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Iptacopan hydrochloride

CAS No. : 1646321-63-2

MCE 站：Iptacopan hydrochloride

产品活性：LNP023 hydrochloride 是一种有效的，具有口服活性的高选择性的 factor B 抑制剂。LNP023 直接可逆且高亲和力结合 factor B，K_D为 7.9 nM。LNP023 抑制 factor B 的 IC₅₀ 值为 10 nM。

研究领域：Immunology/Inflammation

作用靶点：Complement System

In Vitro: LNP023 demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC₅₀ value of 130 nM).
LNP023 exhibits excellent selectivity over other proteases affording IC₅₀ values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM).

In Vivo: 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).
LNP023 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).

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Dexamethasone  |  Cyclosporin A  |  SB290157 trifluoroacetate  |  EG00229  |  Iptacopan  |  Danicopan  |  PMX-53  |  PMX 205 Trifluoroacetate  |  ADH-503  |  AMY-101 acetate  |  BCX 1470 methanesulfonate  |  EG01377 dihydrochloride  |  ATWLPPR Peptide TFA  |  W-54011  |  Compstatin  |  Complement C5-IN-1  |  TLQP-21 TFA  |  C3a (70-77) (TFA)  |  FD-IN-1  |  JR14a  |  NDT 9513727  |  Complement factor D-IN-2

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