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Synonyms: LNP023 hydrochloride, Iptacopan HCl

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $52 | In Stock | In Stock | |
| 2 mg | $74 | In Stock | In Stock | |
| 5 mg | $123 | In Stock | In Stock | |
| 10 mg | $206 | In Stock | In Stock | |
| 25 mg | $372 | In Stock | In Stock | |
| 50 mg | $621 | In Stock | In Stock | |
| 100 mg | $1,030 | In Stock | In Stock | |
| 200 mg | $1,390 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $123 | In Stock | In Stock |
| Description | Iptacopan hydrochloride (LNP023 hydrochloride) is a small-molecule inhibitor and a complement factor B inhibitor (IC50 = 10 nM, KD = 7.9 nM) with high selectivity, oral activity, and cell permeability, used for the treatment of complement-mediated diseases including paroxysmal nocturnal hemoglobinuria, IgA nephropathy, and C3 glomerulopathy. |
| Targets & IC50 | FB:7.9 nM (KD), FB:10 nM, Membrane aTT cellsack Complex (MAC):130 nM |
| In vitro | Methods: Different concentrations of Iptacopan hydrochloride were incubated with SPIO NWs, CLIO NWs, Onivyde, PLD, and mRNA LNPs at 37°C for 30 minutes, and C3 deposition and C5a release were detected. Results: Its IC₅₀ was in the low micromolar range, but showed insufficient inhibition against PLD, and the inhibitory effect exhibited donor-dependent variability. [1] Methods: In n144-1.pdf, Iptacopan hydrochloride was used as a complement factor B inhibitor. Different concentrations of the drug were incubated with human serum and various nanoparticles (SPIO NWs, mRNA LNPs, etc.) at 37°C for 30 minutes in vitro, and the inhibitory efficacy was evaluated by detecting C3 deposition and C5a release. Results: IC₅₀ was in the low micromolar range. [2] |
| In vivo | Methods: Mouse, rat, and Beagle dog models were used to validate the in vivo activity of Iptacopan hydrochloride. The drug premixed with SPIO NWs was administered by intravenous injection (0.63 mg/kg for mice, 0.21–0.99 mg/kg for rats, 0.43 mg/kg for dogs, dissolved in DMSO and mixed with nanoparticles), and detection was performed after single-dose administration. Results:Iptacopan hydrochloride significantly inhibited C3 opsonization, reduced granulocyte uptake, and improved locomotor activity in rats and alleviated blood pressure decline in dogs. [1] |
| Synonyms | LNP023 hydrochloride, Iptacopan HCl |
| Molecular Weight | 458.98 |
| Formula | C25H31ClN2O4 |
| Cas No. | 1646321-63-2 |
| Smiles | Cl.CCO[C@H]1CCN(Cc2c(OC)cc(C)c3[nH]ccc23)[C@@H](C1)c1ccc(cc1)C(O)=O |
| Relative Density. | no data available |
| Storage | Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 50 mg/mL (108.94 mM), Sonication and heating are recommended. DMSO: 252 mg/mL (549.04 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.89 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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