| Field | Specification |
|---|---|
| Alternative names | SOM230 (diaspartate) |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C66H80N12O17 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Pasireotide (diaspartate), also known as SOM230 (diaspartate), is a long-acting cyclohexapeptide somatostatin analogue with agonist activity at somatostatin receptor subtypes sst1, sst2, sst3, sst4, and sst5 (pKi 8.2, 9.0, 9.1, <7.0, and 9.9, respectively). It shows antisecretory, antiproliferative, and proapoptotic activity[1][2]. Its molecular formula is C66H80N12O17, with a molecular weight of 1313.41 g/mol.
Physical & Chemical Properties
| CAS Number | 1421446-02-7 |
|---|---|
| Molecular Formula | C66H80N12O17 |
| Molecular Weight | 1313.41 g/mol |
| 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 |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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 your institution's chemical hygiene plan.
In Vitro
Pasireotide diaspartate 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]. Pasireotide diaspartate effectively blocks GHRH (growth hormone releasing hormone)-induced release of growth hormone (GH) in primary rat pituitary cell cultures (IC50 of 0.4 nM)[1].
In Vivo
Pasireotide (160 mg/kg/mouth; s.c. for 4 months) diaspartate significantly lowers serum insulin, raises serum glucose, shrinks tumor size and increases apoptosis in Pdx1-Cre[2]. In a mouse model of immune-mediated arthritis, Pasireotide (2-50 μg/kg; s.c. twice daily for 42 days) diaspartate exerts antinociceptive and antiinflammatory actions through 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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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
Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. Basic Clin Pharmacol Toxicol 2022 Sep;131(3):174-188. PMID: 35688794
