LXE408|cas:1799330-15-6|西域试剂

LXE408,99.08%

产品编号：Bellancom-131350| CAS NO：1799330-15-6| 分子式：C₂₃H₁₈FN₇O₂| 分子量：443.43

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-131350		￥6900.00	杭州北京（现货）
Bellancom-131350		￥11500.00	杭州北京（现货）

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LXE408

产品介绍

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。

生物活性

LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC₅₀ of 0.04 μM for L. donovani proteasome and an EC₅₀ of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research.

体外研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (6-8 weeks old) infected with L. donovani
Dosage:	0.3, 1, 3, 10 mg/kg
Administration:	PO; twice daily for 8 days
Result:	Led to a 95% and >99.84% reduction of parasite burden in the liver at 1 mg/kg and 10 mg/kg.

Animal Model:	Balb/C mice
Dosage:	5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 3.3 hours, a CL of 2.3 mL/min•kg, and a V_ss of 0.63 L/kg for mouse.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (6-8 weeks old) infected with L. donovani
Dosage:	0.3, 1, 3, 10 mg/kg
Administration:	PO; twice daily for 8 days
Result:	Led to a 95% and >99.84% reduction of parasite burden in the liver at 1 mg/kg and 10 mg/kg.

Animal Model:	Balb/C mice
Dosage:	5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 3.3 hours, a CL of 2.3 mL/min•kg, and a V_ss of 0.63 L/kg for mouse.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (37.59 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2551 mL	11.2757 mL	22.5515 mL
5 mM	0.4510 mL	2.2551 mL	4.5103 mL
10 mM	0.2255 mL	1.1276 mL	2.2551 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.62 mg/mL (1.40 mM); Clear solution

此方案可获得 ≥ 0.62 mg/mL (1.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.62 mg/mL (1.40 mM); Clear solution

此方案可获得 ≥ 0.62 mg/mL (1.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.62 mg/mL (1.40 mM); Clear solution

此方案可获得 ≥ 0.62 mg/mL (1.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。