Name: AKP-11
Rating: 5 (10 reviews)

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HIT ID:HIT217659540
Cas No:1220973-37-4
常用名:AKP-11
IUPAC:2-amino-2-{5-[5-(3-chloro-4-propoxyphenyl)-1,2,4-oxadiazol-3-yl]-1-benzofuran-2-yl}propane-1,3-diol
IUPAC:2-amino-2-{5-[5-(3-chloro-4-propoxyphenyl)-1,2,4-oxadiazol-3-yl]-1-benzofuran-2-yl}propane-1,3-diol
InChI key:YHNUTRJSCOJJKX-UHFFFAOYSA-N

分子式:C22H22ClN3O5
分子量:443.88
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:CCCOc1ccc(cc1Cl)-c1nc(no1)-c1ccc2oc(cc2c1)C(N)(CO)CO
SMILES:CCCOc1ccc(cc1Cl)-c1nc(no1)-c1ccc2oc(cc2c1)C(N)(CO)CO

AKP-11 is a sphingosine-1-phosphate receptor 1 (S1P1) agonist with an EC50 of 0.047 μM for [35S]GTPγS 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-γ 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.

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