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

Pasireotide  (Synonyms: 帕瑞肽; SOM230)

目錄號(hào): HY-16381 純度: 99.88%
COA 產(chǎn)品使用指南 技術(shù)支持

Pasireotide (SOM230) 是一種長效的環(huán)己肽生長激素抑制素類似物，可以提高生長抑素受體的激動(dòng)劑活性，對 sst1/2/3/4/5 的 pKi 分別為 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癥和庫欣病。Pasireotide 還具有抗分泌、抗增殖和促凋亡活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Custom Peptide Synthesis

Pasireotide Chemical Structure

Pasireotide Chemical Structure

CAS No. : 396091-73-9

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2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥1200
In-stock
5 mg ￥3000
In-stock
10 mg ￥4500
In-stock
50 mg   詢價(jià)  
100 mg   詢價(jià)  

* Please select Quantity before adding items.

Other Forms of Pasireotide:

    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 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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]
    體外研究
    (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.
    體內(nèi)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 號(hào)
    性狀

    固體

    顏色

    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]
    中文名稱

    帕瑞肽；帕西瑞肽
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    H2O 中的溶解度 : 20 mg/mL (19.10 mM; adjust pH to 5)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物溶解方案計(jì)算器
    請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請具體參考實(shí)測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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

    * 備注：如您選擇水作為儲(chǔ)備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    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.

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    產(chǎn)品名稱：
    Pasireotide
    目錄號(hào)：
    HY-16381
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