Lu AF27139|cas:2097117-06-9|西域试剂

Lu AF27139,99.69%

产品编号：Bellancom-132981| CAS NO：2097117-06-9| 分子式：C₂₁H₁₉ClF₃N₅O₂S| 分子量：497.92

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货号	价格	库存与货期
Bellancom-132981	￥2800.00	杭州北京（现货）
Bellancom-132981	￥4600.00	杭州北京（现货）
Bellancom-132981	￥9300.00	杭州北京（现货）
Bellancom-132981	￥14900.00	杭州北京（现货）

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Lu AF27139

产品介绍

Lu AF27139 是一种有效的、选择性的、具有口服活性的 P2X7 受体拮抗剂（IC₅₀s 值对人和大鼠分别为 12 和 2.4 nM，K_is 对小鼠、人和大鼠分别为 22、54 和 13 nM ）。Lu AF27139 具有啮齿动物活性和 CNS 渗透特性。Lu AF27139 具有研究中枢神经系统疾病的潜力。

生物活性

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC₅₀s of 12 and 2.4 nM for human and rat, K_is of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.

体外研究

Lu AF27139 (compound 1) (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC₅₀ of 66 nM.
Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose.
Lu AF27139 (compound 1) inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC₅₀ of 38 ± 2.5 nM.
Lu AF27139 (compound 1) concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice.

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

体内研究

Lu AF27139 (compound 1) (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.
Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat.

dose	C_{u, plasma} (nM)^a		C_{u, brain} (nM)^a		C_{u, spinal cord} (nM)^a
(mg/kg, po)	(1 h)	(2 h)	(1 h)	(2 h)	(1 h)	(2 h)
T₁	22.4 ± 4.2	22.8 ± 10	5.4 ± 2.6	6.4 ± 2.0	5.20 ± 0.80	10.0 ± 2.0

a: Free plasma, brain, and spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*f_u), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and f_u is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. f_u, plasma = 0.02 ± 0.00, f_u, spinal cord = 0.07 ± 0.03, and f_u, brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments.

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

Animal Model:	Male Sprague−Dawley rats (280−350 g); Male C57BL mice (18−25g)
Dosage:	3, 10, and 100 mg/kg
Administration:	p.o.
Result:	Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.

体内研究

dose	C_{u, plasma} (nM)^a		C_{u, brain} (nM)^a		C_{u, spinal cord} (nM)^a
(mg/kg, po)	(1 h)	(2 h)	(1 h)	(2 h)	(1 h)	(2 h)
T₁	22.4 ± 4.2	22.8 ± 10	5.4 ± 2.6	6.4 ± 2.0	5.20 ± 0.80	10.0 ± 2.0

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

Animal Model:	Male Sprague−Dawley rats (280−350 g); Male C57BL mice (18−25g)
Dosage:	3, 10, and 100 mg/kg
Administration:	p.o.
Result:	Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (251.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0084 mL	10.0418 mL	20.0835 mL
5 mM	0.4017 mL	2.0084 mL	4.0167 mL
10 mM	0.2008 mL	1.0042 mL	2.0084 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: ≥ 2.08 mg/mL (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。