S1P1 agonist 5,2760666-20-2

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S1P1 agonist 5

CAS No. : 2760666-20-2

MCE 国际站：S1P1 agonist 5

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: 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.

In Vivo: 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.

administration	parameters	rat	dog
i.v.	T1/2 (h)	1.4±0.3	5.70±1.2
	AUC0-∞ (ng*h/mL)	931.3±95.7	14,830.8±5475.4
	CL (mL/min/kg)	17.6±2.0	149.9±62.5
	Vss (L/kg)	1.7±0.2	828.7±134.2
p.o.	Cmax (ng/mL)	1661.1±916.6	3979.4±483.5
	Tmax(h)	0.9±0.8	1.3±0.5
	T1/2 (h)	1.4±0.2	4.9±0.6
	AUC0-∞ (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.

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