TAK-448

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TAK-448

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1234319-68-6

包装与价格：

产品名称

MVT-602

产品介绍

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

生物活性

TAK-448 (MVT-602) is a potent and fullKISS1Ragonist with anIC₅₀of 460 pM and anEC₅₀of 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].

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 (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>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.