cxcr3

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)

rac-NBI-74330 is an effective and selective CXCR3 antagonist.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

L-asarinin ((-)-Episesamin) reduces peripheral blood concentration of IL-12 and inhibits the expression of CXCR3 and TLR4, which means Asarinin may have a role on the TLR4 pathway and produce prolongation of allograft heart survival.

VUF-11222 is a CXCR3 nonmimetic peptide agonist that induces gliosis.VUF 11222 has been used in the study of retinal inflammation.

AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively).

VUF10132 is a full inverse CXCR3 N3.35A agonist.

VUF5834 is a full inverse agonist of CXCR3 N3.35A.

ACT-660602 is an orally active chemokine receptor CXCR3 antagonist (IC50: 204 nM). ACT-660602 inhibits T cell migration and has shown significant effects in an in vivo model of acute lung injury. ACT-660602 can be used to study autoimmune diseases.

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

SCH 546738 is an effective and non-competitive CXCR3 antagonist. SCH 546738 bindings to the human CXCR3 receptor is determined (Ki: 0.4 nM) in multiple experiments.

ACT-672125 is a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases. ACT-672125 showed good physicochemical properties and safety profile. In a proof-of-mechanism model of lung inflammation, ACT-672125 inhibited the recruitment of CXCR3 expressing T cells into the inflamed lung in a dose-dependent manner.

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.

ACT-777991 is an orally active, selective CXCR3 antagonist with demonstrated stability in microsomes and hepatocytes across various animal models. This compound effectively inhibits the migration of activated T cells toward CXCL11.

ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4/5 and CXCR3/4 and shows higher 28-fold selectivity over 26 other GPCRs (less selective at α2A and 5-HT receptors). Induces chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion.

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).

AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an CXCR3 antagonist.

VUF11211 is an effective antagonist of CXCR3 that acts by extending from the minor pocket into the major pocket of the transmembrane domains.

(-)-Asarinin (Eleutheroside B4) shows antibacterial activity.