产品
编 号：F755819
分子式：C38H41ClN4OS
分子量：637.28
分子式：C38H41ClN4OS
分子量：637.28
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CAS No: 2766739-35-7
产品详情
生物活性：
RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression.
体内研究：
RAGE/SERT-IN-1 (0-10 μM; 60 min) has good liver microsomal stability and does not apparently inhibit main CYP enzymes.RAGE/SERT-IN-1 (100 and 200mg/kg; IP; single dosage) does not cause mice death and not significant change in the ratio of organ-to-body weight at 100 mg/kg.RAGE/SERT-IN-1 (60 mg/kg; PO; single dosage) significantly reduces the immobility time in tail suspension test.RAGE/SERT-IN-1 (60 mg/kg for PO, 10 mg/kg for IV; single dosage) exhibits acceptable pharmacokinetic properties in mice.Pharmacokinetic Parameters of RAGE/SERT-IN-1 in male ICR mice.PO (60 mg/kg) IV (10 mg/kg)
T1/2 (h)5.553.46
Cmax (ng/mL)493551745
AUC0-∞ (ng/mL·h)2468423653
CL (mL/min/kg)7.09
VSS (L/kg)1037
F (%)17.1
Animal Model:Male ICR mice (24-26 g)
Dosage:100mg/kg and 200mg/kg
Administration:IP; single (observed for 2 weeks)
Result:All mice were survived and no significant changed in the ratio of organ-to-body weight at a dose of 100 mg/kg.
Animal Model:Male ICR mice
Dosage:60 mg/kg
Administration:PO; single dosage
Result:Significantly reduced the immobility time in tail suspension test.
Animal Model:Male ICR mice
Dosage:60 mg/kg for PO, 10 mg/kg for IV
Administration:PO and IV; single dosage
Result:Exhibited acceptable pharmacokinetic properties in mice.
体外研究：
RAGE/SERT-IN-1 (compound 12) (1-20 μM; 24 hours) does not significantly affect cell viability of SH-SY5Y.
RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression.
体内研究：
RAGE/SERT-IN-1 (0-10 μM; 60 min) has good liver microsomal stability and does not apparently inhibit main CYP enzymes.RAGE/SERT-IN-1 (100 and 200mg/kg; IP; single dosage) does not cause mice death and not significant change in the ratio of organ-to-body weight at 100 mg/kg.RAGE/SERT-IN-1 (60 mg/kg; PO; single dosage) significantly reduces the immobility time in tail suspension test.RAGE/SERT-IN-1 (60 mg/kg for PO, 10 mg/kg for IV; single dosage) exhibits acceptable pharmacokinetic properties in mice.Pharmacokinetic Parameters of RAGE/SERT-IN-1 in male ICR mice.PO (60 mg/kg) IV (10 mg/kg)
T1/2 (h)5.553.46
Cmax (ng/mL)493551745
AUC0-∞ (ng/mL·h)2468423653
CL (mL/min/kg)7.09
VSS (L/kg)1037
F (%)17.1
Animal Model:Male ICR mice (24-26 g)
Dosage:100mg/kg and 200mg/kg
Administration:IP; single (observed for 2 weeks)
Result:All mice were survived and no significant changed in the ratio of organ-to-body weight at a dose of 100 mg/kg.
Animal Model:Male ICR mice
Dosage:60 mg/kg
Administration:PO; single dosage
Result:Significantly reduced the immobility time in tail suspension test.
Animal Model:Male ICR mice
Dosage:60 mg/kg for PO, 10 mg/kg for IV
Administration:PO and IV; single dosage
Result:Exhibited acceptable pharmacokinetic properties in mice.
体外研究：
RAGE/SERT-IN-1 (compound 12) (1-20 μM; 24 hours) does not significantly affect cell viability of SH-SY5Y.
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