TAK-448 acetate

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。

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库存: 现货

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1mg

￥1625.00

1300.00

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5mg

￥4850.00

3880.00

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10mg

￥0.00

0.00

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50mg

￥0.00

0.00

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已选 0 种 0 瓶

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货号: ajce59686
CAS: 1470374-22-1
别名: MVT-602 acetate
分子式: C60H84N16O16
分子量: 1285.41
纯度: >98%
溶解度: DMSO: ≥ 100 mg/mL (77.80 mM); Water: 50 mg/mL (38.90 mM)
储存: Store at -20°C
库存: 现货

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.