产品
编 号：F756725
分子式：C34H35NO6
分子量：553.64
分子式：C34H35NO6
分子量：553.64
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CAS No: 2901084-32-8
产品详情
生物活性：
PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs).
体内研究：
PDE4-IN-12 (5 mg/kg; i.p.; twice daily for 8 days) ameliorates mouse acute colitis induced by DSS (dextran sulfate sodium).PDE4-IN-12 (10 mg/kg; p.o.; single) shows well tolerated in dogs.PDE4-IN-1 (2.5 mg/kg; i.v.; single) shows great plasma exposure, with T1/2 and AUC0-24 h values of 4.18 h and 6522 h?ng/mL.Animal Model:Male C57BL/6 mice (5 to 6-week old; 15-17 g; DSS-induced mouse model).
Dosage:5 mg/kg
Administration:Intraperitoneal injection; twice daily for 8 days.
Result:Ameliorated the acute colitis by decreasing disease activity index, increasing the colon length, and also ameliorating the pathological damages.
Animal Model:Beagle dogs.
Dosage:10 mg/kg (solved in 0.5% CMC-Na solution).
Administration:Oral administration; single.
Result:Exhibited good safety, which caused no emesis on beagle dogs at 10 mg/kg.
Animal Model:Male C57BL/6 mice (5 to 6-week old; 15-17 g).
Dosage:2.5 mg/kg
Administration:Intravenous injection; single.
Result:1.19Pharmacokinetic Parameters of PDE4-IN-12 in Male C57BL/6 mice.T1/2 (h)AUC0-24 h (h?ng/mL)MRT0-24 h (h)CL (mL/min/kg)Vss (mL/kg)
IV (2.5 mg/kg)4.1865221.766.40673
体外研究：
PDE4-IN-12 (compound 22d) (10, 20 μM; 24 h) reduces the release of NO in LPS induced inflammation cell model (indicates anti-inflammatory effect).
PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs).
体内研究：
PDE4-IN-12 (5 mg/kg; i.p.; twice daily for 8 days) ameliorates mouse acute colitis induced by DSS (dextran sulfate sodium).PDE4-IN-12 (10 mg/kg; p.o.; single) shows well tolerated in dogs.PDE4-IN-1 (2.5 mg/kg; i.v.; single) shows great plasma exposure, with T1/2 and AUC0-24 h values of 4.18 h and 6522 h?ng/mL.Animal Model:Male C57BL/6 mice (5 to 6-week old; 15-17 g; DSS-induced mouse model).
Dosage:5 mg/kg
Administration:Intraperitoneal injection; twice daily for 8 days.
Result:Ameliorated the acute colitis by decreasing disease activity index, increasing the colon length, and also ameliorating the pathological damages.
Animal Model:Beagle dogs.
Dosage:10 mg/kg (solved in 0.5% CMC-Na solution).
Administration:Oral administration; single.
Result:Exhibited good safety, which caused no emesis on beagle dogs at 10 mg/kg.
Animal Model:Male C57BL/6 mice (5 to 6-week old; 15-17 g).
Dosage:2.5 mg/kg
Administration:Intravenous injection; single.
Result:1.19Pharmacokinetic Parameters of PDE4-IN-12 in Male C57BL/6 mice.T1/2 (h)AUC0-24 h (h?ng/mL)MRT0-24 h (h)CL (mL/min/kg)Vss (mL/kg)
IV (2.5 mg/kg)4.1865221.766.40673
体外研究：
PDE4-IN-12 (compound 22d) (10, 20 μM; 24 h) reduces the release of NO in LPS induced inflammation cell model (indicates anti-inflammatory effect).
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