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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 .
Vilobelimab (CaCP-29, IFX-1) is a monoclonal anti-C5a antibody to the allergen C5a, a pro-inflammatory complement division product that plays a central role in mediating organ dysfunction. Vilobelimab acts as a C5a inhibitor, inhibiting neutrophil activation, chemotaxis, and reducing inflammatory signalling, and may be used in studies related to sepsis, COVID-19, etc .
W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively .
C5A is a microbicidal peptide, anti-hepatitis C virus (HCV), and anti-HIV agent. C5A disrupts the membrane integrity of the HIV virion as well as the integrity of the conical capsid core that surrounds the viral genome. C5A inhibits in vitro infectivity of a broad range of primary HIV isolates in various primary target cells. C5A protects mice against vaginal and rectal HIV challenges .
C5a Anaphylatoxin (human) is a pro-inflammatory peptide and a leukocyte chemoattractant. C5a Anaphylatoxin (human) can be used to study inflammation and immunity, such as allergic asthma .
C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases .
C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47) .
C5aR-IN-2 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-2 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 49) .
C5aR-IN-3 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-3 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 89) .
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .
CP-289,503 is an inhibitor of the complement C5a receptor with an IC50 of 1 μM. C5a acts as an activator of leukocytes and phagocytes during complement system activation. The C5a receptor can bind to C5a, which can stimulate the upregulation of cell surface integrins and degranulation of inflammatory cells, leading to endothelial cell damage. C5a receptor inhibitors can block C5a signaling and inhibit a variety of inflammatory diseases .
Avdoralimab (IPH 5401) is a fully human IgGκ monoclonal antibody that targets the complement C5a receptor 1 (C5aR1) that prevents its binding to C5a. Avdoralimab can be used for complement-driven inflammatory diseases and solid tumours research .
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research .
PMX 53 monoacetate (3D53 monoacetate) is a potent orally active CD88 (C5aR) antagonist that inhibits C5a-induced neutrophil myeloperoxide release and chemotactic activity. PMX 53 monoacetate has an IC50 value of 20 nM against C5a-induced neutrophil myeloperoxide release. >The value is 22 nM, and the IC50 value of the chemotactic activity is 75 nM. PMX 53 monoacetate is also an agonist of MrgX2 .
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects [5] .
NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC50 of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases .
L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH) .
JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation .
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus .
JPE-1375 is a complement C5a receptor 1(C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases .
SARS-CoV-2 3CLpro-IN-19 (Compound C5a) is a non-covalent, non-peptide SARS-CoV-2 3CLpro inhibitor (IC50s: 0.7 μM). SARS-CoV-2 3CLpro-IN-19 has broad-spectrum activity against Omicron subvariants (BA.5, BQ.1.1, and XBB.1.5) infection in human cells, with EC50 values between 30-69 nM .
Avacincaptad pegol (ARC1905) sodium is a 40KDa PEG-conjugated aptamer. Avacincaptad pegol sodium targets complement factor 5(C5), inhibits the cleavage of C5 into C5a and C5b, limits inflammatory stimulation and complement membrane attack complex (MAC), and is used to study age-related macular degeneration (AMD). Avacincaptad pegol sodium limits irregular cell apoptosis by targeting downstream factors in the complement cascade while preserving the early steps of the complement system. Avacincaptad pegol sodium treats Geographic atrophy (GA) mice .
4-Octylphenol is a hormone disruptor that has gender-specific effects on male reproductive cells, significantly reducing the mitotic index and the number of spermatogonia. 4-Octylphenol can cause inflammatory damage to fish gills by activating the complement system through the C3a/C3aR axis and the C5a/C5aR1 axis, this leads to complement activation and causes immune suppression due to the imbalance between Th1/Th2 cells and regulatory T cells (Treg)/Th17 cells, as well as inflammatory damage via the Toll-like receptor 7 (Toll-like Receptor (TLR))/IκBα/NF-κB pathway .
