卡培立肽
中文名称:
卡培立肽
中文同义词:
卡培立肽;醋酸卡培立肽 89213-87-6;人重组型Α-心房尿钠肽;醋酸卡培立肽;卡培立肽杂质
英文名称:
ANP 1-28, HUMAN
英文同义词:
ATRIAL NATRIURETIC PEPTIDE HUMAN;SER-LEU-ARG-ARG-SER-SER-CYS-PHE-GLY-GLY-ARG-MET: O-ASP-ARG-ILE-GLY-ALA-GLN-SER-GLY-LEU-GLY-CYS-ASN-SER-PHE-ARG-TYR[SLRRSSCFGGR-MET: O-DRIGAQSGLGCNSFRY]DISULFIDE BRIDGE CYS7-CYS23.;Carperitide Acetate, carperitida;Atrial Natriuretic Peptide (1-28) (human) (trifluoroacetate salt);ahANF, Carperitide;H-Ser-Leu-Arg-Arg-Ser-Ser-Cys-Phe-Gly-Gly-Arg-Met-Asp-Arg-Ile-Gly-Ala-Gln-Ser-Gly-Leu-Gly-Cys-Asn-Ser-Phe-Arg-Tyr-OH;Atrial natriureticpeptide-28 (huMan) (9CI);Atrial Natriuretic Factor (1-28) (huMan) αhANF, Carperitide
CAS号:
89213-87-6
分子式:
C127H203N45O39S3
分子量:
3080.44
EINECS号:
686-482-9
相关类别:
多肽原料药;多肽;药物多肽;peptide
Mol文件:
89213-87-6.mol
密度
1.55±0.1 g/cm3(Predicted)
药理作用
卡培立肽是由三得利株式会社与宫崎医科大学共同研究合成、生产的由28个氨基酸构成的α型心房钠尿肽。药理学研究结果表明本药具有扩张血管、利尿作用，临床试验结果表明， 卡培立肽可减轻心脏前、后负荷，增加心脏输出量但不影响心率，对急性心力衰竭具有良好的治疗作用。
卡培立肽是通过刺激心肌伸展，由心室内颗粒合成的，然后通过冠静脉分布全身，作用于血管平滑肌和肾脏等组织，调节血压和体内电解质平衡。
生物活性
Carperitide是一种有效的natriuretic peptide receptor (NPR)-A 激动剂，EC50值为10.8 nM。Carperitide用于治疗充血性心力衰竭。
靶点
Target Value
NPR-A
(Cell-free assay) 10.8 nM(EC50)
Target
Value
NPR-A
(Cell-free assay)
10.8 nM(EC50)
体外研究
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a diuretic, natriuretic, and vasodilatory peptide hormone originally isolated from mammalian hearts. In cultured porcine endothelial cells the inhibition by porcine ANP (1-28) of immunoreactive endothelin-1 secretion after stimulation with Angiotensin II (Ang II) is paralleled by an increase in the cellular cGMP level. Porcine ANP (1-28) strongly inhibits immunoreactive endothelin-1 secretion in porcine aorta after stimulation with Ang II. ANP is a cardiac hormone involved in electrolyte and fluid homeostasis. The inhibition by ANP of endothelin-1 secretion stimulated by angiotensin II (ANGII) and thrombin using cultured human umbilical-vein endothelial cells. Human ANP (1-28) inhibits immunoreactive (ir)-endothelin-1 secretion and increases cyclic GMP in the human umbilical-vein endothelial cells. In glomeruli from normal rats, Human 125 I-ANP (1-28) binds to a single population of high affinity receptors with a mean equilibrium dissociation constant of 0.46 nM. Human ANP (1-28) binds to the glomerular ANP receptor with high affinity stimulated cGMP accumulation. Human ANP (1-28) markedly stimulates cGMP generation, but not cAMP generation in normal rat glomeruli.
