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

Pasireotide ditrifluoroacetate (Synonyms: SOM230 ditrifluoroacetate; Pasireotide TFA salt)

Cat. No.: HY-79135 Purity: 99.27%
Handling Instructions

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

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

Pasireotide ditrifluoroacetate Chemical Structure

Pasireotide ditrifluoroacetate Chemical Structure

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 1543 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 1543 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 210 In-stock
Estimated Time of Arrival: December 31
5 mg USD 690 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Pasireotide ditrifluoroacetate:

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Pasireotide ditrifluoroacetate

    Pasireotide ditrifluoroacetate 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 ditrifluoroacetate 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.
    • Biological Activity

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    • References

    • Customer Review

    Description

    Pasireotide (SOM230) ditrifluoroacetate, 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 ditrifluoroacetate 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 ditrifluoroacetate 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 ditrifluoroacetate 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 ditrifluoroacetate (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 ditrifluoroacetate (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

    1275.25

    Formula

    C₆₂H₆₈F₆N₁₀O₁₃

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (78.42 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.7842 mL 3.9208 mL 7.8416 mL
    5 mM 0.1568 mL 0.7842 mL 1.5683 mL
    10 mM 0.0784 mL 0.3921 mL 0.7842 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.27%

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    Product Name:
    Pasireotide ditrifluoroacetate
    Cat. No.:
    HY-79135
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