Complement System Agonist

Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC₅₀ of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.

TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC₅₀: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca²⁺. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.

C3a receptor agonist 1 (compound benzeneacetamide) is a potent C3a receptor agonist. C3a receptor agonist 1 has the potential for the research of acute inflammation.

BM213 is a selective C5aR agonist, with an EC₅₀ of 59 nM. BM213 specifically activates the C5a-C5aR1 axis, which in turn promotes neutrophil extracellular trap (NET) formation and exacerbates inflammatory responses. BM213 significantly induces ventricular dilationin, promotes myocardial ROS production, and induces cardiomyocyte apoptosis in rats. BM213 can be used for the study of myocardial ischemia/reperfusion (I/R) injury.

C5a Receptor agonist, W5Cha (Peptide 1) is a selective complement C5a receptor (C5aR) agonist (EC₅₀=0.2 μM), a hexapeptide derived from the C-terminus of C5a with specific amino acid modifications. C5a Receptor agonist, W5Cha is able to interact with the Arg-206 site of the C5a receptor through its C-terminal arginine, thereby activating the receptor.

ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

C5aR2 agonist P32 (Ac-RHYPYWR-OH) is a C5aR2-selective agonist. C5aR2 agonist P32 has been shown to elicit multiple immunomodulatory activities, both by down-regulating the C5aR1-mediated cell signalling, and acting in a C5aR1-independent fashion, in vitro and in vivo.

(Trp63,Trp64)​-​C3a(63-77) is a C3a synthetic analogue peptide, which exhibits Ca²⁺ stimulating efficacy in human neutrophils and hC3aR or mC3aR expressing RBL-2H3 cells with EC₅₀ of 9.5, 2.0 and 0.8 nM, respectively.

(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

[DArg10, DAla20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aR agonist (EC₅₀: 87 nM for β-arrestin recruitment). [DArg10, DAla20] TLQP-21 elicits calcium influx. [DArg10, DAla20] TLQP-21 slightly but not significantly potentiates adrenergic-induced lipolysis. [DArg10, DAla20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions.

TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC₅₀: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca²⁺. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.

C5aR2 agonist P32 (Ac-RHYPYWR-OH) acetate is a C5aR2-selective agonist. C5aR2 agonist P32 acetate has been shown to elicit multiple immunomodulatory activities, both by down-regulating the C5aR1-mediated cell signalling, and acting in a C5aR1-independent fashion, in vitro and in vivo.

Leukadherin-1 (Standard) is the analytical standard of Leukadherin-1. This product is intended for research and analytical applications. Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.