Iptacopan, 补体因子 B 抑制剂

伊普塔科潘

Iptacopan

I655394-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

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)

Iptacopan（LNP023）是一种首创的口服生物利用型高活性、高选择性 B 因子抑制剂，IC 50 值为 10 nM。Iptacopan 与人 B 因子的结合是直接、可逆和高亲和性的，其 K D 值为 7.9 nM。Iptacopa

1644670-37-0(DMSO)

C25H30N2O4

422.52 g/mol

CCOC1CCN(C(C1)C2=CC=C(C=C2)C(=O)O)CC3=C(C=C(C4=C3C=CN4)C)OC

抑制剂

补体因子 B 抑制剂