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Iptacopan (LNP023) hydrochloride is an orally bioavailable, highly potent and selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan (LNP023) shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. 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).
In vivo, LNP023 (20-180 mg/kg; oral) prevents KRN (150 μL)-induced arthritis in mice and is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats.
| Molecular Weight | 458.98 |
| Formula | C25H31ClN2O4 |
| CAS Number | 1646321-63-2 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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