Iptacopan (hydrochloride)

Iptacopan (LNP023) hydrochloride 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 hydrochloride 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 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].

Product Specifications

CAS Number

[1646321-63-2]

Product Name Alternative

LNP023 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H315, H319

Target

Complement System

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/lnp023-hydrochloride.html

Purity

99.88

Solubility

DMSO : ≥ 100 mg/mL|H2O : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(O)C1=CC=C([C@H]2N(CC3=C(OC)C=C(C)C4=C3C=CN4)CC[C@H](OCC)C2)C=C1.[H]Cl

Molecular Formula

C25H31ClN2O4

Molecular Weight

458.98

Precautions

H315, H319

References & Citations

[1]Dimitrios C Mastellos, et al. Expanding Complement Therapeutics for the Treatment of Paroxysmal Nocturnal Hemoglobinuria. Semin Hematol. 2018 Jul;55 (3) :167-175.|[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.|[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.