Pasireotide pamoate
Based on 6 publication(s) in Google Scholar
Pasireotide (SOM230) pamoate, 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 pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
For research use only. We do not sell to patients.
- Purity: 99.47%
- CAS No.: 396091-79-5
- Formula: C81H82N10O15
- Molecular Weight:1435.58
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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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pasireotide pamoate
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.
Customer Validation & Images
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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 pamoate 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 pamoate 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 pamoate (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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 396091-79-5
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Appearance Solid
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Molecular Weight 1435.58
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Formula C81H82N10O15
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Color White to off-white
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Synonyms
SOM230 pamoate
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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 pamoate 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 pamoate 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 : 100 mg/mL (69.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.6966 mL | 3.4829 mL | 6.9658 mL | 17.4146 mL |
| 5 mM | 0.1393 mL | 0.6966 mL | 1.3932 mL | 3.4829 mL | |
| 10 mM | 0.0697 mL | 0.3483 mL | 0.6966 mL | 1.7415 mL | |
| 15 mM | 0.0464 mL | 0.2322 mL | 0.4644 mL | 1.1610 mL | |
| 20 mM | 0.0348 mL | 0.1741 mL | 0.3483 mL | 0.8707 mL | |
| 25 mM | 0.0279 mL | 0.1393 mL | 0.2786 mL | 0.6966 mL | |
| 30 mM | 0.0232 mL | 0.1161 mL | 0.2322 mL | 0.5805 mL | |
| 40 mM | 0.0174 mL | 0.0871 mL | 0.1741 mL | 0.4354 mL | |
| 50 mM | 0.0139 mL | 0.0697 mL | 0.1393 mL | 0.3483 mL | |
| 60 mM | 0.0116 mL | 0.0580 mL | 0.1161 mL | 0.2902 mL |
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