RWJ-67657 JNJ 3026582|cas:215303-72-3|西域试剂

RWJ-67657 JNJ 3026582,99.32%

产品编号：Bellancom-15505| CAS NO：215303-72-3| 分子式：C₂₇H₂₄FN₃O| 分子量：425.50

RWJ 67657 (JNJ 3026582) 是一种具有口服活性的选择性 p38α 和 p38β 抑制剂，IC50 分别为 1 和 11 μM。RWJ 67657 对 p38γ 和 p38δ 无活性，是心脏保护剂，具有抗炎和抗肿瘤活性。

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货号	价格	库存与货期
Bellancom-15505	￥800.00	杭州北京（现货）
Bellancom-15505	￥1280.00	杭州北京（现货）
Bellancom-15505	￥2800.00	杭州北京（现货）
Bellancom-15505	￥4480.00	杭州北京（现货）
Bellancom-15505	￥7150.00	杭州北京（现货）

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RWJ-67657 JNJ 3026582

产品介绍

RWJ-67657 (JNJ 3026582) 是一种具有口服活性的选择性 p38α 和 p38β 抑制剂，IC₅₀ 分别为 1 和 11 μM。RWJ-67657 对 p38γ 和 p38δ 无活性，是心脏保护剂，具有抗炎和抗肿瘤活性。

生物活性

RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC₅₀s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.

体外研究

RWJ-67657 inhibits the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells with an IC₅₀ of 3 nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B, with an IC₅₀ value of 13 nM.
RWJ67657 (10 μM; 24 hours) decreases colony formation in MCF-7 cells.

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

Cell Proliferation Assay

Cell Line:	MCF-7 breast carcinoma cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Decreased colony formation.

体内研究
(In Vivo)

RWJ-67657 inhibits TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration.
RWJ-67657 (50 mg/kg; administered orally; once per day for 7 consecutive days) displays a potent anti-inflammatory effect. By both improving the functioning of endothelial progenitor cells (EPCs) and reducing inflammation, EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke^[4].

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

Animal Model:	The db/db mice (male, 8 weeks old) with EPCs^[4]
Dosage:	50 mg/kg
Administration:	Administered orally; once per day for 7 consecutive days
Result:	Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.

体内研究

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

Animal Model:	The db/db mice (male, 8 weeks old) with EPCs^[4]
Dosage:	50 mg/kg
Administration:	Administered orally; once per day for 7 consecutive days
Result:	Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.

体内研究

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

Animal Model:	The db/db mice (male, 8 weeks old) with EPCs^[4]
Dosage:	50 mg/kg
Administration:	Administered orally; once per day for 7 consecutive days
Result:	Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (293.77 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	2.3502 mL	11.7509 mL	23.5018 mL
5 mM	0.4700 mL	2.3502 mL	4.7004 mL
10 mM	0.2350 mL	1.1751 mL	2.3502 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 (4.89 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.89 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 (4.89 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.89 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 (4.89 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.89 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。

*以上所有助溶剂都可在西域网站选购。

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

参考文献

. Shahin R, et al. Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment. Future Sci OA. 2017 Aug 8;3(4):FSO204. [Content Brief]

. Wadsworth SA, et al. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J Pharmacol Exp Ther. 1999 Nov;291(2):680-7. [Content Brief]

. Frigo DE, et al. p38 mitogen-activated protein kinase stimulates estrogen-mediated transcription and proliferation through the phosphorylation and potentiation of the p160 coactivator glucocorticoid receptor-interacting protein 1. Mol Endocrinol. 2006 Ma [Content Brief]

[4]. Bai YY, et al. Synergistic Effects of Transplanted Endothelial Progenitor Cells and RWJ 67657 in Diabetic Ischemic Stroke Models. Stroke. 2015 Jul;46(7):1938-46. [Content Brief]

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RWJ-67657 JNJ 3026582,99.32%

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