TAK-448 acetate (Synonyms: MVT-602 acetate) |
カタログ番号GC37722
One-Click Copy Product Info
|
TAK-448 acetateはオリゴペプチド類似体であり、KISS1受容体（GPR54；IC₅₀=460pM、EC₅₀=632pM）の有力な作動剤として機能する。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1470374-22-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
TAK-448 acetateはオリゴペプチド類似体であり、KISS1受容体（GPR54；IC₅₀=460pM、EC₅₀=632pM）の有力な作動剤として機能する[1-2]。TAK-448 acetateは、内因性kisspeptin-54のC末端類似物である。急性投与は、黄体形成ホルモン（LH）と卵胞刺激ホルモン（FSH）の放出を刺激し、持続的な暴露は、下垂体性腺軸を下方制御し、よってテストステロンのレベルを速やかに減らした。TAK-448 acetateは主に、内分泌調節と前立腺癌の治療に関連する研究に使われる[3-4]。
In vivo（体内）実験で、単回皮下注射（0.03–3mg/kg）として、VCaP前立腺癌異種移植片を持つ雄のF344/N Jcl-rnu/rnuラットに、TAK-448 acetate（TAK-448-SR(1M)の徐放性製剤の形式で）を投与した（移植後の7週目から、4週間ごとに繰り返した）。TAK-448 acetateは、血漿テストステロンとLHのレベルを著しく低下させ、睾丸、前立腺と精嚢の成長を抑制し、血漿前立腺癌特異性の抗原レベルを速やかに減らした[5]。代謝機能障害関連脂肪肝疾患（MASLD）のDIAMOND雄マウスのモデルで、浸透圧ミニポンプを通じて、TAK-448 acetate（0.3nmol/時間）を6週間連続的に皮下投与したところ、TAK-448 acetateは、肝臓の新規脂肪生成を著しく阻害し、肥満、糖尿病と肝細胞癌と関連する遊走脂肪酸の合成を減らし、肝臓脂肪症とインスリン抵抗性を改善し、CIDEAや転写因子SREBP-1cなどの肝心な脂質滴調節因子の発現を下方制御した[6]。
References:
[1] Nishizawa N, Takatsu Y, Kumano S, 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 Potent Testosterone-Suppressive Activity and Excellent Water Solubility. J Med Chem. 2016 Oct 13;59(19):8804-8811.
[2] Stalewski J, Hargrove DM, Wolfe M, et al. Additive effect of simultaneous continuous administration of degarelix and TAK-448 on LH suppression in a castrated rat model. Eur J Pharmacol. 2018 Apr 5;824:24-29.
[3] MacLean DB, Matsui H, Suri A, et al. 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.
[4] Matsui H, Tanaka A, Yokoyama K, et al. Chronic administration of the metastin/kisspeptin analog KISS1-305 or the investigational agent TAK-448 suppresses hypothalamic pituitary gonadal function and depletes plasma testosterone in adult male rats. Endocrinology. 2012 Nov;153(11):5297-308.
[5] Ishikawa K, Tanaka A, Kogame A, 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-sensitive prostate cancer model. Eur J Pharmacol. 2018 Jun 5;828:126-134.
[6] Izarraras K, Shah A, Prasad K, et al. Kisspeptin Mitigates Hepatic De Novo Lipogenesis in Metabolic Dysfunction-Associated Steatotic Liver Disease. Cells. 2025 Aug 20;14(16):1289.
| 動物実験 [1]: | |
動物モデル | DIAMONDマウス（C57BL/6J × 129S1/Svlmバックグラウンド） |
準備方法 | 蔗糖水を持つ西洋食（WDSW）をマウスに6週間投与し、代謝機能障害関連の脂肪性肝疾患（MASLD）を誘発し、浸透式ミニポンプを通じて、TAK-448 acetate（0.3nmol/時間）を6週間皮下投与し、同時にWDSWを維持した。重水素標識水（²H₂O）を最終週に提供し、新型脂肪生成（DNL）を追跡した。肝臓と代謝分析のために、マウスを殺処分した。 |
投与形態 | 0.3nmol/時間；連続的な皮下潅流；6週間 |
アプリケーション | TAK-448 acetateは肝臓DNLを著しく減らし、肝内脂肪酸合成を減少させ、肝臓トリグリセリドの含有量、無血清脂肪酸とALTのレベルを低下させた。TAK-448 acetateは、インスリンの感受性と耐糖性を改善し、AMPK活性化を通じて、肝心な脂質生成調節因子を下方制御し、MASLDに対して潜在的な治療能力を示した。 |
References: | |
| Cas No. | 1470374-22-1 | SDF | |
| 同義語 | MVT-602 acetate | ||
| Formula | C60H84N16O16 | M.Wt | 1285.41 |
| 溶解度 | DMSO: ≥ 100 mg/mL (77.80 mM); Water: 50 mg/mL (38.90 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 778 μL | 3.8898 mL | 7.7796 mL |
| 5 mM | 155.6 μL | 778 μL | 1.5559 mL |
| 10 mM | 77.8 μL | 389 μL | 778 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)