LXE408,1799330-15-6

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LXE408

CAS No. : 1799330-15-6

MCE 国际站：LXE408

产品活性：LXE408 是一种口服有效的，非竞争性的，动素体选择性蛋白酶体 (proteasome) 抑制剂。LXE408 抑制 L. donovani 蛋白酶体 (IC₅₀=0.04 μM) 和 L. donovani (EC₅₀=0.04 μM)。LXE408 具有较弱的透过血脑屏障能力。LXE408 具有用于内脏利什曼病 (VL) 研究的潜力。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Proteasome  |  Parasite

In Vitro: LXE408 (compound 1) can occupy the pocket as a ternary complex with the proteasome. LXE408 shows no inhibition of the hERG channel (IC₅₀>30 μM) in a manual patch clamp assay. LXE408 has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice).

In Vivo: LXE408 (compound 1; 0.3-10 mg/kg; PO; twice daily for 8 days) potently reduces the parasite burden in the liver in a dose-dependent manner.
LXE408 (1, 3, 10, 20 mg/kg; p.o.; b.i.d.; for 10 days) effects robust healing of parasite-induced skin lesions at the base of the tail in BALB/c mice infected with L. major.
LXE408 (5 mg/kg IV and 20 mg/kg PO) has a T_1/2 of 3.3 hours for mouse. LXE408 (3 mg/kg IV and 10 mg/kg PO) has a T_1/2 of 3.8 hours, a CL of 2.1 mL/min•kg, and a V_ss of 0.53 L/kg for male Sprague-Dawley rat.
LXE408 (0.3 mg/kg IV and 1.0 mg/kg PO) has a T_1/2 of 3.8 hours for male beagle dog. LXE408 (0.3 mg/kg IV and 10 mg/kg PO) has a T_1/2 of 9.7 hours for male cynomolgus monkey.

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