Pasireotide Pamoate
Modify Date: 2024-01-10 21:11:54
Pasireotide Pamoate structure
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Common Name | Pasireotide Pamoate | ||
|---|---|---|---|---|
| CAS Number | 396091-79-5 | Molecular Weight | 1435.576 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C81H82N10O15 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Pasireotide PamoatePasireotide 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 |
|---|---|
| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C81H82N10O15 |
|---|---|
| Molecular Weight | 1435.576 |
| Exact Mass | 1434.596069 |
| 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) |