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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : 50 mg/mL (108.94 mM), Sonication and heating are recommended. DMSO : 50 mg/mL (108.94 mM), Sonication is recommended.
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Keywords | LNP 023 | hemoglobinuria | inhibit | PNH | Iptacopan hydrochloride | atypical | pathogenesis | Inhibitor | LNP023 | factor B | system | LNP 023 Hydrochloride | Iptacopan | Complement System | complement | paroxysmal | syndrome | LNP-023 | pathway | LNP-023 Hydrochloride | hemolytic | uremic | alternative | LNP023 Hydrochloride | nocturnal | Iptacopan Hydrochloride |
Inhibitors Related | EG01377 2HCl | SB290157 trifluoroacetate | LEP(116-130)(mouse)TFA(258276-95-8 free base) | BCX 1470 hydrochloride | Complement C5-IN-1 | ADH-503 | CP-289 | Dexamethasone | CP-447697 | Complement factor D-IN-2 | Cyclosporin A | 3-Phenoxybenzaldehyde |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |