396091-79-5

396091-79-5 structure

Name: Pasireotide Pamoate
Chemical Name: Pasireotide Pamoate
CAS Number: 396091-79-5
Molecular Formula: C₈₁H₈₂N₁₀O₁₅
Molecular Weight: 1435.576
Catalog: Signaling Pathways GPCR/G Protein Somatostatin Receptor
Create Date: 2019-12-19 17:25:48
Modify Date: 2024-01-10 21:11:54
Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves 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].

Name	Pasireotide Pamoate
Synonyms	4,4'-Methylenebis(3-hydroxy-2-naphthoic acid) - cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-benzyl-L-tyrosyl-L-phenylalanyl-(4R)-4-{[(2-aminoethyl)carbamoyl]oxy}-L-prolyl] (1:1) 2-Naphthalenecarboxylic acid, 4,4'-methylenebis[3-hydroxy-, compd. with cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl] (1:1)

Description	Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves 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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor
Target	pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]
In Vitro	Pasireotide pamoate exhibits unique high-affinity binding to human somatostatin receptors[1]. Pasireotide pamoate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells with an IC50 of 0.4±0.1 nM[1].
In Vivo	Pasireotide pamoate (160mg/Kg/month; s.c.; for 4 months) decreases serum insulin levels and increases serum glucose levels in Pdx1-Cre[2]. Pasireotide pamoate displays a reduction in tumor activity and reduces Pancreatic Neuroendocrine Tumor (PNET) size in Pdx1-Cre[2]. Pasireotide pamoate increases apoptosis in PNETs in Pdx1-Cre[2]. Pasireotide pamoate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in in a mouse model of immune-mediated arthritis[3]. Animal Model: Eight 12-month old mice carrying the Men1 allele, Men1 floxed/floxed conditional knockout (Pdx1-Cre)[2] Dosage: 60mg/kg Administration: Subcutaneous injection; very month; for 4 months Result: Decreased serum insulin levels and increases serum glucose levels in Pdx1-Cre.
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. [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.

Molecular Formula	C₈₁H₈₂N₁₀O₁₅
Molecular Weight	1435.576
Exact Mass	1434.596069

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