Takrolimus

Из Википедије, слободне енциклопедије
Takrolimus
Tacrolimus-Armistead-2D-skeletal.png
Tacrolimus-3D-sticks.png
Klinički podaci
Prodajno ime Advagraf, Hecoria, Prograf, Protopic
Drugs.com Monografija
Način primene Oralno, intravenozno, topikalno
Farmakokinetički podaci
Poluvreme eliminacije 35 h
Identifikatori
CAS broj 104987-11-3 ДаY
ATC kod D11AH01 (WHO) , L04AD02
PubChem CID 445647
DrugBank DB00864 ДаY
ChemSpider 4976056 ДаY
KEGG C01375 ДаY
ChEBI CHEBI:61049 ДаY
ChEMBL CHEMBL269732 ДаY
Hemijski podaci
Formula C44H69NO12
Molarna masa 804,018
Fizički podaci
Tačka topljenja 126 °C (259 °F)

Takrolimus je organsko jedinjenje, koje sadrži 44 atoma ugljenika i ima molekulsku masu od 804,018 Da.[1][2][3][4][5][6][7]

Osobine[уреди]

Osobina Vrednost
Broj akceptora vodonika 12
Broj donora vodonika 3
Broj rotacionih veza 7
Particioni koeficijent[8] (ALogP) 4,8
Rastvorljivost[9] (logS, log(mol/L)) -7,9
Polarna površina[10] (PSA, Å2) 178,3

Reference[уреди]

  1. Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, Kohsaka M, Aoki H, Imanaka H: FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1987 Sep;40(9):1249-55. PMID 2445721
  2. Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91. PMID 15896681
  3. Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, Schreiber SL: Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. PMID 1715244
  4. Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike F, Takada Y, Inui K: Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient. Drug Metab Pharmacokinet. 2006 Apr;21(2):122-5. PMID 16702731
  5. Hanifin JM, Paller AS, Eichenfield L, Clark RA, Korman N, Weinstein G, Caro I, Jaracz E, Rico MJ: Efficacy and safety of tacrolimus ointment treatment for up to 4 years in patients with atopic dermatitis. J Am Acad Dermatol. 2005 Aug;53(2 Suppl 2):S186-94. PMID 16021174
  6. Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. doi:10.1093/nar/gkq1126. PMC 3013709слободно за читање. PMID 21059682.  edit
  7. David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. doi:10.1093/nar/gkm958. PMC 2238889слободно за читање. PMID 18048412.  edit
  8. Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o. 
  9. Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. doi:10.1021/ci000392t. PMID 11749573.  edit
  10. Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. doi:10.1021/jm000942e. PMID 11020286.  edit

Literatura[уреди]

Spoljašnje veze[уреди]

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