标签归档：mvt

TAK-448(Synonyms: MVT-602)

发表于由

TAK-448;(Synonyms: MVT-602)

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

TAK-448amp;;(Synonyms: MVT-602)

TAK-448 Chemical Structure

CAS No. : 1234319-68-6

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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TAK-448 的其他形式现货产品:

TAK-448 acetate

生物活性

TAK-448 (MVT-602) 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 (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

1225.36

Formula

C58H80N16O14
CAS 号

1234319-68-6
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. 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.