Complement System

By Targets:	Complement System (14) HIV Protease (1) Liposome (1)
By Research Areas:	Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (13) Metabolic Disease (2)

Targets Recommended: Complement System

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N9481

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

HY-128570

FD-IN-1	Complement System	Inflammation/Immunology
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-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC₅₀s of 7.7 and 6.5 µM, respectively .

HY-P990091

Riliprubart SAR 445088	Complement System	Inflammation/Immunology
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .

HY-P1036

Compstatin 1 Publications Verification	Complement System	Others
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-P1036A

Compstatin TFA 1 Publications Verification	Complement System	Others
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 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. Compstatin TFA exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-W049802

N-((Allyloxy)carbonyl)-N-methyl-L-alanine	Complement System	Inflammation/Immunology
N-((Allyloxy)carbonyl)-N-methyl-L-alanine is a Alanine derivative. N-((Allyloxy)carbonyl)-N-methyl-L-alanine can be used for the synthesis of inhibitors of complement factor D. Complement factor D inhibitors can be used in the research of immune system related disease .

HY-P9914

Eculizumab Anti-Human C5, Humanized Antibody	Complement System	Cardiovascular Disease
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 .

HY-147604

Factor B-IN-2	Complement System	Inflammation/Immunology
Factor B-IN-2 (Example 1 target compound) is a potent complement factor B inhibitor, with an IC₅₀ of 1.5 μM. Factor B-IN-2 can be used for the research of diseases related to inflammation and immunity .

HY-147605

Factor B-IN-3	Complement System	Inflammation/Immunology
Factor B-IN-3 (Example 3 target compound) is a potent complement factor B inhibitor. Factor B-IN-3 can be used for the research of diseases related to inflammation and immunity .

HY-147606

Factor B-IN-4	Complement System	Inflammation/Immunology
Factor B-IN-4 (Example 13 target compound) is a potent complement factor B inhibitor, with an IC₅₀ of 1 μM. Factor B-IN-4 can be used for the research of diseases related to inflammation and immunity .

HY-147607

Factor B-IN-5	Complement System	Inflammation/Immunology
Factor B-IN-5 (Example 5 target compound) is a potent complement factor B inhibitor, with an IC₅₀ of 1.2 μM. Factor B-IN-5 can be used for the research of diseases related to inflammation and immunity .

HY-N2996

Ganodermanondiol	HIV Protease	Infection
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum .Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC₅₀ of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC₅₀ of 41.7μM .

HY-163378

C5aR1 antagonist 1	Complement System	Inflammation/Immunology
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 .

HY-127105

Iptacopan 3 Publications Verification LNP023	Complement System	Metabolic Disease Inflammation/Immunology
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC₅₀ value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a K_D of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .

HY-127105A

Iptacopan hydrochloride 3 Publications Verification LNP023 hydrochloride	Complement System Liposome	Metabolic Disease Inflammation/Immunology
LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a K_D of 7.9 nM. LNP023 inhibits factor B with an IC₅₀ value of 10 nM .

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus	2988 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery. MCE covalent inhibitor library contains 2988 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc. MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

Covalent Screening Library Plus

2988 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 2988 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

Cat. No.	Product Name	Target	Research Area

HY-P1036

Compstatin 1 Publications Verification	Complement System	Others
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-P1036A

Compstatin TFA 1 Publications Verification	Complement System	Others
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 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. Compstatin TFA exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-P1398

Compstatin control peptide	Peptides	Inflammation/Immunology
Compstatin control peptide is a negative control of Compstatin (HY-P1036). Compstatin is a potent complement system C3 inhibitor .

HY-W049802

N-((Allyloxy)carbonyl)-N-methyl-L-alanine	Complement System	Inflammation/Immunology
N-((Allyloxy)carbonyl)-N-methyl-L-alanine is a Alanine derivative. N-((Allyloxy)carbonyl)-N-methyl-L-alanine can be used for the synthesis of inhibitors of complement factor D. Complement factor D inhibitors can be used in the research of immune system related disease .

HY-P1398A

Compstatin control peptide TFA	Peptides	Inflammation/Immunology
Compstatin control peptide TFA is a negative control of Compstatin (HY-P1036). Compstatin is a potent complement system C3 inhibitor .

HY-P5528

2Abz-SLGRKIQIK(Dnp)-NH2	Peptides	Others
2Abz-SLGRKIQIK(Dnp)-NH2 is a biological active peptide. (This peptide is a second complement component (C2), the physiological substrate for the proenzyme Cls, first complement component. The complement system is a central component of host defense but can also contribute to the inflammation seen in pathological conditions. The C1s protease of the C1 complex initiates the host defense pathway. This peptide employs 2Abz/Dnp FRET pair for quantitation of complement enzyme activity.)

Cat. No.	Product Name	Target	Research Area

HY-P990091

Riliprubart SAR 445088	Complement System	Inflammation/Immunology
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .

HY-P9914

Eculizumab Anti-Human C5, Humanized Antibody	Complement System	Cardiovascular Disease
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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N9481

Lipoteichoic acid	Structural Classification Natural Products Microorganisms Classification of Application Fields Source classification Inflammation/Immunology Disease Research Fields	Complement System
Lipoteichoic acid, a cell wall component of Staphylococcus aureus, activates the complement system via C3 induction and CD55 inhibition .

HY-N2996

Ganodermanondiol	Infection Triterpenes Structural Classification Microorganisms Classification of Application Fields Terpenoids Polyporaceae Source classification Plants Disease Research Fields	HIV Protease
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum .Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC₅₀ of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC₅₀ of 41.7μM .

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