[CAS NO. 1065609-00-8] AR453588
PRODUCTS SPECIFICATIONS [1065609-00-8]
DESCRIPTION [1065609-00-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 519.64 |
| Molecular Formula | C25H25N7O2S2 |
| SMILES | CC(N1CCC(C2=NSC(NC3=NC=C(SC4=NC=CC=C4)C=C3OC5=CC=CN=C5C)=N2)CC1)=O |
Summary
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC 50 of 42 nM. AR453588 shows anti-hyperglycemic activity [1] .
In Vivo
AR453588 (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice
[1]
.
AR453588 (3-30 mg/kg; p.o.; once-daily for 14 days) shows anti-hyperglycemic activity in a dose-ranging 14 day ob/ob mouse
[1]
.
AR453588 (10 mg/kg; p.o.) treatment shows that the T
max
, AUC
inf
, Vss, C
max
and
F
are 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively
[1]
.
AR453588 (1 mg/kg; i.v.) treatment shows that the CL, AUC
inf
, Vss, and t
1/2
are 21.6 mL/min/kg, 0.77 h μg /mL, 0.746 L/kg and 1.28 hours, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male diabetic ob/ob mice [1] |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | Orally once-daily for 14 days |
| Result: | Lowered the fasted blood glucose from the control animals on day 14 as well as the AUC of the OGTT (oral glucose tolerance tests). |
| Animal Model: | Male CD-1 mice [1] |
| Dosage: | 10 mg/kg |
| Administration: | p.o. (Pharmacokinetic Analysis) |
| Result: | The T max , AUC inf , Vss, C max and F were 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively. |
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 ( 192.44 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9244 mL | 9.6220 mL | 19.2441 mL |
| 5 mM | 0.3849 mL | 1.9244 mL | 3.8488 mL |
| 10 mM | 0.1924 mL | 0.9622 mL | 1.9244 mL |