | 0.6508 mL | 3.2539 mL | 6.5079 mL |
| 10 mM | 0.3254 mL | 1.6270 mL | 3.2539 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution