JNJ-55308942|cas:2166558-11-6|西域试剂

JNJ-55308942,99.95%

产品编号：Bellancom-123857| CAS NO：2166558-11-6| 分子式：C₁₇H₁₂F₅N₇O| 分子量：425.32

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	价格	库存与货期
Bellancom-123857	￥2500.00	杭州北京（现货）
Bellancom-123857	￥3800.00	杭州北京（现货）
Bellancom-123857	￥7500.00	杭州北京（现货）
Bellancom-123857	￥12000.00	杭州北京（现货）

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JNJ-55308942

产品介绍

JNJ-55308942 是一种高亲和力、选择性、可透过血脑屏障的 P2X7 功能拮抗剂 (hP2X7: IC₅₀=10 nM, K_i=7.1 nM; rP2X7: IC₅₀=15 nM, K_i=2.9 nM)。JNJ-55308942 口服生物利用度高，可与大脑 P2X7 结合并阻断 IL-1β 从成年啮齿动物脑中释放。

生物活性

JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC₅₀=10 nM, K_i=7.1 nM; rP2X7: IC₅₀=15 nM, K_i=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.

体外研究

JNJ-55308942 shows pK_is of 8.1and 8.5 for recombinant human and rat P2X7 channels, respectively. In human blood and in mouse blood and microglia, JNJ-55308942 attenuates IL-1β release in a potent and concentration-dependent manner.

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

体内研究

JNJ-55308942 (30 mg/kg; p.o.) attenuates LPS-induced microglial activation in mice.
In a model of Bacillus Calmette-Guerin (BCG)-induced depression, JNJ-55308942 dosed orally (30 mg/kg), reversed the BCG-induced deficits of sucrose preference and social interaction. After oral dosing, the compound exhibited both dose and concentration-dependent occupancy of rat brain P2X7 with an ED₅₀ of 0.07 mg/kg. The P2X7 antagonist (3 mg/kg, oral) blocked Bz-ATP-induced brain IL-1β release in conscious rats, demonstrating functional effects of target engagement in the brain.
JNJ-55308942 (5 mg/kg; p.o.) shows the F, V_ss, CL, C_max and AUC_24h values are 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.

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

Animal Model:	Sixteen male C57/BL6J mice
Dosage:	30 mg/kg
Administration:	P.o. (after an i.p. injection of LPS (0.8 mg/kg, i.p.))
Result:	Significantly attenuated the effect of LPS on FSC, CD45 surface expression and CD11b surface expression.

Animal Model:	Rat
Dosage:	P.o. (Pharmacokinetic Analysis)
Administration:	5 mg/kg
Result:	The F, V_ss, CL, C_max and AUC_{24h_{were 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.}}

体内研究

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

Animal Model:	Sixteen male C57/BL6J mice
Dosage:	30 mg/kg
Administration:	P.o. (after an i.p. injection of LPS (0.8 mg/kg, i.p.))
Result:	Significantly attenuated the effect of LPS on FSC, CD45 surface expression and CD11b surface expression.

Animal Model:	Rat
Dosage:	P.o. (Pharmacokinetic Analysis)
Administration:	5 mg/kg
Result:	The F, V_ss, CL, C_max and AUC_{24h_{were 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.}}

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (235.12 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3512 mL	11.7559 mL	23.5117 mL
5 mM	0.4702 mL	2.3512 mL	4.7023 mL
10 mM	0.2351 mL	1.1756 mL	2.3512 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 (sealed storage, away from moisture and light)。-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: ≥ 4 mg/mL (9.40 mM); Clear solution

此方案可获得 ≥ 4 mg/mL (9.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 40.0 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: ≥ 4 mg/mL (9.40 mM); Clear solution

此方案可获得 ≥ 4 mg/mL (9.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 40.0 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: ≥ 4 mg/mL (9.40 mM); Clear solution

此方案可获得 ≥ 4 mg/mL (9.40 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 40.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。