| CAS NO: | 1470374-22-1 |
| 规格: | 98% |
| 分子量: | 1285.41 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| 1mg | 电议 |
| 5mg | 电议 |
Background:
TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM[1]. IC50: 460 pM (KISS1R)[1]EC50: 632 pM (KISS1R)[1]
TAK-448 acetate (0.01-3 mg/kg; given i.h.; dosings on day 0 and 28) has greater anti-tumor effects in VCaP xenograft model[2]. Animal Model: Rat VCaP xenograft androgen-sensitive prostate cancer model (7-week-old rats)
[1]. Nishizawa N, et al. Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly PotentTestosterone-Suppressive Activity and Excellent Water Solubility. J Med Chem. 2016 Oct 13;59(19):8804-8811. [2]. Ishikawa K,et al. Usefulness of pharmacokinetic/efficacy analysis of an investigational kisspeptin analog, TAK-448, in quantitatively evaluating anti-tumor growth effect in the rat VCaP androgen-sensitiveprostate cancer model. Eur J Pharmacol. 2018 Jun 5;828:126-134.
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