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

Pasireotide pamoate (Synonyms: SOM230 pamoate)

Cat. No.: HY-108768
Handling Instructions

Pasireotide (SOM230) pamoate, 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 pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

For research use only. We do not sell to patients.

Pasireotide pamoate Chemical Structure

Pasireotide pamoate Chemical Structure

CAS No. : 396091-79-5

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Top Publications Citing Use of Products

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

    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 pamoate purchased from MCE. Usage Cited in: Hepatology. 2017 Oct;66(4):1197-1218.

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

    Pasireotide (SOM230) pamoate, 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 pamoate 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]

    In Vitro

    Pasireotide pamoate 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 pamoate 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.

    In Vivo

    Pasireotide pamoate (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 pamoate (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].

    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
    Molecular Weight

    1435.58

    Formula

    C₈₁H₈₂N₁₀O₁₅

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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