Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC 50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a K D of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) 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). Iptacopan (LNP023) 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. LNP023 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 mice with KRN-induced arthritisDosage: 20, 60, and 180 mg/kg Administration: Orally gavaged; twice a day (b.i.d.) for 14 days Result: Blocked KRN-induced arthritis. IC50& Target:KD: 7.9 nM (factor B),IC50: 10 nM (factor B)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Iptacopan
CAS number：1644670-37-0(DMSO) molecular formula：C25H30N2O4
overview
compound introduction
Specs
| Chinese alias | 伊普塔科潘 | ||
| English alias | - | ||
| CAS number | 1644670-37-0(DMSO) | molecular formula | C25H30N2O4 |
| molecular weight | 422.52 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
