LNP023
| 中文名称 | LNP023 |
|---|---|
| 中文同义词 | IPTACOPAN;化合物 T11864;4-((2S,4S)-4-乙氧基-1-((5-甲氧基-7-甲基-1H-吲哚-4-基)甲基)哌啶-2-基)苯甲酸;伊帕替康 |
| 英文名称 | 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid |
| 英文同义词 | 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid;EOS-62416;LNP023;Benzoic acid, 4-[(2S,4S)-4-ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]-;LNP023(LNP-023;LNP0233 |
| CAS号 | 1644670-37-0 |
| 分子式 | C25H30N2O4 |
| 分子量 | 422.52 |
| EINECS号 | |
| 相关类别 | 医药原料 |
| Mol文件 | 1644670-37-0.mol |
| 结构式 |  |
LNP023 性质
| 沸点 | 599.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.25±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：50.0（最大浓度 mg/mL）；118.34（最大浓度 mM） |
| 酸度系数(pKa) | 4.07±0.10(Predicted) |
KD: 7.9 nM (factor B)
IC50: 10 nM (factor B)
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).
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).
| Animal Model: | C57BL/6 mice with KRN-induced arthritis |
| Dosage: | 20, 60, and 180 mg/kg |
| Administration: | Orally gavaged; twice a day (b.i.d.) for 14 days |
| Result: | Blocked KRN-induced arthritis. |