R-7050(Synonyms: TNF-α Antagonist III)

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R-7050 (Synonyms: TNF-α Antagonist III) 纯度: 99.26%

R-7050 (TNF-α Antagonist III) 是一种肿瘤坏死因子受体 (TNFR) 拮抗剂,对 TNFα 具有更高选择性。

R-7050(Synonyms: TNF-α Antagonist III)

R-7050 Chemical Structure

CAS No. : 303997-35-5

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥847 In-stock
5 mg ¥770 In-stock
10 mg ¥1350 In-stock
25 mg ¥2700 In-stock
50 mg ¥4700 In-stock
100 mg ¥8200 In-stock
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500 mg   询价  

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R-7050 相关产品

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生物活性

R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

IC50 & Target[1]

TNFα

 

体外研究
(In Vitro)

R-7050 (TNF-α Antagonist III) is a potent and fully reversible hit with greater selectivity toward TNFα. In TNFα-induced intercellular adhesion molecule 1 (ICAM-1) expression, R-7050 inhibition potency (EC50=0.63 μM) is 2- to 3-fold greater than EC50 for IL-1β-induced ICAM-1 expression (EC50=1.45 2 μM). R-7050 inhibits phosphorylation of both the JNK pathway (MKK4, JNKs, and ATF2) and p38 pathway (MKK3/6, p38, and MAPKAP2)[1]. R-7050 is a cell-permeable triazoloquinoxaline compound that selectively inhibits TNF-α induced cellular signaling. Unlike biologic TNF inhibitors (e.g. Infliximab, Etanercept, Adalimumab) that directly bind TNF-α and function as decoy receptors, R-7050 does not affect binding of TNF-α to TNFR. In contrast, R-7050 selectively inhibits the association of TNFR with intracellular adaptor molecules (e.g. TRADD, RIP), limits receptor internalization, and prevents subsequent cellular responses after TNF-α binding[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

R-7050 (TNF-α Antagonist III) (6 mg/kg) reduces Evans blue extravasation to 28.7±5.9 μg and 30.3±1.9 μg Evans blue/g brain tissue when administered at 0.5 h or 2 h post-ICH, respectively (p<0.05 and p<0.01 vs ICH, respectively; not significantly different from sham). Brain water content, a measure of brain edema, increases from 75.6±0.3% in sham-operated mice to 81.5±0.5% at 24h post-ICH (p<0.05 vs. sham). 6, 12, or 18 mg/kg R-7050 reduces brain water content to 78.5±0.3%, 78.3±0.3%, or 79.3±0.5%, respectively (all treatments p<0.05 vs. ICH; treatments not significantly different from each other). Notably, mice treated with 18 mg/kg exhibit a reduction in general activity/locomotion. As is observed with Evans blue extravasation, R-7050 (6 mg/kg) significantly reduces brain water content after ICH. Administration of R-7050 at 0.5h or 2h post-ICH attenuates brain water content to levels observed in sham-operated mice (p<0.05 vs ICH, not significantly different from sham)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

380.77

Formula

C16H8ClF3N4S

CAS 号

303997-35-5

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 : 25 mg/mL (65.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6263 mL 13.1313 mL 26.2626 mL
5 mM 0.5253 mL 2.6263 mL 5.2525 mL
10 mM 0.2626 mL 1.3131 mL 2.6263 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 (6.57 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.57 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 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。

    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: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 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。

    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: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18.

    [2]. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6.

Animal Administration
[2]

Mice[2]
A mouse collagenase model of ICH is utilized. Briefly, male CD-1 mice (8-10 weeks old) are placed into a stereotactic frame and a 0.5 mm diameter burr hole is drilled over the parietal cortex, 2.2 mm lateral to the bregma. A 26-gauge Hamilton syringe, loaded with 0.04 U of bacterial type IV collagenase in 0.5 μL saline, is lowered 3 mm deep from the skull surface directly into the left striatum. The syringe is depressed at a rate of 450 nL/min and left in place for several minutes after the procedure to prevent solution reflux and excess diffusion. Sham animals undergo the same surgical procedure, except that saline is stereotactically injected rather than collagenase. After the syringe is removed, bone wax is used to close the burr hole, the incision is surgically stapled, and mice are kept warm until recovery of the righting reflex. R-7050 (6-18 mg/kg) is administered via intraperitoneal route at the time of injury or up to 2 h post-ICH[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18.

    [2]. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6.

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