| Identification | Back Directory | [Name]
4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid | [CAS]
1644670-37-0 | [Synonyms]
LNP023
EOS-62416
4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid
Benzoic acid, 4-[(2S,4S)-4-ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]- | [Molecular Formula]
C25H30N2O4 | [MDL Number]
MFCD32174282 | [MOL File]
1644670-37-0.mol | [Molecular Weight]
422.52 |
| Chemical Properties | Back Directory | [Boiling point ]
599.1±50.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);118.34(Max Conc. mM) | [form ]
Solid | [pka]
4.07±0.10(Predicted) | [color ]
Off-white to gray |
| Hazard Information | Back Directory | [Biological Activity]
Iptacopan (LNP023) is a first-in-class, potent, and orally active and highly selective factor B inhibitor with IC50 of 10 nM. Iptacopan binds factor B directly and reversibly with high affinity with a KD of 7.9 nM. Iptacopan targets the underlying cause of C3 glomerulopathy. | [in vitro]
Iptacopan (LNP023) demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC 50 value of 130 nM).
It exhibits excellent selectivity over other proteases affording IC 50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM) . | [in vivo]
Iptacopan (LNP023; 20-180 mg/kg; oral administration) 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. < br/> It exhibits moderate half-lives (T 1/2 ; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and C max (Wistar Han rats 410 nM, beagle dogs 2200 nM) following oral administration (rat 30 and, dog 10 mg/kg).
Iptacopan exhibits terminal elimination half-lives (T 1/2 ; 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 respectively) ). | Animal Model: | C57BL/6 mice with KRN-induced arthritis | | Dosage: | 20, 60, and 180 mg/kg | | Administration: | Orally gavaged; twice a day (bid) for 14 days | | Result: | Blocked KRN-induced arthritis. | | [target]
KD: 7.9 nM (factor B)
IC50: 10 nM (factor B) | [storage]
Store at -20°C |
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