Complement System Inhibitor

Avacopan-d₄ (CCX168-d₄) is the deuterium labeled Avacopan (HY-17627). Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC₅₀ of 0.1 nM.

Factor B-IN-6 is an orally active Factor B inhibitor. Factor B-IN-6 exhibits significant inhibitory activity against activation of the human serum serotonin pathway. Factor B-IN-6 can improve the severity of renal lesions and renal function, and reduce urinary protein in animal models. Factor B-IN-6 is useful for kidney disease research.

Pulchinenoside J is a lupane-type triterpenoid saponin and a complement system inhibitor that acts via the classical pathway. Pulchinenoside J can be isolated from the roots of Pulsatilla chinensis.

Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan TFA can be used in research of immune-mediated necrotising myopathy (IMNM).

TAT-327 is cell-penetrating peptide. TAT-327 selectively inserts into cancer cell membranes and shows potent antitumor activity. TAT-327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. TAT-327 significantly inhibits tumor growth in HT-29 xenograft mcie models.

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.

Factor B-IN-5 is an orally active complement factor B (CFB) inhibitor. Factor B-IN-5 alleviates kidney damage in diabetes nephropathy by inhibiting the over activation of complement system and improving mitochondrial function. Factor B-IN-5 can improve renal tubulointerstitial inflammation and fibrosis. Factor B-IN-5 can be used for research on diabetic nephropathy.

Iptacopan (LNP023) hydrochloride hydrate is an effective and orally-active highly selective factor B inhibitor with an IC₅₀ value of 10 nM and K_D of 7.9 nM. Iptacopan hydrochloride hydrate exerts a proximal effect in the complement cascade reaction, preventing the destruction (hemolysis) of red blood cells in PNH and the damage of renal cells in IgAN and C3G. Iptacopan hydrochloride hydrate can be used for the study of complement-mediated diseases, particularly paroxysmal nocturnal hemoglobinuria (PNH), primary immunoglobulin A nephropathy (IgAN), and complement 3 glomerulopathy (C3G).

C1s-IN-1 (compound A1) is a selective and competitive inhibitor of C1s. C1s-IN-1 binds directly to C1s with a K_d of 9.8 μM.

ASP-1948 is a human monoclonal antibody (mAb) targeting NRP1/VEGF165R/CD34. ASP-1948 reverses the suppressive effects of regulatory T cells. ASP-1948 can be used in solid tumors research.

Factor B-IN-8 (Compound (3R ,4R )-15) is a potent, selective and orally active factor B inhibitor with an IC₅₀ of 10.2 nM. Factor B-IN-8 can effectively inhibit the binding of factor B to C3b and the subsequent formation of C3 convertase (C3bBb). Factor B-IN-8 can inhibit the deposition of membrane attack complex (MAC) mediated by alternativepathway with an IC₅₀ of 59.3 nM. Factor B-IN-8 can reduce the cleavage of factor B protein and decrease the deposition of complement C3d in the glomeruli and renal tubules. Factor B-IN-8 can be used for researches of arthritis and paroxysmal nocturnal hemoglobinuria (PNH).

CP-EPS8-NLS is a peptide with anti-AML property. CP-EPS8-NLS interferes with EPS8-associated signaling and exerts anti-AML activity in various AML cell types. CP-EPS8-NLS has potent antitumor activity in xenograft tumor models. CP-EPS8-NLS downregulates EPS8 expression and its downstream pathway.

Refinicopan is a complement factor D inhibitor with an IC₅₀ of 10 nM. Refinicopan inhibits hemolysis of rabbit red blood cells. Refinicopan can be used to study diseases mediated by complement factor D.

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.

Agazisiran sodium scrambled negative control is the sequence scrambled negative control of Agazisiran sodium.

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.

GT103 is a human-derived monoclonal antibody targeting complement factor H (CFH). GT103 binds to a conformationally distinct epitope of CFH on tumor cells. GT103 activates the classical complement pathway, induces complement-dependent cytotoxicity, and triggers antibody-dependent cellular phagocytosis (ADCP) of tumor cells. GT103 increases calreticulin translocation to tumor cell plasma membranes. GT103 mediates B-cell activation via Syk kinase phosphorylation. GT103 inhibits tumor growth and metastasis in animal models. GT103 can be used for the research of non-small cell lung cancer.

Vensobafusp alfa (KP-104) is a fusion protein composed of an IgG4 monoclonal antibody directed against terminal complement protein C5 fused to the complement factor H 1-5 domain (FH1-5). Vensobafusp alfa shows anti-inflammatory and immunomodulatory activities. The isotype control for Vensobafusp alfa can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003)..

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.

Tubulin/NRP1-IN-1 (compound TN-2) is a dual inhibitor of Tubulin and NRP1 with IC₅₀s of 0.71 and 0.85 μM, respectively. Tubulin/NRP1-IN-1 significantly inhibits the viability of prostate tumor cell lines and induces apoptosis.