SB-3CT 是一种有效竞争型的金属蛋白酶MMP-2和MMP-9抑制剂,Ki值分别为 13.9 nM、600 nM。SB-3CT 对明胶酶具有高选择性。SB-3CT 可透过血脑屏障,具有神经保护和抗癌作用。
生物活性 | SB-3CT is a potent and competitive matrix metalloproteinaseMMP-2andMMP-9inhibitor withKivalues of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity[1][2][3]. |
IC50& Target[1] | MMP-2 13.9 nM (Ki) | MMP-9 600 nM (Ki) |
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体外研究 (In Vitro) | SB-3CT has shown efficacy in an animal model of severe traumatic brain injury (TBI). SB-3CT inhibits MMP-9 with an inhibition constant Kiof 400±15 nM[1]. Inhibition of PC3 tumor growth by SB-3CT could also be a direct consequence of reduced extracellular matrix degradation within the bone tissue by the tumor cells themselves and/or by osteoclasts. Indeed, SB-3CT treatment is associated with a reduced osteolytic response, indicating that SB-3CT helps to preserve bone integrity[3].
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体内研究 (In Vivo) | SB-3CT (i.p.; 50 mg/kg; every other day; five weeks) inhibits intraosseous growth of human PC3 cells within the marrow of human fetal femur fragments previously implanted in SCID mice[3].
Animal Model: | Five-week-old male C.B.-17.SCID mice[3] | Dosage: | 50 mg/kg | Administration: | IP; every other day; five weeks | Result: | Inhibited intraosseous growth of human PC3 cells within the marrow of human fetal femur fragments previously implanted in SCID mice. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(163.19 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 3.2637 mL | 16.3185 mL | 32.6371 mL | 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 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 (sealed storage, 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 20% Cremophor EL 70% ddH2O Solubility: 5 mg/mL (16.32 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (8.16 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.16 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.16 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。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.16 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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