(R,R)-MK 287 is a tetrahydrofuran derivative that effectively inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with K1 values of 6.1 ± 1.5, 3.2 ± 0.7, and 5.49 ± 2.3 nM, respectively. The inhibition is stereospecific and competitive. Its racemate, L-668,750, is less potent, and its enantiomer, L-680574, is only 1/20 as potent as MK 287. MK 287 inhibits the binding of [3H]C18-PAF to human PMN membranes, reducing the affinity of the radioligand without changing the number of receptor sites. The binding of other radioligands (e.g., LTB4, LTC4, C5a, FMLP) to their specific receptors is unchanged at 1-10 microM MK 287. [3H]MK 287 binds to human platelet and PMN membranes with KD values of 2.1 ± 0.6 and 2.9 ± 1.2 nM. When tested on isolated human cells, MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50 = 56 ± 38 nM or ED50 = 1.5 ± 0.5 nM for gel-filtered platelets) and elastase release from PMNs (ED50 = 4.4 ± 2.6 nM). In vivo studies, MK 287 inhibited PAF-induced lethality in mice (ED50 = 0.8 mg/kg oral) and PAF-induced bronchospasm in guinea pigs (ED50 = 0.18 mg/kg intraduodenally and 0.19 mg/kg intravenously). The inhibition of PAF-induced bronchospasm was accompanied by a rightward shift in the concentration-response curve for PAF-induced platelet aggregation measured in vitro.
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5(C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM) .
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 .
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects [5] .
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5(C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM) .
C5A is a microbicidal peptide, anti-hepatitis C virus (HCV), and anti-HIV agent. C5A disrupts the membrane integrity of the HIV virion as well as the integrity of the conical capsid core that surrounds the viral genome. C5A inhibits in vitro infectivity of a broad range of primary HIV isolates in various primary target cells. C5A protects mice against vaginal and rectal HIV challenges .
C5a Anaphylatoxin (human) is a pro-inflammatory peptide and a leukocyte chemoattractant. C5a Anaphylatoxin (human) can be used to study inflammation and immunity, such as allergic asthma .
C5aR1 antagonist peptide is a biological active peptide. (This linear peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions to inhibit C5a binding and function at human and rat C5a receptors. C5a is crucial to triggering cellular immune responses and its overexpression is involved in arthritis, Alzheimer’s disease, cystic fibrosis, systemic lupus erythematosus, and other immunoinflammatory diseases.)
Vilobelimab (CaCP-29, IFX-1) is a monoclonal anti-C5a antibody to the allergen C5a, a pro-inflammatory complement division product that plays a central role in mediating organ dysfunction. Vilobelimab acts as a C5a inhibitor, inhibiting neutrophil activation, chemotaxis, and reducing inflammatory signalling, and may be used in studies related to sepsis, COVID-19, etc .
Avdoralimab (IPH 5401) is a fully human IgGκ monoclonal antibody that targets the complement C5a receptor 1 (C5aR1) that prevents its binding to C5a. Avdoralimab can be used for complement-driven inflammatory diseases and solid tumours research .
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research .
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus .
Complement C5/C5a Protein, Human is a recombinant human complement C5a. C5a is a 74-amino acid glycoprotein generated on activation of the C system. Complement C5 is cleaved by proteolysis in the terminal phase of complement activation generating the pro-inflammatory C5a and membrane attack complex nucleator C5b. C5a is an inflammatory mediator generated by complement activation that positively regulates various arms of immune defense, including Toll-like receptor 4 (TLR4) signaling.
Complement C5/C5a Protein, Mouse is a recombinant mouse complement component 5a (C5a). C5a is a potent pro-inflammatory mediator and acts as an essential part of the innate immune response.
