化合物LXE408 fumarate T39214L
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Product IntroductionBioactivity英文名: LXE408 fumarate描述: LXE408 fumarate 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
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Product Introduction
Bioactivity
英文名: LXE408 fumarate
描述: LXE408 fumarate 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 fumarate 抑制 L. donovani 蛋白酶体 (IC50=0.04 μM) 和 L. donovani (EC50=0.04 μM)。LXE408 fumarate 具有较弱的透过血脑屏障能力。LXE408 fumarate 具有用于内脏利什曼病 (VL) 研究的潜力。
体外活性: LXE408 fumarate occupy the pocket as a ternary complex with the proteasome. In a manual patch clamp assay, LXE408 fumarate shows no inhibition of the hERG channel (IC50>30 μM). LXE408 fumarate has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice)[1].
体内活性: LXE408 fumarate ( 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 fumarate (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 fumarate (5 mg/kg IV and 20 mg/kg PO) has a T1/2 of 3.3 hours for mouse. LXE408 fumarate (3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 3.8 hours, a CL of 2.1 mL/min•kg, and a Vss of 0.53 L/kg for male Sprague-Dawley rat. LXE408 fumarate (0.3 mg/kg IV and 1.0 mg/kg PO) has a T1/2 of 3.8 hours for male beagle dog. LXE408 fumarate (0.3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 9.7 hours for male cynomolgus monkey[1].
存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 5.6 mg/mL (10 mM)
关键字: LXE408 Fumarate | 1799330-15-6 Free base | LXE 408 Fumarate | 1799330-15-6 | LXE-408 Fumarate
相关产品: Proteasome-IN-1 | PD 151746 | Epoxomicin | Tomatine | KZR-504 | Alloxan monohydrate | Saxagliptin hydrate | Z-Leu-Leu-Tyr-COCHO | Gly-Pro-pNA hydrochloride | Aprotinin
相关库: Ubiquitination Compound Library
Bioactivity
英文名: LXE408 fumarate
描述: LXE408 fumarate 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 fumarate 抑制 L. donovani 蛋白酶体 (IC50=0.04 μM) 和 L. donovani (EC50=0.04 μM)。LXE408 fumarate 具有较弱的透过血脑屏障能力。LXE408 fumarate 具有用于内脏利什曼病 (VL) 研究的潜力。
体外活性: LXE408 fumarate occupy the pocket as a ternary complex with the proteasome. In a manual patch clamp assay, LXE408 fumarate shows no inhibition of the hERG channel (IC50>30 μM). LXE408 fumarate has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice)[1].
体内活性: LXE408 fumarate ( 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 fumarate (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 fumarate (5 mg/kg IV and 20 mg/kg PO) has a T1/2 of 3.3 hours for mouse. LXE408 fumarate (3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 3.8 hours, a CL of 2.1 mL/min•kg, and a Vss of 0.53 L/kg for male Sprague-Dawley rat. LXE408 fumarate (0.3 mg/kg IV and 1.0 mg/kg PO) has a T1/2 of 3.8 hours for male beagle dog. LXE408 fumarate (0.3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 9.7 hours for male cynomolgus monkey[1].
存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 5.6 mg/mL (10 mM)
关键字: LXE408 Fumarate | 1799330-15-6 Free base | LXE 408 Fumarate | 1799330-15-6 | LXE-408 Fumarate
相关产品: Proteasome-IN-1 | PD 151746 | Epoxomicin | Tomatine | KZR-504 | Alloxan monohydrate | Saxagliptin hydrate | Z-Leu-Leu-Tyr-COCHO | Gly-Pro-pNA hydrochloride | Aprotinin
相关库: Ubiquitination Compound Library
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