| Identification | Back Directory | [Name]
2-((2-(3-cyclohexyl-3-((1r,4r)-4-propoxycyclohexyl)ureido)thiazol-5-yl)thio)aceticacid | [CAS]
859525-02-3 | [Synonyms]
GK1-399
TTP-399
EOS-60382
cadisegliatin
2-((2-(3-cyclohexyl-3-((1r,4r)-4-propoxycyclohexyl)ureido)thiazol-5-yl)thio)aceticacid
{2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid | [Molecular Formula]
C21H33N3O4S2 | [MOL File]
859525-02-3.mol | [Molecular Weight]
455.63 |
| Chemical Properties | Back Directory | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 125 mg/mL (274.35 mM; Need ultrasonic) | [form ]
Solid | [pka]
3.26±0.10(Predicted) | [color ]
Off-white to pale purple |
| Hazard Information | Back Directory | [Uses]
Cadisegliatin (TTP-399) is a potential, orally active liver-selective glucokinase (GK) activator. Cadisegliatin has antihyperglycaemic activity. Cadisegliatin can be used for the research of type 2 diabetes[1][2]. | [in vivo]
TTP399 (200 mg/kg, per os, p.o.) has no effect on plasma glucose and insulin in fasted rats[2].
TTP399 (75 or 150 mg/kg, per day, for 4 weeks) improves glucose homeostasis in ob/ob mouse model[2].
TTP399 (50 mg/kg, per day, for 13 weeks) is effective in reducing plasma glucose during an oral glucose tolerance test (OGTT) in minipigs model[2]. | Animal Model: | Nondiabetic fasted rats[2] | | Dosage: | 200 mg/kg | | Administration: | 200 mg/kg, per os (p.o.) | | Result: | Did not change the insulin and glucose concentrations in plasma. |
| Animal Model: | ob/ob mouse model[2] | | Dosage: | 75 or 150 mg/kg | | Administration: | 75 or 150 mg/kg, per day, for 4 weeks | | Result: | Reduced the expression of HbA1c, blood glucose concentrations, lactate concentrations and liver glycogen depots.
Improved the lipid profile, reduced plasma, liver TG concentrations and the weight gain at the highest dose.
|
| Animal Model: | Gottingen minipigs[2] | | Dosage: | 50 mg/kg | | Administration: | 50 mg/kg, per day, for 13 weeks | | Result: | Eliminated the blood glucose excursion in Minipigs. |
| [References]
[1] International Nonproprietary Names for Pharmaceutical Substances (INN)
[2] Adrian Vella, et al. Targeting hepatic glucokinase to treat diabetes with TTP399, a hepatoselective glucokinase activator. Sci Transl Med. 2019 Jan 16;11(475):eaau3441. DOI:10.1126/scitranslmed.aau3441 |
|
|