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Pasireotide pamoate

Catalog No. T12369 CAS 396091-79-5

Synonyms: SOM230 pamoate

Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

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Pasireotide pamoate, CAS 396091-79-5

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Description	Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
Targets&IC50	SST2:9 (pki), SST5:9.9(pki), SST4:<7.0 (pki), SST1:pki:8.2 , SST3:9.1(pki)
In vitro	SOM230, a novel, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1-sst5).?SOM230 has potent, long-lasting inhibitory effects on growth hormone and insulin-like growth factor-1 release[1]
In vivo	Untreated SSTR2(-/-) mice with AIA displayed joint swelling and mechanical hyperalgesia similar to that seen in SSTR2(+/+) mice.?In wild-type mice, both octreotide and pasireotide significantly attenuated knee joint swelling and histopathologic manifestations of arthritis to an extent comparable to that of dexamethasone.?In SSTR2(-/-) mice, the antiinflammatory effects of both octreotide and pasireotide were completely abrogated.?Prolonged administration of pasireotide also inhibited joint swelling and protected against joint destruction during AIA flare reactions.?In addition, both octreotide and pasireotide reduced inflammatory hyperalgesia.?The antinociceptive actions of octreotide were abolished in SSTR2(-/-) mice, but those of pasireotide were retained.?In dorsal root ganglia of naive wild-type mice, only SSTR1 and SSTR2A, but not SSTR3 or SSTR5, were detected in a subset of small- and medium-diameter neurons[1].

Synonyms	SOM230 pamoate
Molecular Weight	1435.58
Formula	C81H82N10O15
CAS No.	396091-79-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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.

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Keywords

Pasireotide pamoate 396091-79-5 Others SOM230 pamoate inhibitor inhibit

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