human cxcr3

SCH 546738 是一种可口服且具有选择性和高效性的 CXCR3 拮抗剂，可减轻自身免疫性疾病的发展并延迟移植物排斥反应。

PS372424 is a specific agonist of human CXCR3, with anti-inflammatory activity.

(R)-SCH 546738为SCH 546738的R-构型。该化合物是一种口服有效的非竞争性CXCR3拮抗剂，其对人类CXCR3受体的Ki值为0.4 nM。

ZK 756326 是一种选择性的非肽 CCR8 趋化因子受体激动剂（IC50：1.8 μM，在人体内；2.6 μM，在小鼠体内）。对 CCR4 5 和 CXCR3 4 没有活性，比其他 26 种 GPCR 的选择性高 28 倍（对 α2A 和 5-HT 受体的选择性较低）。诱导趋化性并抑制 Env 介导的 (HIV) 细胞-细胞融合。

CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM). 1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonistsBioorg. Med. Chem. Lett.16(1)200-203(2006)

PS372424 is a specific agonist of human CXCR3. It has been shown to induce phosphorylation of ERK and block CXCL11 induced migration of CD45+ cells to air pouches generated on humanized mice.