Pasireotide (aspartate) (TFA)

Pasireotide (aspartate) TFA, 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/proapoptotic activity[1][2][3][4].

Product Specifications

Product Name Alternative

SOM230 (aspartate) (TFA)

UNSPSC

12352005

Target

Apoptosis; Somatostatin Receptor

Related Pathways

Apoptosis; GPCR/G Protein; Neuronal Signaling

Field of Research

Metabolic Disease

Smiles

O=C(N1[C@]([H])(C(N[C@@H](C(N[C@@H](C(N[C@H](C(N[C@H]2CC3=CC=C(C=C3)OCC4=CC=CC=C4)=O)CCCCN)=O)CC5=CNC6=C5C=CC=C6)=O)C7=CC=CC=C7)=O)C[C@H](C1)OC(NCCN)=O)[C@@H](NC2=O)CC8=CC=CC=C8.OC(C[C@@H](C(O)=O)N)=O.OC(C[C@@H](C(O)=O)N)=O.FC(C(O)=O)(F)F.[F,Cl,Br,I]

Molecular Formula

C66H80N12O17.XCF3COOH

Molecular Weight

1313.4 (free base)

References & Citations

[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. |[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.|[3]chmid HA, et, al. Pasireotide (SOM230) : development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008 May 14;286 (1-2) :69-74. |[4] 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.