产品
编 号：F752412
分子式：C21H22N6O3S
分子量：438.5
分子式：C21H22N6O3S
分子量：438.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2414484-25-4
产品详情
生物活性：
IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes.
体内研究：
IHMT-MST1-58 (compound 19) (p.o, 50 mg/kg/day, QD) combination with metformin led to the decline of fasting blood glucose, show protective effect of β cells and decrease the hemoglobin A1c level in the STZ-induced T1D/T2D mouse models.Pharmacokinetic Parameters of IHMT-MST1-58 in different species (i.v. or p.o; 1 mg/kg, 5 mg/kg and 10 mg/kg). miceratsbeagle dogs
parameteri.v.(1 mg/kg)p.o.(10 mg/kg)i.v.(1 mg/kg)p.o.(10 mg/kg)i.v.(1 mg/kg)p.o.(10 mg/kg)
AUC0-t(ng/mL*h)501.155832553±155.14858±2648764.5±82.9 4939±1067
t1/2(h)1.71.813.51±0.343.03±0.26.47±0.715.79±1.09
Cmax/F (ng/mL)12401922944.0±219.11717±276466.7±45.21113±417
F(%)-110.8-73.3±40.1-106.5±20.9
Animal Model:mice
Dosage:50 mg/kg
Administration:oral, single
Result:parameterplasmapancreas
Cmax(ng/mL)3990±39012216±1509
AUC0-t(ng/mL*h)13621±212751394±10098
Cl(mL/h/kg)3734±641996±189
Animal Model:T1D mouse models and T2D mouse models
Dosage:50 mg/kg
Administration:p.o, 50 mg/kg/day, QD
Result:Decreased the FBG level, improved the food intake and water consumption, had lowHbA1c and a goodantidiabetic effect, improved the histological structure of the islet.
Animal Model:mice, Sprague Dawley rats, and beagle dogs
Dosage:1 mg/kg, 5 mg/kg and 10 mg/kg
Administration:intravenous injection and oral administration
Result:Displayed acceptable pharmacokinetic properties in different species.
体外研究：
IHMT-MST1-58 (compound 19) shows good activity against MST1 with an IC50 value of 23 nM.IHMT-MST1-58 (1 μM) displays strong inhibitory activity against MST1 (IC50 = 23 nM), weak activity against MST2 (IC50 = 652 nM), but no activity against NEK3 even at 10 μM (IC50 > 10 μM) .IHMT-MST1-58 (1 μM) shows strong binding affinity to MST1 and weak binding affinity to MST2 with Kd values of 240 nM and 2.7 μM.IHMT-MST1-58 (0.1-10 μM; 1-2 h) inhibits the phosphorylation of MST1 in vitro.IHMT-MST1-58 (0.03, 0.1 and 0.3 μM; 48 h) exhibits a significant protective effect of β cells from the damage caused by inflammatory cytokines.
IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes.
体内研究：
IHMT-MST1-58 (compound 19) (p.o, 50 mg/kg/day, QD) combination with metformin led to the decline of fasting blood glucose, show protective effect of β cells and decrease the hemoglobin A1c level in the STZ-induced T1D/T2D mouse models.Pharmacokinetic Parameters of IHMT-MST1-58 in different species (i.v. or p.o; 1 mg/kg, 5 mg/kg and 10 mg/kg). miceratsbeagle dogs
parameteri.v.(1 mg/kg)p.o.(10 mg/kg)i.v.(1 mg/kg)p.o.(10 mg/kg)i.v.(1 mg/kg)p.o.(10 mg/kg)
AUC0-t(ng/mL*h)501.155832553±155.14858±2648764.5±82.9 4939±1067
t1/2(h)1.71.813.51±0.343.03±0.26.47±0.715.79±1.09
Cmax/F (ng/mL)12401922944.0±219.11717±276466.7±45.21113±417
F(%)-110.8-73.3±40.1-106.5±20.9
Animal Model:mice
Dosage:50 mg/kg
Administration:oral, single
Result:parameterplasmapancreas
Cmax(ng/mL)3990±39012216±1509
AUC0-t(ng/mL*h)13621±212751394±10098
Cl(mL/h/kg)3734±641996±189
Animal Model:T1D mouse models and T2D mouse models
Dosage:50 mg/kg
Administration:p.o, 50 mg/kg/day, QD
Result:Decreased the FBG level, improved the food intake and water consumption, had lowHbA1c and a goodantidiabetic effect, improved the histological structure of the islet.
Animal Model:mice, Sprague Dawley rats, and beagle dogs
Dosage:1 mg/kg, 5 mg/kg and 10 mg/kg
Administration:intravenous injection and oral administration
Result:Displayed acceptable pharmacokinetic properties in different species.
体外研究：
IHMT-MST1-58 (compound 19) shows good activity against MST1 with an IC50 value of 23 nM.IHMT-MST1-58 (1 μM) displays strong inhibitory activity against MST1 (IC50 = 23 nM), weak activity against MST2 (IC50 = 652 nM), but no activity against NEK3 even at 10 μM (IC50 > 10 μM) .IHMT-MST1-58 (1 μM) shows strong binding affinity to MST1 and weak binding affinity to MST2 with Kd values of 240 nM and 2.7 μM.IHMT-MST1-58 (0.1-10 μM; 1-2 h) inhibits the phosphorylation of MST1 in vitro.IHMT-MST1-58 (0.03, 0.1 and 0.3 μM; 48 h) exhibits a significant protective effect of β cells from the damage caused by inflammatory cytokines.
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