| Identification | Back Directory | [Name]
Pasireotide Acetate | [CAS]
396091-76-2 | [Synonyms]
Pasireotide Acetate
Pasireotide Acetate(acetate)
Somatostatin Receptor,sst3,Inhibitor,SOM230,SOM 230,Pasireotide,proapoptotic,sst1,antiproliferative,inhibit,somatostatin,SSTRs,sst4,SOM-230,SSTR,sst5,antisecretory,Pasireotide Acetate,sst2 | [Molecular Formula]
C60H70N10O11 | [MDL Number]
MFCD32666205 | [MOL File]
396091-76-2.mol | [Molecular Weight]
1107.28 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO : 100 mg/mL (90.31 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to off-white | [Sequence]
Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-Lys-{Tyr(4-Bzl)}-Phe] |
| Hazard Information | Back Directory | [Uses]
Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2][3]. | [in vivo]
Pasireotide acetate (160 mg/kg/month; 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 acetate (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[4]. | 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
[4] Schmid HA, et, al. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008 May 14;286(1-2):69-74. DOI:10.1016/j.mce.2007.09.006 |
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