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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

Specification
Reference Reading

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.