| Field | Specification |
|---|---|
| Alternative names | SOM230 pamoate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C81H82N10O15 |
| Purity | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Pasireotide pamoate, also known as SOM230 pamoate, is a long-acting cyclohexapeptide somatostatin analogue that can improve agonist activity at somatostatin receptor subtypes sst1/2/3/4/5 (pKi values of 8.2, 9.0, 9.1, less than 7.0, and 9.9, respectively). It shows antisecretory, antiproliferative, and proapoptotic activity[1][2]. It is supplied as a white to off-white solid (C81H82N10O15, MW 1435.58) at 99.47% purity.
Physical & Chemical Properties
| CAS Number | 396091-79-5 |
|---|---|
| Molecular Formula | C81H82N10O15 |
| Molecular Weight | 1435.58 g/mol |
| Purity | 99.47% |
| Appearance | Solid |
| Color | White to off-white |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 100 mg/mL (69.66 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| 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). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (69.66 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
Pasireotide pamoate binds human somatostatin receptors with unique high affinity (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively)[1]. In primary cultures of rat pituitary cells, Pasireotide pamoate effectively inhibits growth hormone releasing hormone (GHRH) induced growth hormone (GH) release, with an IC50 of 0.4 nM[1].
In Vivo
Pasireotide pamoate (160 mg/kg/mouth; s.c. for 4 months) significantly lowers serum insulin, raises serum glucose, reduces tumor size, and increases apoptosis in Pdx1-Cre[2]. In a mouse model of immune-mediated arthritis, Pasireotide pamoate (2-50 μg/kg; s.c. twice daily for 42 days) exerts antinociceptive and antiinflammatory actions via the SSTR2 receptor[3].
| Animal Model | 12 month-old conditional Men1 knockout mice with insulinoma[2] |
|---|---|
| Dosage | 160 mg/kg/mouth |
| Administration | S.c. every month for 4 months |
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. Hepatology 2017 Oct;66(4):1197-1218.
Genomic and transcriptomic features of androgen receptor signaling inhibitor resistance in metastatic castration-resistant prostate cancer. J Clin Invest 2024 Aug 13;134(19):e178604. PMID: 39352383
Patient-derived tumor organoids for personalized medicine in a patient with rare hepatocellular carcinoma with neuroendocrine differentiation: a case report. Commun Med (Lond) 2022 Jul 1:2:80. PMID: 35789568
Combination of a Histone Deacetylase 6 Inhibitor and a Somatostatin Receptor Agonist Synergistically Reduces Hepatorenal Cystogenesis in an Animal Model of Polycystic Liver Disease. Am J Pathol 2018 Apr;188(4):981-994.
Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. Basic Clin Pharmacol Toxicol 2022 Sep;131(3):174-188. PMID: 35688794
Universidad De Salamanca. 2022 Oct.
