Pasireotide pamoate - CAS# 396091-79-5

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.

Product information

CAS Number: 396091-79-5

Molecular Weight: 1435.58

Formula: C81H82N10O15

Chemical Name: (3S, 6R, 9S, 12S, 15S, 19R, 20aS)-6-((1H-indol-3-yl)methyl)-9-(4-aminobutyl)-15-benzyl-12-(4-(benzyloxy)benzyl)-1, 4, 7, 10, 13, 16-hexaoxo-3-phenylicosahydropyrrolo[1, 2-a][1, 4, 7, 10, 13, 16]hexaazacyclooctadecin-19-yl (2-aminoethyl)carbamate 4, 4'-methylenebis(3-hydroxy-2-naphthoate)

Smiles: NCCNC(=O)O[C@@H]1C[C@H]2C(=O)N[C@@H](C3=CC=CC=C3)C(=O)N[C@H](CC3=CNC4C=CC=CC3=4)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)OCC3=CC=CC=C3)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N2C1.OC(=O)C1=CC2=CC=CC=C2C(CC2C3=CC=CC=C3C=C(C=2O)C(O)=O)=C1O

InChiKey: HSXBEUMRBMAVDP-QKXVGOHISA-N

InChi: InChI=1S/C58H66N10O9.C23H16O6/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72);1-10,24-25H,11H2,(H,26,27)(H,28,29)/t43-,46+,47+,48-,49+,50+,51+;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Pasireotide pamoate exhibits unique high-affinity binding to human somatostatin receptors. 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.

In Vivo:

Pasireotide pamoate (160mg/Kg/month; s.c.; for 4 months) decreases serum insulin levels and increases serum glucose levels in Pdx1-Cre. Pasireotide pamoate displays a reduction in tumor activity and reduces Pancreatic Neuroendocrine Tumor (PNET) size in Pdx1-Cre. Pasireotide pamoate increases apoptosis in PNETs in Pdx1-Cre. Pasireotide pamoate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in in a mouse model of immune-mediated arthritis.

Products are for research use only. Not for human use.