HS014 TFA

发表于由

HS014 TFA; 纯度: 98.81%

HS014 TFA 是一种高效、选择性的黑素皮质素-4 (MC4) 受体拮抗剂，对人 MC4、MC1、MC3 和 MC5 受体的 Ki 值分别为 3.16、108、54.4 和 694 nM。HS014 TFA 调节吗啡对小鼠行为的影响。HS014 TFA 增加自由喂养大鼠的食物摄取量。

HS014 TFAamp;;

HS014 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ￥4500 In-stock
5 mg ￥13500 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

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HS014 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library
  • Peptide Library

生物活性

HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats[1][2][3].

体内研究
(In Vivo)

The dose-effect curve of morphine for locomotor activity was shifted downwards in C57Bl/6 mice pretreated with HS014 TFA and in A(y) mice. The dose-effect curve of morphine for antinociception is shifted two- and threefold to the left in C57Bl/6 mice pretreated with HS014 TFA and in A(y) mice, respectively[2].
Pretreatment with HS014 TFA blocks the effect of IL-1beta on food intake and respiratory exchange ratio (RER) at later time points (beyond 8 h post injection), as well as the hypoactivity and increases metabolic rate[4].

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

1677.78

Formula

C73H95F3N20O19S2
Sequence

Ac-Cys-Glu-His-{D-2Nal}-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (Disulfide bridge:Cys1-Cys8)
Sequence Shortening

Ac-CEH-{D-2Nal}-RWGCPPKD-NH2 (Disulfide bridge:Cys1-Cys8)
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)
参考文献

  • [1]. Schiöth HB,et al. Discovery of novel melanocortin4 receptor selective MSH analogues. Br J Pharmacol. 1998;124(1):75-82.

    [2]. Ercil NE, et al. HS014, a selective melanocortin-4 (MC4) receptor antagonist, modulates the behavioral effects of morphine in mice. Psychopharmacology (Berl). 2005;180(2):279-285.

    [3]. Kask A, et al. Selective antagonist for the melanocortin 4 receptor (HS014) increases food intake in free-feeding rats. Biochem Biophys Res Commun. 1998;245(1):90-93.