TAK-448 acetate(Synonyms: MVT-602 acetate)

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TAK-448 acetate;(Synonyms: MVT-602 acetate) 纯度: 99.37

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 acetateamp;;(Synonyms: MVT-602 acetate)

TAK-448 acetate Chemical Structure

CAS No. : 1470374-22-1

规格 价格 是否有货 数量
1 mg ￥1500 In-stock
5 mg ￥4500 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

TAK-448 acetate 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

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 Target

IC50: 460 pM (KISS1R)[1]
EC50: 632 pM (KISS1R)[1]
体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat VCaP xenograft androgen-sensitive prostate cancer model (7-week-old rats)
Dosage: 0.01, 0.03, 0.3, 3 mg/kg
Administration: Given i.h.; dosings on day 0 and 28
Result: Had greater anti-tumor effects in VCaP xenograft model.

Clinical Trial

分子量

1285.41

Formula

C60H84N16O16
CAS 号

1470374-22-1
Sequence Shortening

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

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

DMSO : ≥ 100 mg/mL (77.80 mM)

H2O : 50 mg/mL (38.90 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7780 mL 3.8898 mL 7.7796 mL
5 mM 0.1556 mL 0.7780 mL 1.5559 mL
10 mM 0.0778 mL 0.3890 mL 0.7780 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (1.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.94 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (1.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.94 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [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.