LNP023
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- CAS号:
- 1644670-37-0
- 英文名:
- 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid
- 英文别名:
- LNP023;LNP0233;EOS-62416;LNP023(LNP-023;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]-
- 中文名:
- LNP023
- 中文别名:
- 伊帕替康;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
- CBNumber:
- CB23142721
- 分子式:
- C25H30N2O4
- 分子量:
- 422.52
- MOL File:
- 1644670-37-0.mol
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LNP023化学性质
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沸点:
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599.1±50.0 °C(Predicted)
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密度:
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1.25±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO:50.0(Max Conc. mg/mL);118.34(Max Conc. mM)
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酸度系数(pKa):
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4.07±0.10(Predicted)
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LNP023性质、用途与生产工艺
Iptacopan (LNP023) 是一种首创的，有效的，具有口服活性的高选择性的 factor B 抑制剂，IC50 值为 10 nM。Iptacopan 直接可逆且高亲和力结合 factor B，KD为 7.9 nM。Iptacopan 可靶向 C3 肾小球病的根本病因。
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).
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Animal Model:
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C57BL/6 mice with KRN-induced arthritis
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Dosage:
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20, 60, and 180 mg/kg
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Administration:
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Orally gavaged; twice a day (b.i.d.) for 14 days
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Result:
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Blocked KRN-induced arthritis.
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LNP023
上下游产品信息
上游原料
下游产品
1644670-37-0, LNP023 相关搜索:
- 黄金产品
- 医药原料
- 伊帕替康
- 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
- 化合物 T11864
- IPTACOPAN
- 1644670-37-0
- LNP0233
- LNP023(LNP-023
- Benzoic acid, 4-[(2S,4S)-4-ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]-
- LNP023
- EOS-62416
- 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid