Pasireotide Diaspartate
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Pasireotide Diaspartate

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Pasireotide is an orphan drug approved for the treatment of Cushing's disease in patients who fail or are ineligible for surgical therapy. It is a somatostatin receptor (SSTR) agonist with selectively for SST1, SST2, SST3, and SST5 over SST4 (IC50s = 9.3, 1, 1.5, 0.16, and >100 nM, respectively, for human recombinant receptors).

Category
Peptide Inhibitors
Catalog number
BAT-010798
CAS number
820232-50-6
Molecular Formula
C58H66N10O9·2C4H7NO4
Molecular Weight
1313.41
Pasireotide Diaspartate
IUPAC Name
(2S)-2-aminobutanedioic acid;[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate
Synonyms
SOM230
Related CAS
396091-73-9 396091-77-3 (L-aspartate)
Appearance
Crystalline Solid
Purity
≥95%
Sequence
H-Asp-OH.H-Asp-OH.cyclo[Hyp(Unk)-Phg-D-Trp-Lys-Tyr(Bn)-Phe]
InChI
InChI=1S/C58H66N10O9.2C4H7NO4/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;2*5-2(4(8)9)1-3(6)7/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);2*2H,1,5H2,(H,6,7)(H,8,9)/t43-,46+,47+,48-,49+,50+,51+;2*2-/m100/s1
InChI Key
NEEFMPSSNFRRNC-WTTBPHDXSA-N
Canonical SMILES
C1C(CN2C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN.C(C(C(=O)O)N)C(=O)O.C(C(C(=O)O)N)C(=O)O
1. Tofacitinib
Dennis J Cada,Danial E Baker,Terri L Levien,Kendra Demaris Hosp Pharm . 2013 May;48(5):413-24. doi: 10.1310/hpj4805-413.
Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation/medication use evaluation (DUE/MUE) is also provided each month. With a subscription, the monographs are sent in print and are also available on-line. Monographs can be customized to meet the needs of a facility. A drug class review is now published monthly with The Formulary Monograph Service. Through the cooperation of The Formulary, Hospital Pharmacy publishes selected reviews in this column. For more information about The Formulary Monograph Service, call The Formulary at 800-322-4349. The May 2013 monograph topics are ado-trastuzumab emtansine, pomalidomide, mipomersen, pasireotide diaspartate, and glycerol phenylbutyrate. The DUE/MUE is on atypical antipsychotics, extended release.
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