TAK-448 acetate (MVT-602 acetate) 是一种有效的 KISS1R 激动剂，IC₅₀ 值为 460 pM，EC₅₀ 值为 632 pM。

TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC 50 of 460 pM and an EC 50 of 632 pM.

Solid

IC50: 460 pM (KISS1R)
EC50: 632 pM (KISS1R)

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Rat VCaP xe

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

Ac-{d-Tyr}-{Hyp}-NTF-{Aza-Gly}-L-{Arg(Me)}-W-NH2

[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.

In Vitro: DMSO : ≥ 100 mg/mL (77.80 mM)H₂O : 50 mg/mL (38.90 mM; Need ultrasonic)