Iptacopan hydrochloride
Based on 13 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1646321-63-2
- Formula: C25H31ClN2O4
- Molecular Weight:458.98
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Iptacopan hydrochloride
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.
Customer Validation & Images
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WB
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Imaging
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In Vivo Efficacy Study
Biological Activity
LNP023 demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC50 value of 130 nM)[2].
LNP023 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 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].
LNP023 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.
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Animal Model:C57BL/6 mice with KRN-induced arthritis[2]
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Dosage:20, 60, and 180 mg/kg
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Administration:Orally gavaged; twice a day (b.i.d.) for 14 days
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Result:Blocked KRN-induced arthritis.
Chemical Information
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CAS No. 1646321-63-2
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Appearance Solid
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Molecular Weight 458.98
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Formula C25H31ClN2O4
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Color Off-white to gray
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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
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Synonyms
LNP023 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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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 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 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.
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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 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 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.
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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 hydrochloride 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.
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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 -
Solvent & Solubility
DMSO : ≥ 100 mg/mL (217.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (108.94 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1787 mL | 10.8937 mL | 21.7874 mL | 54.4686 mL |
| 5 mM | 0.4357 mL | 2.1787 mL | 4.3575 mL | 10.8937 mL | |
| 10 mM | 0.2179 mL | 1.0894 mL | 2.1787 mL | 5.4469 mL | |
| 15 mM | 0.1452 mL | 0.7262 mL | 1.4525 mL | 3.6312 mL | |
| 20 mM | 0.1089 mL | 0.5447 mL | 1.0894 mL | 2.7234 mL | |
| 25 mM | 0.0871 mL | 0.4357 mL | 0.8715 mL | 2.1787 mL | |
| 30 mM | 0.0726 mL | 0.3631 mL | 0.7262 mL | 1.8156 mL | |
| 40 mM | 0.0545 mL | 0.2723 mL | 0.5447 mL | 1.3617 mL | |
| 50 mM | 0.0436 mL | 0.2179 mL | 0.4357 mL | 1.0894 mL | |
| 60 mM | 0.0363 mL | 0.1816 mL | 0.3631 mL | 0.9078 mL | |
| 80 mM | 0.0272 mL | 0.1362 mL | 0.2723 mL | 0.6809 mL | |
| 100 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5447 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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