NKH 477(达福尔考辛)

NKH 477(达福尔考辛)用途

NKH477 (Colforsin dapropate hydrochloride) 是一种新型水溶性毛喉素衍生物,主要通过对舒张性心脏功能的有益作用来改善心力衰竭。 NKH477 直接激活腺苷酸环化酶 (adenylate cyclase) 的催化单元并增加细胞内 cAMP。 NKH477 在体内具有改变的细胞因子谱而发挥抗增殖作用,抑制大鼠原位肺同种异体移植物的急性排斥。

NKH 477(达福尔考辛)名称

[ CAS 号 ]:
138605-00-2

[ 中文名 ]:
NKH477

[ 英文名 ]:
NKH477

[英文别名 ]:

colforsindapropatehydrochloride
Adehl
NKH 477
colforsin daropate hydrochloride
MKH 477

NKH 477(达福尔考辛)生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷酸环化酶

[ 靶点 ]

Adenylate Cyclase[1]

[体内研究]

NKH477(盐酸Colforsin dapropate hydrochloride)(口服；1-3mg/kg/天；第3天和第5天)以剂量依赖性方式延长同种异体肺移植物的存活[1]。动物模型：无特定病原体的近交雄性Lewis大鼠(LEW),体重250-280g[1]剂量：1,2或3mg/kg/天。给药：口服；每日；第3天和第5天结果：以剂量依赖性方式延长同种异体肺移植物存活。

[参考文献]

[1]. Nakashima S, et al. Antiproliferative effects of NKH477, a forskolin derivative, on cytokine profile in rat lung allografts. J Heart Lung Transplant. 2005 Apr;24(4):462-9.

NKH 477(达福尔考辛)物理化学性质

[ 沸点 ]:
571.4ºC at 760mmHg

[ 分子式 ]:
C₂₇H₄₄ClNO₈

[ 分子量 ]:
546.093

[ 闪点 ]:
176ºC

[ 精确质量 ]:
545.275574

[ PSA ]:
122.60000

[ LogP ]:
2.82450

[ 蒸汽压 ]:
5.29E-16mmHg at 25°C

[ 储存条件 ]:
2-8°C

NKH 477(达福尔考辛)MSDS

详细MSDS(安全技术说明书)

NKH 477(达福尔考辛)安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
P264-P301 + P310

[ 危害码 (欧洲) ]:
T

[ 安全声明 (欧洲) ]:
28-36/37-45

[ 危险品运输编码 ]:
UN 2811 6.1 / PGII

[ RTECS号 ]:
AY5992600

NKH 477(达福尔考辛)文献

Analysis of compartmentalized cAMP: a method to compare signals from differently targeted FRET reporters.

Methods Mol. Biol. 1071 , 59-71, (2014)

Förster resonance energy transfer (FRET)-based reporters are important tools to study the spatiotemporal compartmentalization of cyclic adenosine monophosphate (cAMP) in living cells. To increase the ...

Chemically induced pluripotent stem cells (CiPSCs): a transgene-free approach.

J. Mol. Cell Biol. 5(5) , 354-5, (2013)

Induced pluripotent stem cells (iPSCs) could be generated by a single gene Oct4 and chemical compounds, in which exogenous expression of Oct4 was indispensable for reprogramming. Recent advances in ch...

Activation of cAMP signaling attenuates impaired hepatic glucose disposal in aged male p21-activated protein kinase-1 knockout mice.

Endocrinology 155(6) , 2122-32, (2014)

p21-activated protein kinase-1 (Pak1) plays a role in insulin secretion and glucagon-like peptide-1 (GLP-1) production. Pak1(-/-) mice were found to carry a defect in ip pyruvate tolerance test (IPPTT...

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