Pasireotide (diaspartate)
Based on 2 publication(s) in Google Scholar
Pasireotide (SOM230) diaspartate, 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 diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity.
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- No. CAS: 1421446-02-7
- Fòrmula: C66H80N12O17
- Peso molecular:1313.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Pasireotide (diaspartate)
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Actividad biológica
Descripciòn
IC50 & Target
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]
In Vitro
Pasireotide diaspartate 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 diaspartate 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pasireotide (2-50 μg/kg; s.c. twice daily for 42 days) diaspartate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:12 month-old conditional Men1 knockout mice with insulinoma[2]
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Dosage:160 mg/kg/mouth
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Administration:S.c. every month for 4 months
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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.
Chemical Information
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No. CAS 1421446-02-7
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Peso molecular 1313.41
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Fòrmula C66H80N12O17
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SMILES
NCCCC[C@@H](C(N[C@H]1CC2=CC=C(C=C2)OCC3=CC=CC=C3)=O)NC([C@H](NC([C@H](C4=CC=CC=C4)NC([C@H]5N(C([C@H](CC6=CC=CC=C6)NC1=O)=O)C[C@H](OC(NCCN)=O)C5)=O)=O)CC7=CNC8=C7C=CC=C8)=O.OC(C[C@H](N)C(O)=O)=O.OC(C[C@H](N)C(O)=O)=O
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Synonyms
SOM230 (diaspartate)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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J Clin Invest
Genomic and transcriptomic features of androgen receptor signaling inhibitor resistance in metastatic castration-resistant prostate cancer. [Abstract]2024 Aug 13;134(19):e178604. PMID: 39352383 -
Basic Clin Pharmacol Toxicol
Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. [Abstract]2022 Sep;131(3):174-188. PMID: 35688794
Pureza y Documentación
Referencias
[1]. Lewis I, et, al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem. 2003 Jun 5;46(12):2334-44. [Content Brief]
[2]. Quinn TJ, et, al. Pasireotide (SOM230) is effective for the treatment of pancreatic neuroendocrine tumors (PNETs) in a multiple endocrine neoplasia type 1 (MEN1) conditional knockout mouse model. Surgery. 2012 Dec;152(6):1068-77. [Content Brief]
[3]. Imhof AK, et, al. Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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