D[LEU4,LYS8]-VP TFA

发表于由

D[LEU4,LYS8]-VP TFA; 纯度: 98.16%

D[LEU4,LYS8]-VP TFA 是血管加压素 V1b 受体的选择性激动剂，对大鼠，人类和小鼠 V1b 受体的 Ki 值分别为 0.16 nM，0.52 nM 和 1.38 nM。D[LEU4,LYS8]-VP TFA 具有较弱的抗利尿剂、升压药和体外催产素活性。

D[LEU4,LYS8]-VP TFAamp;;

D[LEU4,LYS8]-VP TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥800 In-stock
10 mg ￥1300 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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D[LEU4,LYS8]-VP TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Macrocyclic Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Peptide Library

生物活性

D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities[1][2].

IC50 Target

vasopressin V1b receptor[1]
分子量

1140.25

Formula

C49H68F3N11O13S2
Sequence

{Mpa}-Tyr-Phe-Leu-Asn-Cys-Pro-Lys-Gly (Disulfide bridge:Mpa1-Cys6)
Sequence Shortening

{Mpa}-YFLNCPKG-NH2 (Disulfide bridge:Mpa1-Cys6)
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)
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]. Ana P, et, al. Pharmacological and physiological characterization of d[Leu4, Lys8]vasopressin, the first V1b-selective agonist for rat vasopressin/oxytocin receptors. Endocrinology. 2007 Sep; 148(9): 4136-46.

    [2]. Ana P, et, al. Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8. J Med Chem. 2007 Feb 22; 50(4): 835-47.