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

Pasireotide (diaspartate)  (Synonyms: SOM230 (diaspartate))

目录号: HY-16381B
产品使用指南

摩尔计算器

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

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Pasireotide (diaspartate) Chemical Structure

Pasireotide (diaspartate) Chemical Structure

CAS No. : 1421446-02-7

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Pasireotide (diaspartate) 的其他形式现货产品:

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Other Forms of Pasireotide (diaspartate):

Pasireotide (diaspartate) 相关抗体

Top Publications Citing Use of Products

    Pasireotide (diaspartate) 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 (diaspartate) 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:

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    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) diaspartate, 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 diaspartate 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 diaspartate 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 diaspartate 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 (diaspartate) 相关抗体:
    体内研究
    (In Vivo)

    Pasireotide (160 mg/kg/mouth; s.c. for 4 months) diaspartate 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) diaspartate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis[3].

    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

    1313.41

    Formula

    C66H80N12O17
    CAS 号
    运输条件

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

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Pasireotide (diaspartate) 相关分类

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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    质量   浓度   体积   分子量 *
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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2
    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:

    Pasireotide (diaspartate)1421446-02-7SOM230 (diaspartate)Somatostatin ReceptorSSTRsSSTRsomatostatinsst1sst2sst3sst4sst5antisecretoryantiproliferativeproapoptoticInhibitorinhibitorinhibit

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    目录号：
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