| Identification | Back Directory | [Name]
Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl], 4,4'-methylenebis[3-hydroxy-2-naphthalenecarboxylate] (1:1) | [CAS]
396091-79-5 | [Synonyms]
SOM230 pamoate
Pasireotide pamoate
Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl], 4,4'-methylenebis[3-hydroxy-2-naphthalenecarboxylate] (1:1) | [Molecular Formula]
C58H66N10O9.C23H16O6 | [MDL Number]
MFCD34469176 | [MOL File]
396091-79-5.mol | [Molecular Weight]
1435.6 |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
Pasireotide pamoate (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre[2].
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]. | 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.
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| [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. DOI:10.1021/jm021093t
[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. DOI:10.1016/j.surg.2012.08.021
[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. DOI:10.1002/art.30410 |
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