| Name | Iptacopan hydrochloride |
| Description | Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. |
| In vitro | LNP023 demonstrates 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]. |
| In vivo | LNP023 (20-180 mg/kg; oral administration) demonstrates efficacy in both prophylactic and therapeutic dosing in a rat model of membranous nephropathy and prevents KRN (150 μL)-induced arthritis in mice[2]. Following oral administration (rat 30 mg/kg, dog 10 mg/kg), 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)[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 50 mg/mL (108.94 mM), Sonication and heating are recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.89 mM), Sonication is recommended. DMSO : 252 mg/mL (549.04 mM), Sonication is recommended.
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| Keywords | uremic | system | syndrome | PNH | pathway | pathogenesis | paroxysmal | nocturnal | LNP-023 Hydrochloride | LNP023 Hydrochloride | LNP-023 | LNP023 | LNP 023 Hydrochloride | LNP 023 | Iptacopan hydrochloride | Iptacopan | Inhibitor | inhibit | hemolytic | hemoglobinuria | factor B | ComplementSystem | Complement System | complement | atypical | alternative |
| Inhibitors Related | EG01377 2HCl | Iptacopan | BCX 1470 hydrochloride | Complement C5-IN-1 | Avacopan | ADH-503 | CP-289 | Dexamethasone acetate | Dexamethasone | Cyclosporin A | Dextran sulfate sodium salt (MW 5000) | 3-Phenoxybenzaldehyde |
| Related Compound Libraries | Highly Selective Inhibitor Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |