Diclofenac 是一种有效的，非选择性抗炎剂，为COX的抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的IC50值分别为 4 和 1.3 nM。Diclofenac 对绵羊 COX-1 和 COX-2 的IC50值分别为 5.1 μM，0.84 μM。Diclofenac 通过活化 caspase 级联反应来诱导神经干细胞凋亡 (apoptosis)。
| 生物活性 | Diclofenac is a potent and nonselective anti-inflammatory agent, acts as aCOXinhibitor, withIC50s of 4 and 1.3 nM for humanCOX-1andCOX-2in CHO cells[1], and 5.1 and 0.84 μM for ovineCOX-1andCOX-2, respectively[2]. Diclofenac inducesapoptosisof neural stem cells (NSCs) via the activation of thecaspasecascade[3]. |
| IC50& Target[1][2] | Human COX-2 1.3 nM (IC50, in CHO cells) | Human COX-1 4 nM (IC50, in CHO cells) | Ovine COX-2 0.84 μM (IC50) | Ovine COX-1 5.1 μM (IC50) |
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体外研究
(In Vitro) | Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50of 7±3 nM[1].
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner[3].
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3[3].
Cell Viability Assay[3] | Cell Line: | Neural stem cells (NSCs) | | Concentration: | 1, 3, 10, 30, 60 μM | | Incubation Time: | 1 day | | Result: | Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM. |
Western Blot Analysis[3] | Cell Line: | Neural stem cells (NSCs) | | Concentration: | 10, 30 or 60 μM | | Incubation Time: | 6 hours | | Result: | The activation of caspase-3 was increased in a concentration-dependent manner. |
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体内研究
(In Vivo) | Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal51Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days[1].
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats[1].
| Animal Model: | Male Sprague-Dawley rats (150±200 g)[1] | | Dosage: | 3 mg/kg | | Administration: | Oral administration, b.i.d., for 5 days | | Result: | Resulted in a significant increase in faecal51Cr excretion. |
| Animal Model: | Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2] | | Dosage: | 10 mg/kg | | Administration: | Administered via oral route just prior to induction of inflammation | | Result: | Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h). |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(422.08 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.3767 mL | 16.8833 mL | 33.7667 mL | | 5 mM | 0.6753 mL | 3.3767 mL | 6.7533 mL | | 10 mM | 0.3377 mL | 1.6883 mL | 3.3767 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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；
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此方案可获得 ≥ 2.08 mg/mL (7.02 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.02 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本网站选购。
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