1644670-38-1
Chemical Structure
Iptacopan TFA
Synonym(s): LNP023 TFA
- CAS No.: 1644670-38-1
- Formula:C27H31F3N2O6
- Molecular Weight:536.55
IUPAC Name: 2,2,2-trifluoroacetic acid compound with 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic acid (1:1)
InChIKey: FOZKTOHHKYHDGB-CQERKEQDSA-N
SMILES: C(C(O)=O)(F)(F)F.C(C1=C2C(=C(C)C=C1OC)NC=C2)N3[C@@H](C[C@@H](OCC)CC3)C4=CC=C(C(O)=O)C=C4
Biological Activity: Iptacopan (LNP023) TFA is an effective and orally-active highly selective factor B inhibitor with an IC50 value of 10 nM and KD of 7.9 nM. Iptacopan TFA 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 TFA 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)[1][2][3].
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Iptacopan TFA | Iptacopan (LNP023) TFA is an effective and orally-active highly selective factor B inhibitor with an IC50 value of 10 nM and KD of 7.9 nM. Iptacopan TFA 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 TFA 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). | |||||||||||||||||||||
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- [1]. Dimitrios C Mastellos, et al. Expanding Complement Therapeutics for the Treatment of Paroxysmal Nocturnal Hemoglobinuria. Semin Hematol. 2018 Jul;55(3):167-175. [Content Brief]
- [2]. Anna Schubart, et al. Small-molecule Factor B Inhibitor for the Treatment of Complement-Mediated Diseases. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. [Content Brief]
- [3]. Nello Mainolfi, et al. Discovery of 4-((2 S,4 S)-4-Ethoxy-1-((5-methoxy-7-methyl-1 H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases. J Med Chem. 2020 Jun 11;63(11):5697-5722. [Content Brief]
Keywords
