AKP-11

• Target:

  Others|||LPL Receptor

• Related Pathways:

  Others|||GPCR/G Protein

• Bioactivity:

  AKP-11 is a sphingosine-1-phosphate receptor 1 (S1P1) agonist with an EC50 of 0.047 ?M for [35S]GTP?S binding to CHO-K1 cell membranes expressing human S1P1. It reduces S1P1 surface expression and enhances Akt and ERK phosphorylation in CHO cells with S1P1-HA at a 100 nM concentration. At doses of 1.3 and 3 mg/kg, AKP-11 lowers IFN-? and IL-17 protein levels in the spinal cord and mitigates disease severity in a rat experimental autoimmune encephalomyelitis (EAE) model. Additionally, it decreases peripheral total lymphocyte and specific T cell subsets (CD4+, CD8+, and CD26L+ T cells) counts in both EAE rats and healthy controls at a 1.3 mg/kg dosage.

• Smiles:

  ClC=1C=C(C=CC1OCCC)C2=NC(=NO2)C=3C=CC=4OC(=CC4C3)C(N)(CO)CO

• Molecular Formula:

  C22H22ClN3O5

• Molecular Weight:

  443.88

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  1220973-37-4