Iptacopan hydrochloride hydrate
Based on 13 publication(s) in Google Scholar
Iptacopan (LNP023) hydrochloride hydrate 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 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).
For research use only. We do not sell to patients.
- CAS No.: 2447007-60-3
- Formula: C25H33ClN2O5
- Molecular Weight:476.99
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Iptacopan hydrochloride hydrate
More- Cell Stem Cell. 2023 Oct 5;30(10):1315-1330.e10. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Gut Microbes. 2025 Dec;17(1):2484386. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Jun 3;122(22):e2424570122. [Abstract]
- Blood Adv. 2024 Aug 13;8(15):4181-4193. [Abstract]
- Kidney Int Rep. 2026 Mar 3;11(5):106413. [Abstract]
- J Biol Chem. 2024 Jul;300(7):107467. [Abstract]
- Biomed Chromatogr. 2024 Nov;38(11):e6002. [Abstract]
- Biomed Chromatogr. 2021 Mar;35(3):e5006. [Abstract]
- medRxiv. 2026 Feb 2:2026.01.31.26345168. [Abstract]
- bioRxiv. 2026 Jan 1:2025.12.31.697141. [Abstract]
- State University of New York. 2025.
- Biomed Pharmacother. 2022 Sep:153:113433. [Abstract]
-
WB
-
Bio/Physico-chemical Assay
-
In Vivo Efficacy Study
-
In Vivo Imaging
-
In Vivo Efficacy Study
Biological Activity
Chemical Information
-
CAS No. 2447007-60-3
-
Molecular Weight 476.99
-
Formula C25H33ClN2O5
-
SMILES
CC(C=C1OC)=C(NC=C2)C2=C1CN3[C@H](C4=CC=C(C=C4)C(O)=O)C[C@H](CC3)OCC.Cl.O
-
Synonyms
LNP023 hydrochloride hydrate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (13)
-
Journal Impact Factor
-
Most Recent
-
Cell Stem Cell
Complement factor D targeting protects endotheliopathy in organoid and monkey models of COVID-19. [Abstract]2023 Oct 5;30(10):1315-1330.e10. PMID: 37802037
Iptacopan hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Oct 5;30(10):1315-1330.e10. [Abstract]
Relative quantification of blood perfusion area in human vessels after Iptacopan (LNP023, 25 mg/kg; p.o.; 1 h before extracellular domain (ECD) injection) and spike-ECD or sham (ECD+DMSO) treatment to before treatment (mean ± SE; n = 3; Welch’s t-test; **p < 0.01). The results showed that LNP023 effectively inhibited thrombus formation in an engineered human vascular model.
Iptacopan hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Oct 5;30(10):1315-1330.e10. [Abstract]
Intravital imaging of the organoid-transplanted mice treated with complement factor B inhibitor LNP023 and spike-ECD. Iptacopan (LNP023, 25 mg/kg; p.o) was orally administrated 1 hr before spike-ECD treatment. The organoid-derived human vascular and blood flow are visualized using a hCD31 and FITC-dextran, respectively.
-
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Gut Microbes
M28 family peptidase derived from Peribacillus frigoritolerans initiates trained immunity to prevent MRSA via the complosome-phosphatidylcholine axis. [Abstract]2025 Dec;17(1):2484386. PMID: 40159598
Iptacopan hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2484386. [Abstract]
Western blot analysis of HIF-1α protein expression in M28-trained macrophages 3 days after inhibition of CFB (Iptacopan, 10 µM) or C3aR (SB290157, 10 µM). Data were presented as means ± SEM.
Iptacopan hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2484386. [Abstract]
After pretreatment with the Iptacopan (CFB inhibitor) and SB290157 (C3aR inhibitor, 10 µM) for 24 hours, cells were treated with M28 (5 µg/mL) for an additional 24 hours. The cells were then washed twice with PBS to remove M28, and incubation was continued. 5 days later, macrophages were lysed to assess the phosphatidylcholine content. The results showed that, following treatment with the inhibitor, the phosphatidylcholine content within M28-trained macrophages decreased.
-
Proc Natl Acad Sci U S A
Host complement C3 promotes malaria transmission by killing symbiotic bacteria in the mosquito midgut. [Abstract]2025 Jun 3;122(22):e2424570122. PMID: 40434644 -
Blood Adv
CG001, a C3b-targeted complement inhibitor blocks three complement pathways: development and preclinical evaluation. [Abstract]2024 Aug 13;8(15):4181-4193. PMID: 38865712 -
Kidney Int Rep
Response to the Letter to the Editor Entitled "Defining "Dominance" in Atypical Hemolytic Uremic Syndrome: Distinguishing Amplification From Initiation". [Abstract]2026 Mar 3;11(5):106413. PMID: 41971459 -
J Biol Chem
Reconstitution of the alternative pathway of the complement system enables rapid delineation of the mechanism of action of novel inhibitors. [Abstract]2024 Jul;300(7):107467. PMID: 38876307 -
Biomed Chromatogr
Pharmacokinetic study of iptacopan and its two acyl glucuronide metabolites in monkey plasma by liquid chromatography combined with electrospray ionization tandem mass spectrometry. [Abstract]2024 Nov;38(11):e6002. PMID: 39228060 -
Biomed Chromatogr
Pharmacokinetics and metabolism of LNP023 in rats by liquid chromatography combined with electrospray ionization-tandem mass spectrometry. [Abstract]2021 Mar;35(3):e5006. PMID: 33067853 -
medRxiv
2026 Feb 2:2026.01.31.26345168. PMID: 41674601 -
bioRxiv
2026 Jan 1:2025.12.31.697141. PMID: 41509372 -
-
Biomed Pharmacother
2022 Sep:153:113433. PMID: 36076550
Iptacopan hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 Sep:153:113433. [Abstract]
Iptacopan (LNP023, 30 mg/kg; gavage; once daily for 2 weeks) alleviated skin lesions, alopecia, and splenomegaly, effectively improving the lupus-like signs in MRL/lpr mice.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)