HS028

• 产品号: H4402
• 分子式: C17H34O3
• 分子量: 286.45006

产品别名

• 标题: HS028
• IUPAC标准名: methyl 16-hydroxyhexadecanoate
• IUPAC传统名: methyl 16-hydroxyhexadecanoate
• 别名: Melanocortin 4 Receptor antagonist; MC4 Receptor antagonist

产品登记号

• MDL号: MFCD02179660

产品性质

• 相关基因信息: human ... POMC(5443)
• 外观: lyophilized powder
• 保存温度: -20°C
• 德国WGK号: 3

产品详细信息

详细说明 (English)

Amino Acid Sequence
Ac-Cys-Glu-His-diCl-D-Phe-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
Biochem/physiol Actions
HS028 (cyclic [AcCys11, dichloro-D-phenylalanine14, Cys18, Asp-NH2(22)]-beta-MSH11-22) showed high affinity (Ki of 0.95nM) and high (80 fold) MC4 receptor selectivity over the MC3 receptor. HS028 antagonised a alpha-MSH induced increase in cyclic AMP production in transfected cells expressing the MC3 and MC4 receptors, whereas it seemed to be a partial agonist for the MC1 and MC5 receptors. Chronic intracerebroventricularly (i.c.v.) administration of HS028 by osmotic minipumps significantly increased both food intake and body weight in a dose dependent manner without tachyphylaxis for a period of 7 days. This is further evidence that the MC4 receptor is an important mediator of long term weight homeostasis.

详细说明 (简体中文)

Amino Acid Sequence
Ac-Cys-Glu-His-diCl-D-Phe-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
Biochem/physiol Actions
HS028 (cyclic [AcCys11, dichloro-D-phenylalanine14, Cys18, Asp-NH2(22)]-beta-MSH11-22) showed high affinity (Ki of 0.95nM) and high (80 fold) MC4 receptor selectivity over the MC3 receptor. HS028 antagonised a alpha-MSH induced increase in cyclic AMP production in transfected cells expressing the MC3 and MC4 receptors, whereas it seemed to be a partial agonist for the MC1 and MC5 receptors. Chronic intracerebroventricularly (i.c.v.) administration of HS028 by osmotic minipumps significantly increased both food intake and body weight in a dose dependent manner without tachyphylaxis for a period of 7 days. This is further evidence that the MC4 receptor is an important mediator of long term weight homeostasis.