TAK-448 TFA

• CAT Number: I009688
• CAS Number: 1433222-47-9 (TFA salt); 1234319-68-6 (free base).
• Molecular Formula: C60H81F3N16O16
• Molecular Weight: 1339.4
• Purity: ≥95%
• Synonyms: TAK448; TAK 448; TAK-448; TAK-448 TFA.;(S)-2-((2S,4R)-1-(acetyl-D-tyrosyl)-4-hydroxypyrrolidine-2-carboxamido)-N1-((2S,3R)-1-(((S)-1-(2-(((S)-1-(((S)-1-(((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-5-(3-methylguanidino)-1-oxopentan-2-yl)ami
• Solubility: soluble in DMSO, dilute HCl, not soluble in water.
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• SMILES: O=C(N)[C@H](CC1=CNC2=C1C=CC=C2)NC([C@H](CCCNC(NC)=N)NC([C@H](CC(C)C)NC(NNC([C@H](CC3=CC=CC=C3)NC([C@H]([C@H](O)C)NC([C@H](CC(N)=O)NC([C@H]4N(C([C@@H](CC5=CC=C(O)C=C5)NC(C)=O)=O)C[C@H](O)C4)=O)=O)=O)=O)=O)=O)=O.O=C(O)C(F)(F)F

TAK-448 (Cat. No: I009688) is a potential oligopeptide analog of kisspeptin. In animal experiments, acute administration of TAK-448 stimulated LH/FSH release, while continuous sc exposure rapidly down-regulated the pituitary-gonadal axis and rapidly reduced T levels in a dose-dependent manner. TAK-448 is known to have anti-tumor effects by inhibiting androgen ( luteinizing hormone and testosterone ) levels.

Reference

1:Williams R. Discontinued in 2013: oncology drugs. Expert Opin Investig Drugs. 2015 Jan;24(1):95-110. Epub 2014 Oct 14. PubMed PMID: 25315907.2:MacLean DB, Matsui H, Suri A, Neuwirth R, Colombel M. Sustained exposure to the investigational Kisspeptin analog, TAK-448, down-regulates testosterone into the castration range in healthy males and in patients with prostate cancer: results from two phase 1 studies. J Clin Endocrinol Metab. 2014 Aug;99(8):E1445-53. doi: 10.1210/jc.2013-4236. Epub 2014 Apr 24. PubMed PMID: 24762108.3:Matsui H, Masaki T, Akinaga Y, Kiba A, Takatsu Y, Nakata D, Tanaka A, Ban J, Matsumoto S, Kumano S, Suzuki A, Ikeda Y, Yamaguchi M, Watanabe T, Ohtaki T, Kusaka M. Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide. Eur J Pharmacol. 2014 Jul 15;735:77-85. doi: 10.1016/j.ejphar.2014.03.058. Epub 2014 Apr 18. PubMed PMID: 24747751.