Dibutyryl-cGMP sodium (Bt2cGMP sodium) 是细胞可渗透的 cGMP 类似物,可优先激活 cGMP 依赖性蛋白激酶 (PKG)。Dibutyryl-cGMP sodium 抑制 γ 凝血酶刺激的人血小板中 [3H]-花生四烯酸的释放。Dibutyryl-cGMP sodium 可通过激活ATP 敏感的K+通道而具有缓解疼痛作用。
生物活性 | Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activatescGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation ofATP-sensitive K+channels[1][2][3]. |
IC50& Target | cGMP-dependent protein kinase (PKG)[1]; ATP-sensitive K+channels[3] |
体外研究 (In Vitro) | Dibutyryl-cGMP is able to induce process elongation and branching in astrocytes resulting from a rapid, reversible and concentration-dependent redistribution of glial fibrillary acidic protein (GFAP) and actin filaments without significant change in protein levels[1]. When cells are co-incubated with Dibutyryl-cGMP (100 μM) stress fibre formation is prevented and cells acquired a stellate morphology in cerebellar astrocytes[1]. In cells treated with Dibutyryl-cGMP (100 μM, 2 h) the particulate fraction is nearly devoid of RhoA protein. Dibutyryl-cGMP prevents RhoA-membrane association[1]. Using the scratchwound model, the size of the wound is significantly smaller in cells treated with Dibutyryl-cGMP after the wound indicating that dbcGMP accelerates wound closure[1].
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体内研究 (In Vivo) | Dibutyryl-cGMP (50-200 μg/paw; subcutaneous injection; male Wistar rats) treatment antagonizes the hyperalgesic effect of PGE2 in a dose-dependent manner. Maximal antinociceptive effect of DbcGMP is at 1 h after administration and last for plus 2 h[3].
Animal Model: | Male Wistar rats (180- 250 g) injection with Prostaglandin E2 (PGE2)[3] | Dosage: | 50 μg/paw, 75 μg/paw, 100 μg/paw and 200 μg/paw | Administration: | Subcutaneous injection | Result: | Antagonized the hyperalgesic effect of PGE2 (2 μg/paw), in a dose-dependent manner. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, stored under nitrogen, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(197.09 mM;Need ultrasonic) DMSO : 100 mg/mL(197.09 mM;Need ultrasonic) 配制储备液 1 mM | 1.9709 mL | 9.8547 mL | 19.7095 mL | 5 mM | 0.3942 mL | 1.9709 mL | 3.9419 mL | 10 mM | 0.1971 mL | 0.9855 mL | 1.9709 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℃, 6 months; -20℃, 1 month (stored under nitrogen, away from moisture)。-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;
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 (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 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-CDin saline) Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 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 μL20% 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 (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 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本网站选购。
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