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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Complement System-LNP023
LNP023

Chemical Structure : LNP023

CAS No.: 1644670-37-0

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LNP023 (Iptacopan, LNP-023, LNP 023)

货号: PC-36148Not For Human Use, Lab Use Only.

Iptacopan (LNP023) is a highly potent, reversible, selective inhibitor of factor B (IC50=10 nM), the proteolytically active component of the C3 and C5 convertases.

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5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Iptacopan (LNP023) is a highly potent, reversible, selective inhibitor of factor B (IC50=10 nM), the proteolytically active component of the C3 and C5 convertases.
Iptacopan (LNP023) shows direct, reversible, and high-affinity binding to human FB with Kd of 7.9 nM in SPR assays, demonstrates potent inhibition of AP-induced MAC formation in 50% human serum with IC50 of 0.13 uM.
Iptacopan (LNP023) shows no inhibition of factor D (FD), as well as classical or lectin complement pathway activation (up to 100 uM), and no significant effects (up to 10 μM) in a broad assay panel of receptors, ion channels, kinases, and proteases.
Iptacopan (LNP023) blocks zymosan-induced MAC formation membrane attack complex (MAC) with IC50 of 0.15 uM, prevents KRN-induced arthritis in mice and is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats afer oral adminstration.
Iptacopan (LNP023) also prevents complement activation in sera from C3 glomerulopathy patients and the hemolysis of human PNH erythrocytes.

物理化学性质&存储条件

分子量 422.525
分子式 C25H30N2O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic acid

参考文献

1. Schubart A, et al. Proc Natl Acad Sci U S A. 2019 Mar 29. pii: 201820892.

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