JNJ4796 - CAS:2241664-16-2

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JNJ4796

目录号 : KM10269 CAS No. : 2241664-16-2 纯度 : 98%

Data Sheet 产品使用指南

JNJ4796 是具有口服活性的流感病毒融合性抑制剂，通过抑制血球凝集素 (HA) 介导的融合来中和甲型流感病毒。JNJ4796 和广泛中和抗体 (bnAbs) 的功能类似。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

JNJ4796 is an oral active fusion inhibitor of influenza virus, neutralizing influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs).

体外研究

Like bnAb CR6261, the mechanism of action of JNJ4796 is demonstrated to be based on inhibition of the pH-sensitive conformational change of HA that triggers fusion of the viral and endosomal membranes and release of the viral genome into the host cell.

体内研究

Oral administration of JNJ4796 protects mice from lethal challenge of 25 times the median lethal dose (LD₅₀) of H1N1 A/Puerto Rico/8/1934 virus. Doses of 50 and 10 mg/kg of JNJ4796 twice daily, initiated one day before challenge and continuing for 7 days, results in 100% survival at day 21 in comparison to the less potent compound JNJ8897 for which less than 50% survival is achieved.
Oral doses of JNJ4796 results in dose-dependent efficacy after a sublethal viral challenge (LD₉₀), with twice daily administration of 15 and 5 mg/kg of JNJ4796 giving rise to 100% survival.

Animal Model:	Female BALB/cAnNCrl mice intranasally infected with 2 × 25 μL of 25 × LD₅₀ or 1 × LD₉₀ of H1N1 A/Puerto Rico/8/34 dissolved in sterile phosphate buffered saline (D-PBS)
Dosage:	50 and 10 mg/kg.
Administration:	Oral twice daily for 7 days.
Result:	Resulted in 100% survival at day 21 in comparison to the less potent compound JNJ8897.

分子式

C₂₈H₂₇N₉O₃

分子量

537.57

CAS号

2241664-16-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (186.02 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8602 mL	9.3011 mL	18.6022 mL
5 mM	0.3720 mL	1.8602 mL	3.7204 mL
10 mM	0.1860 mL	0.9301 mL	1.8602 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: ≥ 2.5 mg/mL (4.65 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.65 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.65 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.65 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。