产品
编 号：F755577
分子式：C23H24ClN2NaO4
分子量：450.89
分子式：C23H24ClN2NaO4
分子量：450.89
产品类型
规格
价格
是否有货
结构图
CAS No: 2760666-20-2
产品详情
生物活性：
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
体内研究：
S1P1 agonist 5 shows good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).S1P1 agonist 5 (10 mg/kg; p.o.) inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours.S1P1 agonist 5 (3, 10 mg/kg, p.o., once daily for 20 days) ameliorates the disease progression and overall severity in EAE mice, showing favorable drug-like properties.Pharmacokinetic Parameters of S1P1 in rats, male beagle dogs.administrationparameters rat dog
i.v.T1/2 (h)1.4±0.35.70±1.2
AUC0-∞ (ng*h/mL)931.3±95.714,830.8±5475.4
CL (mL/min/kg)17.6±2.0149.9±62.5
Vss (L/kg)1.7±0.2828.7±134.2
p.o.Cmax (ng/mL)1661.1±916.63979.4±483.5
Tmax(h)0.9±0.81.3±0.5
T1/2 (h)1.4±0.24.9±0.6
AUC0-∞ (ng*h/mL)5044.9±106123,109.9±7752.2
F (%)54.231.8
Rats, 1 mg/kg for i.v.; 10 mg/kg for p.o.. dogs, 2 mg/kg i.v.;10 mg/kg for p.o.Animal Model:rats, male beagle dogs
Dosage:
Administration:1 mg/kg for i.v. and 10 mg/kg for p.o (rats); 2 mg/kg for i.v. and 10 mg/kg for p.o.(dogs)
Result:Showed good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).
Animal Model:male wistar rats (5 week, 160-180 g)
Dosage:10 mg/kg
Administration:p.o.
Result:Inhibited the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours.
Animal Model:female C57BL/6 mice (10 weeks,19?22 g) (experimental autoimmune encephalitis (EAE) mouse model)
Dosage:3, 10 mg/kg (dissolved in 2.5% DMSO and 5% Kolliphor HS 15 (Sigma-Aldrich) in distilled water)
Administration:p.o., once daily, 20 days
Result:Ameliorated the disease progression and overall severity in EAE mice, showing favorable drug-like properties.
体外研究：
S1P1 agonist 5 (compound 21l) shows excellent in vitro efficacies with EC50s of 7.03 nM and 11.8 nM for β-arrestin recruitment and internalization, respectively.
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
体内研究：
S1P1 agonist 5 shows good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).S1P1 agonist 5 (10 mg/kg; p.o.) inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours.S1P1 agonist 5 (3, 10 mg/kg, p.o., once daily for 20 days) ameliorates the disease progression and overall severity in EAE mice, showing favorable drug-like properties.Pharmacokinetic Parameters of S1P1 in rats, male beagle dogs.administrationparameters rat dog
i.v.T1/2 (h)1.4±0.35.70±1.2
AUC0-∞ (ng*h/mL)931.3±95.714,830.8±5475.4
CL (mL/min/kg)17.6±2.0149.9±62.5
Vss (L/kg)1.7±0.2828.7±134.2
p.o.Cmax (ng/mL)1661.1±916.63979.4±483.5
Tmax(h)0.9±0.81.3±0.5
T1/2 (h)1.4±0.24.9±0.6
AUC0-∞ (ng*h/mL)5044.9±106123,109.9±7752.2
F (%)54.231.8
Rats, 1 mg/kg for i.v.; 10 mg/kg for p.o.. dogs, 2 mg/kg i.v.;10 mg/kg for p.o.Animal Model:rats, male beagle dogs
Dosage:
Administration:1 mg/kg for i.v. and 10 mg/kg for p.o (rats); 2 mg/kg for i.v. and 10 mg/kg for p.o.(dogs)
Result:Showed good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).
Animal Model:male wistar rats (5 week, 160-180 g)
Dosage:10 mg/kg
Administration:p.o.
Result:Inhibited the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours.
Animal Model:female C57BL/6 mice (10 weeks,19?22 g) (experimental autoimmune encephalitis (EAE) mouse model)
Dosage:3, 10 mg/kg (dissolved in 2.5% DMSO and 5% Kolliphor HS 15 (Sigma-Aldrich) in distilled water)
Administration:p.o., once daily, 20 days
Result:Ameliorated the disease progression and overall severity in EAE mice, showing favorable drug-like properties.
体外研究：
S1P1 agonist 5 (compound 21l) shows excellent in vitro efficacies with EC50s of 7.03 nM and 11.8 nM for β-arrestin recruitment and internalization, respectively.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备