2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor
  4. Pasireotide

Pasireotide  (Synonyms: 帕瑞肽; SOM230)

目录号: HY-16381 纯度: 99.88%
COA 产品使用指南 技术支持

Pasireotide (SOM230) 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 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 还具有抗分泌、抗增殖和促凋亡活性。

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Custom Peptide Synthesis

Pasireotide

Pasireotide Chemical Structure

CAS No. : 396091-73-9

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2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
1 mg ￥1200
In-stock
5 mg ￥3000
In-stock
10 mg ￥4500
In-stock
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100 mg   询价  

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Pasireotide 相关抗体

Top Publications Citing Use of Products

    Pasireotide purchased from MCE. Usage Cited in: Am J Pathol. 2018 Apr;188(4):981-994.  [Abstract]

    Representative western blot and quantitation of band density show an increase expression of acetylated α-tubulin in PCK cholangiocytes upon ACY-1215 and ACY-1215+Pasireotide treatment.

    Pasireotide purchased from MCE. Usage Cited in: Hepatology. 2017 Oct;66(4):1197-1218.  [Abstract]

    Concurrent treatment of ADPKD cholangiocytes by SBI-115 and Pasireotide decreases cell proliferation, cholangiocyte spheroid growth, and cAMP levels.

    查看 Somatostatin Receptor 亚型特异性产品:

    查看所有亚型
    SSTR1 SSTR2 SSTR3 SSTR5 SSTR4

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide 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 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 effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC50 of 0.4 nM[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Pasireotide 相关抗体:
    体内研究
    (In Vivo)

    Pasireotide (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre[2].
    Pasireotide (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Clinical Trial
    分子量

    1047.21

    Formula

    C58H66N10O9
    CAS 号
    性状

    固体

    颜色

    White to off-white

    Sequence

    Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-Lys-{Tyr(4-Bzl)}-Phe]
    Sequence Shortening

    Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-K-{Tyr(4-Bzl)}-F]
    中文名称

    帕瑞肽；帕西瑞肽
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Sealed storage, away from moisture

    Powder -80°C 2 years
    -20°C 1 year

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 45.45 mg/mL (43.40 mM; adjust pH to 1 with 1 M HCl)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 0.9549 mL 4.7746 mL 9.5492 mL
    5 mM 0.1910 mL 0.9549 mL 1.9098 mL
    查看完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.88%

    COA (304 KB) LCMS (97 KB)

    产品使用指南 (1538 KB)
    参考文献

    Pasireotide 相关分类

    完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 0.9549 mL 4.7746 mL 9.5492 mL 23.8730 mL
    5 mM 0.1910 mL 0.9549 mL 1.9098 mL 4.7746 mL
    10 mM 0.0955 mL 0.4775 mL 0.9549 mL 2.3873 mL
    15 mM 0.0637 mL 0.3183 mL 0.6366 mL 1.5915 mL
    20 mM 0.0477 mL 0.2387 mL 0.4775 mL 1.1936 mL
    25 mM 0.0382 mL 0.1910 mL 0.3820 mL 0.9549 mL
    30 mM 0.0318 mL 0.1592 mL 0.3183 mL 0.7958 mL
    40 mM 0.0239 mL 0.1194 mL 0.2387 mL 0.5968 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Pasireotide396091-73-9SOM230帕瑞肽帕西瑞肽SOM 230SOM-230Somatostatin ReceptorSSTRsSSTRsomatostatinsst1sst2sst3sst4sst5antisecretoryantiproliferativeproapoptoticInhibitorinhibitorinhibit

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    目录号：
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