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S1P1 agonist 1

MCE China：S1P1 agonist 1

Brand：MedChemExpress (MCE)

Cat. No.HY-104069

CAS：1220973-37-4

Purity：98.75%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.

In Vitro：S1P1 Agonist 1 binds to S1P1 is internalized and activates intracellular AKT and ERKs cellular signaling pathways. S1P1 Agonist 1 mediated S1P1 downregulation is independent of sphingosine kinase activity indicating it to be a direct agonist of S1P1. S1P1 Agonist 1 decreases cell surface expression of S1P1 in in vitro cell culture model[1].

In Vivo：S1P1 Agonist 1 (1.3mg/kg) attenuates EAE disease. EAE is the animal model of multiple sclerosis which is extensively used for investigating clinical studies for multiple sclerosis drugs. S1P1 Agonist 1 treatment reduces peripheral total blood lymphocyte and T lymphocyte counts significantly. The reduction in total lymphocytes and T cells are 48% and 41% in AKP-11 treated animals, respectively. The reduction in the CD4+ and CD8+ T cell populations are 41% and 40% in S1P1 Agonist 1 treated animals, respectively. S1P1 Agonist 1 treatment reduces CNS infiltration of T cells and Cytokines and enhances neuroprotection. S1P1 Agonist 1 treatment has little effect on the heart rate of animals. The decrease in blood pressure is also smaller with S1P1 Agonist 1 treatment as compared animals treated with FTY720[1].

Animal Administration：Rats: EAE is induced in female Lewis rats with guinea pig MBP (25 μg/rat). EAE developed rats are divided into 3 groups on day 11 or 12 after immunization and administered vehicle or S1P1 Agonist 1 (3 or 1.3 mg/kg) or FTY720 (1 mg/kg) orally every day until day 26. Rats are administrated orally with 1.3 mg/kg S1P1 Agonist 1, 1 mg/kg FTY720 and vehicle. After post administration, heart rates are measured at 1, 2, 4, 6, 12, and 24 hr[1].

IC50 & Target：S1P1[1] In Vitro S1P1 Agonist 1 binds to S1P1 is internalized and activates intracellular AKT and ERKs cellular signaling pathways. S1P1 Agonist 1 mediated S1P1 downregulation is independent of sphingosine kinase activity indicating it to be a direct agonist of S1P1. S1P1 Agonist 1 decreases cell surface expression of S1P1 in in vitro cell culture model[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> S1P1 agonist 1 Related Antibodies

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References：

[1]. Samuvel DJ, et al. AKP-11 - A Novel S1P1 Agonist with Favorable Safety Profile Attenuates Experimental Autoimmune Encephalomyelitis in Rat Model of Multiple Sclerosis. PLoS One. 2015 Oct 29;10(10):e0141781.  [Content Brief]