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

Pasireotide (Synonyms: SOM 230; SOM 320)

Cat. No.: HY-16381
Handling Instructions

Pasireotide(SOM 230) 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 Chemical Structure

Pasireotide Chemical Structure

CAS No. : 396091-73-9

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Top Publications Citing Use of Products

    Pasireotide 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 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(SOM 230) 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 value: 8.2/9.0/9.1/<7.0/9.9(pKi, sst1/2/3/4/5) [1] in vitro: SOM230 showed a lower potency of GH release inhibition (IC(50), 0.5 nM), compared with OCT (IC(50), 0.02 nM) and SRIF-14 (IC(50), 0.02 nM). A positive correlation was found between sst(2) but not sst(5) mRNA levels in the adenoma cells and the inhibitory potency of OCT on GH release in vivo and in vitro, and the effects of SOM230 and SRIF-14 in vitro [2]. In cultures of human fetal pituitary cells, SOM230 inhibited GH secretion by 42 +/- 9% (P = 0.002) but had no effect on TSH release. SOM230 inhibited GH release from GH-secreting adenoma cultures by 34 +/- 8% (P = 0.002), PRL by 35 +/- 4% from PRL-secreting adenomas (P = 0.01), and alpha-subunit secretion from nonfunctioning pituitary adenomas by 46 +/- 18% (P = 0.34) [3]. in vivo: On day 7, there was a decrease in serum insulin levels from 1.06 ± 0.28 μg/L to 0.37 ± 0.17 μg/L (P = .0128) and a significant increase in serum glucose from 4.2 ± 0.45 mmol/L to 7.12 ± 1.06 mmol/L (P = .0075) in the treatment group but no change in the control group [4]. In wild-type mice, both octreotide and pasireotide significantly attenuated knee joint swelling and histopathologic manifestations of arthritis to an extent comparable to that of dexamethasone. In SSTR2(-/-) mice, the antiinflammatory effects of both octreotide and pasireotide were completely abrogated [5].

    Clinical Trial
    Molecular Weight

    1047.21

    Formula

    C₅₈H₆₆N₁₀O₉

    CAS No.

    396091-73-9

    SMILES

    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

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    Room temperature in continental US; may vary elsewhere.

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

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    Keywords:

    PasireotideSOM 230SOM 320SOM230SOM-230SOM320SOM-320Somatostatin ReceptorSSTRsSSTRInhibitorinhibitorinhibit

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