Complement System

C5a receptor peptide antagonist

Cyclosporine (cyclosporin A), a immunosuppressive agent, inhibits phosphatase activity of calcineurin with IC50 value of 5 nM .

SB 290157 (trifluoroacetate salt) is a potent and selective C3a receptor antagonist with an IC50 of 200 nM.

C5a receptor (C5aR) competitive antagonist

Complement inhibitor

C5a receptor antagonist

CD11b/CD18 activator

control peptide for Compstatin, a complement inhibitor

C3a 70-77 (Complement 3a (70-77)) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.

PMX 205 Trifluoroacetate is a potent complement C5a receptor (C5aR; CD88) antagonist.

BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.

BCX 1470 methanesulfonate inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.

Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5).

FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM.

LNP023 (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM.

Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM.

(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.

AMY-101 (Cp40) is the efficient inhibitor of the central complement component C3, with sub-nanomolar affinity for C3 (K D = 0.5nmol/L).

Dexamethasone is a corticosteroid compound that has been used as an adjuvant to reduce postoperative pain.

PMX 53 is a potent, cell-permeable, and orally active C5a receptor (CD88) antagonist with an IC 50 value of 20nM.

Negative control for PMX 53

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.

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.