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: 98.21%
Handling Instructions

Pasireotide (ditrifluoroacetate) is a stable cyclohexapeptide somatostatin mimic that 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).

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

Pasireotide ditrifluoroacetate Chemical Structure

Pasireotide ditrifluoroacetate Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1543 In-stock
Estimated Time of Arrival: December 31
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
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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

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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pasireotide (ditrifluoroacetate) is a stable cyclohexapeptide somatostatin mimic that 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).

    IC50 & Target

    pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)

    In Vitro

    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±0.1 nM[1].

    In Vivo

    Pasireotide potently suppressess GH secretion in rats. The ED50 values determined at 1 and 6 h after injection of pasireotide indicates its very long duration of action in vivo. In the rat, pasireotide strongly decreases IGF-1 plasma levels, with the efficacy being markedly enhanced compared with the effects elicited by SMS 201-995 after 7 days of treatment. Furthermore, in rats, dogs, and rhesus monkeys, pasireotide potently and dose-dependently decreases IGF-1 levels for prolonged periods of time without desensitization[1]. Pasireotide (160 mg/kg/month, s.c.) decreases serum insulin levels and increases serum glucose levels, reduces PNET tumor size, and demonstrates a reduction in tumor activity on PET/CT scan in Pdx1-Cre; Men1 floxed/floxed conditional knockout mice[2]. Pasireotide (50 μg/kg) inhibits arthritic joint swelling in a dose-dependent manner, strongly inhibits joint swelling during the acute phase of AIA. Pasireotide- and octreotide-treated mice show significantly increased mechanical thresholds on the inflamed side. Pasireotide potently decreases secondary hyperalgesia to mechanical and thermal stimuli. Mechanical thresholds in the pasireotide-treated mice are significantly higher than those in the saline-treated or octreotide-treated animals[3].

    Clinical Trial
    Molecular Weight

    1275.25

    Formula

    C₆₂H₆₈F₆N₁₀O₁₃

    SMILES

    O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.NCCCC[[email protected]@H](C(N[[email protected]]1CC2=CC=C(C=C2)OCC3=CC=CC=C3)=O)NC([[email protected]](NC([[email protected]](C4=CC=CC=C4)NC([[email protected]]5N(C([[email protected]](CC6=CC=CC=C6)NC1=O)=O)C[[email protected]](OC(NCCN)=O)C5)=O)=O)CC7=CNC8=C7C=CC=C8)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vivo:
    • 1.

      Pasireotide is dissolved in sterile water[4].

    References
    Animal Administration
    [1]

    Mice are anesthetized using halothane and then shaved on their flank for subcutaneous injection of either phosphate buffered saline (PBS) buffer or Pasireotide at a concentration of 160 mg/Kg/month (64 mg/mL) every month for 4 months. The mice underwent a 24-h fast prior to collecting whole blood via a retro-orbital bleeding technique weekly at pre- and post-treatments. Serum glucose is measured by enzymatic colorimetric assay using a GM7 Analyzer. Serum insulin is measured by enzyme-linked immunosorbent assay (ELISA) with the UltrasensitiveMouse Insulin ELISA kit according to the manufacturer’s instructions.

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

    References

    Purity: 98.21%

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    Keywords:

    Pasireotide ditrifluoroacetateSOM230 ditrifluoroacetatePasireotideSomatostatin ReceptorSSTRsSSTRInhibitorinhibitorinhibit

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    Product name:
    Pasireotide ditrifluoroacetate
    Cat. No.:
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