1. GPCR/G Protein
    Neuronal Signaling
  2. Somatostatin Receptor
  3. Pasireotide L-aspartate salt

Pasireotide L-aspartate salt (Synonyms: SOM230 L-aspartate)

Cat. No.: HY-79136 Purity: 99.44%
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).

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Pasireotide L-aspartate salt Chemical Structure

Pasireotide L-aspartate salt Chemical Structure

CAS No. : 396091-77-3

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1 mg USD 210 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 L-aspartate salt:

Top Publications Citing Use of Products

Publications Citing Use of MCE Pasireotide L-aspartate salt

    Pasireotide L-aspartate salt 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 L-aspartate salt 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

    1180.31

    Formula

    C₆₂H₇₃N₁₁O₁₃

    CAS No.

    396091-77-3

    SMILES

    N[[email protected]@H](CC(O)=O)C(O)=O.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 Vitro: 

    DMSO : 1 mg/mL (0.85 mM; Need ultrasonic)

    References

    Purity: 99.44%

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    Keywords:

    PasireotideSOM230SOM 230SOM-230Somatostatin ReceptorSSTRsSSTRInhibitorinhibitorinhibit

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    Pasireotide L-aspartate salt
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