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產品名稱: 1646321-63-2
產品型號:
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簡單介紹
1646321-63-2，LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.
1646321-63-2
的詳細介紹
1646321-63-2，LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.
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別名
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化合物LNP023 hydrochloride , Iptacopan HCl , LNP023 hydrochloride ,
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純度
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99.84%
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分子量
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458.98
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分子式
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C25H31ClN2O4
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CAS No.
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1646321-63-2
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產品描述
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LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.
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體外活性
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LNP023 demonstrates 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)[3].
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體內活性
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LNP023 (20-180 mg/kg; oral administration) is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats and prevents KRN (150 μL)-induced arthritis in mice[2]. After oral administration (rat 30 and, dog 10 mg/kg), LNP023 exhibits moderate half-lives (T1/2; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and Cmax (Wistar Han rats 410 nM, beagle dogs 2200 nM)[3].
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