Pasireotide (SOM230) ditrifluoroacetate 是一种长效的环己肽生长激素抑制素类似物,可以提高生长抑素受体的激动剂活性,对sst1/2/3/4/5的pKi分别为 8.2/9.0/9.1/<7.0/9.9。Pasireotide ditrifluoroacetate 具有抗分泌、抗增殖和促凋亡活性。
生物活性 | Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity atsomatostatin receptors(subtypessst1/2/3/4/5,pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2]. |
IC50& Target | pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3),<7.0 (sst4), 9.9 (sst5)[1] |
体外研究 (In Vitro) | Pasireotide ditrifluoroacetate exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively)[1]. Pasireotide ditrifluoroacetate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC50of 0.4 nM[1].
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体内研究 (In Vivo) | Pasireotide ditrifluoroacetate (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis inPdx1-Cre[2]. Pasireotide ditrifluoroacetate (2-50 μg/kg; s.c. twice daily for 42 days) exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis[3].
Animal Model: | 12 month-old conditional Men1 knockout mice with insulinoma[2] | Dosage: | 160 mg/kg/mouth | Administration: | S.c. every month for 4 months | Result: | Decreased the serum insulin from 1.060 μg/L to 0.3653 μg/L and increased the serum glucose from 4.246 mM to 7.122 mM. Significantly reduced the tumor size and increased apoptosis. |
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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 : 100 mg/mL(78.42 mM;Need ultrasonic) H2O : 33.33 mg/mL(26.14 mM;Need ultrasonic) 配制储备液 1 mM | 0.7842 mL | 3.9208 mL | 7.8416 mL | 5 mM | 0.1568 mL | 0.7842 mL | 1.5683 mL | 10 mM | 0.0784 mL | 0.3921 mL | 0.7842 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.96 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 (1.96 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.96 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 (1.96 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.96 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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