Avacopan is a potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.

Danicopan (ACH-4471, ACH-0144471) is a highly potent, orally active Factor D inhibitor with Kd of 0.54 nM, inhibits the proteolytic activity of purified Factor D against substrate Factor B in complex with C3b, blocking production of Bb fragment IC50 of 15 nM.

Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.

(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.

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.

Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system.

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.

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.

AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.

FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN

Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases.

Compstatin control peptide is a complement inhibitor that binds and inhibits cleavage of complement C3.

POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research

POT-4 TFA (AL-78898A TFA), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 TFA can be used for age-related macular degeneration research.

Compstatin control peptide TFA is a complement inhibitor that binds and inhibits cleavage of complement C3.

Vemircopan is a complement factor D inhibitor.

Lipoteichoic acid, a cell wall component of Staphylococcus aureus, activates the complement system via C3 induction and CD55 inhibition.

Cemdisiran is an N-acetylgalactosamine (GalNAc) conjugated siRNA for the treatment of complement-mediated diseases by suppressing liver production of complement 5 (C5) protein.

AMY-101 (Cp40) is a peptidic inhibitor of the central complement component C3 for the management of patients with ARDS caused by SARS-CoV-2 infection.AMY-101 is a novel complement C3-targeted therapeutic based on the 3 rd-generation compstatin analog Cp40.

C5 complement inhibitor 7 (C5-IN-7) is a potent, small-molecule inhibitor of C5 complement protein with serum assay IC50 of <5 nM (2% human serum complement inhibition).C5-IN-7 demonstrated excellent potency and good aqueous solubility, inhibited MAC deposition with IC50 of 1 uM in a complement inhibition assay using 50% human whole blood.The C5 triple mutants (C704R, V705I and N707H) were not inhibited by C5 complement protein inhibitor 7 up to 100 uM.C5 complement protein inhibitor 7 binds within the predicted pocket between the C5a and MG8 domains in close proximity to the C5 convertase cleavage site (R751-L752).

DF2593A (DF 2593A) is a potent, selective, noncompetitive allosteric inhibitor of C5aR with IC50 of 5 nM (C5a-induced human PMN migration inhibition), and rat and mouse orthologs (IC50=6.0 nM and IC50=1.0 nM, respectively); dispalys >1,000-fold selective versus other chemoattractants, including CXCL8 and CXCL1 (CI50>10 uM), as well as on a panel of different GPCRs and ion channels; DF2593A demonstrated antinociceptive effects in several models of inflammatory pain and effectively inhibited articular hyperalgesia in CFA-induced mechanical and thermal hyperalgesia and arthritic nociception.

JPE1375 is a potent, peptidomimetic C5a receptor antagonist with IC50 of 39 nM.JPE1375 inhibits neutrophil influx in the RPAR in mice.

Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC50 value of 14.3 nM. Pelecopan can target factor D to prevent both intravascular and extravascular hemolysis in PNH. Pelecopan also be used for other alternative pathway (AP) mediated diseases.

CP-447697 is a lipophilic C5a receptor antagonist with an IC50 value of 31 nM. CP-447697 can be used for the research of inflammation.

CMP-1611 is a small molecule inhibitor of protease of the complement classical pathway, C1r, directly inhibits classical pathway-specific complement activation in a dose-dependent manner.

DF3016A (DF 3016A) is a potent and selective C5aR inhibitor with IC50 of 50 nM (C5a-induced human PMN migration and IC50 of 45 and 37 nM against rat and mouse C5aR, respectively.

T-ALZ01 (CMP-1696) is a small molecule inhibitor of complement component C1r.

Peptide WWGKKYRASKLGLAR is a super agonist of complement factor C3aR, 12-15 times more active than natural C3a.