Complement C5 is activated by C5 convertase, inducing C5-C9 assembly to form the membrane attack complex. The transient C6 binding site on C5b is critical for the formation of the cleavage complex. Complement C5/C5a Protein, Cynomolgus is the recombinant cynomolgus-derived Complement C5/C5a protein, expressed by E. coli , with tag free. The total length of Complement C5/C5a Protein, Cynomolgus is 74 a.a., with molecular weight of ~11 kDa.
Complement C5/C5a Protein, Mouse is a recombinant mouse complement component 5a (C5a). C5a is a potent pro-inflammatory mediator and acts as an essential part of the innate immune response.
Complement C5 is activated by C5 convertase, inducing C5-C9 assembly to form the membrane attack complex. The transient C6 binding site on C5b is critical for the formation of the cleavage complex. Complement C5 Protein, Human (HEK293, His) is the recombinant human-derived Complement C5 protein, expressed by HEK293 , with C-His labeled tag. The total length of Complement C5 Protein, Human (HEK293, His) is 1658 a.a., with molecular weight of 110-114 kDa (α chain) & 69-73 kDa (β chain), respectively.
C5AR1 Protein-VLP, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236. Tags can only be detected under denaturing conditions.
The C5AR2 protein is a receptor for C3a, C4a, and C5a peptides as well as ASP/C3adesArg, C4adesArg, and C5adesArg, and is weakly coupled to G(i)-mediated signaling pathways. It interacts with C3 and exhibits higher affinity for the lipogenic hormone ASP. C5AR2 Protein, Human (Cell-Free, His) is the recombinant human-derived C5AR2 protein, expressed by E. coli Cell-free , with C-10*His labeled tag. The total length of C5AR2 Protein, Human (Cell-Free, His) is 337 a.a., with molecular weight of 38.9 kDa.
Complement C5/C5a Protein activates late complement components to form the membrane attack complex, C5-C9. C5b binds C6, initiating lytic complex assembly. C5a, produced by C5 degradation, acts as an anaphylatoxin, inducing local inflammation. C5a stimulates intracellular calcium release, smooth muscle contraction, vascular permeability, histamine release, and acts as a chemokine, guiding leukocyte migration. Complement C5/C5a Protein, Mouse (Biotinylated) is the recombinant mouse-derived Complement C5/C5a protein, expressed by E. coli, with tag free. The total length of Complement C5/C5a Protein, Mouse (Biotinylated) is 77 a.a., with molecular weight of ~9 KDa.
Complement C5/C5a Protein, a component of the complement system, is involved in the immune response and inflammation. It is cleaved to generate C5a, a potent pro-inflammatory mediator. Complement C5/C5a Protein's role in immune regulation and its potential as a therapeutic target make it a promising candidate for the treatment of inflammatory disorders and autoimmune diseases. Complement C5a anaphylatoxin Protein, Pig (P.pastoris, His) is the recombinant pig-derived Complement C5a anaphylatoxin protein, expressed by P. pastoris , with N-His labeled tag.
Complement C5 is activated by C5 convertase, inducing C5-C9 assembly to form the membrane attack complex. The transient C6 binding site on C5b is critical for the formation of the cleavage complex. Complement C5/C5a Protein, Human (His) is the recombinant human-derived Complement C5/C5a protein, expressed by E. coli , with N-His labeled tag. The total length of Complement C5/C5a Protein, Human (His) is 74 a.a., with molecular weight of 13-14 kDa.
Avacincaptad pegol (ARC1905) sodium is a 40KDa PEG-conjugated aptamer. Avacincaptad pegol sodium targets complement factor 5(C5), inhibits the cleavage of C5 into C5a and C5b, limits inflammatory stimulation and complement membrane attack complex (MAC), and is used to study age-related macular degeneration (AMD). Avacincaptad pegol sodium limits irregular cell apoptosis by targeting downstream factors in the complement cascade while preserving the early steps of the complement system. Avacincaptad pegol sodium treats Geographic atrophy (GA) mice .
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