Iptacopan TFA
Based on 13 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- CAS No.: 1644670-38-1
- Formula: C27H31F3N2O6
- Molecular Weight:536.55
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Iptacopan TFA
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]
- Biomed Pharmacother. 2022 Sep:153:113433. [Abstract]
- Blood Adv. 2024 Jun 12:bloodadvances.2024012874. [Abstract]
- Kidney Int Rep. 2026 Mar 3;11(5):106413. [Abstract]
- J Biol Chem. 2024 Jun 12:107467. [Abstract]
- Biomed Chromatogr. 2024 Sep 3: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.
-
WB
-
Bio/Physico-chemical Assay
-
In Vivo Efficacy Study
-
In Vivo Imaging
-
In Vivo Efficacy Study
Biological Activity
Iptacopan (LNP023) TFA demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC50 value of 130 nM)[2].
Iptacopan (LNP023) TFA exhibits excellent selectivity over other proteases affording IC50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LNP023 TFA exhibits moderate half-lives (T1/2; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and Cmax (Wistar Han rats 410 nM, beagle dogs 2200 nM) following oral administration (rat 30 and, dog 10 mg/kg)[3].
Iptacopan TFA exhibits terminal elimination half-lives (T1/2; Wistar Han rats 7 h, beagle dogs 5.6 h) due to high plasma clearance (8, and 2 mL/min/kg respectively combined with large volumes of distribution (2.3, and 0.6 L/kg respectively) following intravenous administration (rat 1.0 and, dog 0.1 mg/kg)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1644670-38-1
-
Molecular Weight 536.55
-
Formula C27H31F3N2O6
-
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
-
Synonyms
LNP023 TFA
-
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 TFA 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 TFA 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 TFA 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 TFA 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 -
Biomed Pharmacother
2022 Sep:153:113433. PMID: 36076550
Iptacopan TFA 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.
-
Blood Adv
CG001, a C3b-targeted complement inhibitor blocks three complement pathways: development and preclinical evaluation. [Abstract]2024 Jun 12:bloodadvances.2024012874. 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 Jun 12:107467. 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 Sep 3: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 -
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)