Pasireotide (SOM230) acetate 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 acetate 可以抑制 GH、IGF-I 和 ACTH 的分泌，可用于研究肢端肥大症和库欣病。Pasireotide acetate 还具有抗分泌、抗增殖和促凋亡活性。
| 生物活性 | Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2][3]. |
| 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 acetate 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 acetate 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 acetate (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 acetate (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[4].
| 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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| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| Sequence Shortening | Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-K-{Tyr(4-Bzl)}-F] |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture and light, under nitrogen | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(90.31 mM;Need ultrasonic) H2O : 1 mg/mL(0.90 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 0.9031 mL | 4.5157 mL | 9.0313 mL | | 5 mM | 0.1806 mL | 0.9031 mL | 1.8063 mL | | 10 mM | 0.0903 mL | 0.4516 mL | 0.9031 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 and light, under nitrogen)。-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 (2.26 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (2.26 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (2.26 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.26 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 (2.26 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.26 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。 4. 请依序添加每种溶剂： PBS Solubility: 2 mg/mL (1.81 mM); Clear solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
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