S1P1 agonist 5 是一种选择性和具有口服活性的S1P1激动剂。S1P1 agonist 5 抑制淋巴细胞从淋巴组织排出到外周血。S1P1 agonist 5 具有研究多发性硬化症 (MS) 的潜力。

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) [1].

S1P1 agonist 5 (compound 21l) shows excellent in vitro efficacies with EC 50 s of 7.03 nM and 11.8 nM for β -arrestin recruitment and internalization, respectively [1].

S1P1 agonist 5 shows good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%) [1]. 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 [1]. 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 [1]. Pharmacokinetic Parameters of S1P1 in rats, male beagle dogs [1]. administration parameters rat dog i.v. T 1/2 (h) 1.4±0.3 5.70±1.2 AUC 0-∞ (ng*h/mL) 931.3±95.7 14,830.8±5475.4 CL (mL/min/kg) 17.6±2.0 149.9±62.5 V ss (L/kg) 1.7±0.2 828.7±134.2 p.o. C max (ng/mL) 1661.1±916.6 3979.4±483.5 T max (h) 0.9±0.8 1.3±0.5 T 1/2 (h) 1.4±0.2 4.9±0.6 AUC 0-∞ (ng*h/mL) 5044.9±1061 23,109.9±7752.2 F (%) 54.2 31.8 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. [1] Animal Model: rats, male beagle dogs [1] 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) [1] 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) [1] 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.

C23H24ClN2NaO4

450.89

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years