Pasireotide L-aspartate salt
Based on 6 publication(s) in Google Scholar
Pasireotide (SOM230) L-aspartate salt, 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 L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.
For research use only. We do not sell to patients.
- Purity: 97.0%
- CAS No.: 396091-77-3
- Formula: C62H73N11O13
- Molecular Weight:1180.31
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Pasireotide L-aspartate salt
More- Hepatology. 2017 Oct;66(4):1197-1218. [Abstract]
- J Clin Invest. 2024 Aug 13;134(19):e178604. [Abstract]
- Commun Med (Lond). 2022 Jul 1:2:80. [Abstract]
- Am J Pathol. 2018 Apr;188(4):981-994. [Abstract]
- Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188. [Abstract]
- Universidad De Salamanca. 2022 Oct.
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WB
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Cell Proliferation/Viability Assay
Biological Activity
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]
Pasireotide L-aspartate salt 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 L-aspartate salt 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.
Pasireotide L-aspartate salt (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].
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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CAS No. 396091-77-3
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Appearance Solid
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Molecular Weight 1180.31
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Formula C62H73N11O13
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Color Off-white to light yellow
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Synonyms
SOM230 L-aspartate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Hepatology
TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. [Abstract]2017 Oct;66(4):1197-1218. PMID: 28543567
Pasireotide L-aspartate salt purchased from MedChemExpress. Usage Cited in: Hepatology. 2017 Oct;66(4):1197-1218. [Abstract]
Concurrent treatment of ADPKD cholangiocytes by SBI-115 and Pasireotide decreases cell proliferation, cholangiocyte spheroid growth, and cAMP levels.
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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 -
Commun Med (Lond)
Patient-derived tumor organoids for personalized medicine in a patient with rare hepatocellular carcinoma with neuroendocrine differentiation: a case report. [Abstract]2022 Jul 1:2:80. PMID: 35789568 -
Am J Pathol
Combination of a Histone Deacetylase 6 Inhibitor and a Somatostatin Receptor Agonist Synergistically Reduces Hepatorenal Cystogenesis in an Animal Model of Polycystic Liver Disease. [Abstract]2018 Apr;188(4):981-994. PMID: 29366679
Pasireotide L-aspartate salt purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2018 Apr;188(4):981-994. [Abstract]
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.
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Basic Clin Pharmacol Toxicol
Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. [Abstract]2022 Sep;131(3):174-188. PMID: 35688794 -
Solvent & Solubility
DMSO : 1 mg/mL (0.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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)