Complement System Antagonist

SB290157 trifluoroacetate is a potent and selective C3a receptor antagonist with an IC₅₀ of 200 nM.

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.

EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC₅₀ of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.

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.

PMX 205 Trifluoroacetate is a specific complement C5aR1 isoform antagonist.

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

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.

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 K_i value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca²⁺ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC₅₀s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.

NRP1 antagonist 1 (compound 12a) is a potent NRP1 antagonist with an IC₅₀ of 19.1 μM. NRP1 antagonist 1 has the potential for cancer research.

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.

NRP1 antagonist 2 (Compound 1) is an NRP1 antagonist.

Izicopan (INF056) is a complement factor C5a receptor antagonist. Izicopan inhibits C5a-induced calcium mobilization with an IC₅₀ of 10-100 nM.

SB290157 (trifluoroacetate) (Standard) is the analytical standard of SB290157 (trifluoroacetate) (HY-101502A). This product is intended for research and analytical applications. SB290157 trifluoroacetate is a potent and selective C3a receptor antagonist with an IC50 of 200 nM.

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.

[DArg10, Aib20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aRpartial agonist, C3aR functional antagonist (EC₅₀: 854 nM for β-arrestin recruitment). [DArg10, Aib20] TLQP-21 shows no significant calcium flux activity. [DArg10, Aib20] TLQP-21 shows no activity in potentiating adrenergic-induced lipolysis. [DArg10, Aib20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions.

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.

C5aR antagonist-1 is a potent C5aR antagonist with an IC₅₀ of < 5 nM. C5aR antagonist-1 is applicable to the research of crescentic and necrotizing glomerular lesions.

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.

ACT-1014-6470 is an orally active, potent, reversible, and selective C5aR1 antagonist. ACT-1014-6470 demonstrates potent inhibition of C5aR1 activation. ACT-1014-6470 can be used in the research of inflammatory diseases.

EG00229 trifluoroacetate (Standard) is the analytical standard of EG00229 (trifluoroacetate) (HY-10799). This product is intended for research and analytical applications. EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC₅₀ of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.