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(S)-2,6-二甲基-5-硝基-4-(2-三氟甲基)苯基)-1,4-二氢吡啶-3-甲酸甲酯

用途

Bay-K-8644 (S)-(-)- 是 L 型钙离子通道激动剂。Bay-K-8644 (S)-(-)- 激活 Ba2+电流 (IBa),EC50 为 32 nM。

名称

[ CAS 号 ]:
98625-26-4

[ 中文名 ]:
Bay-K-8644((S)-(-)-)

[ 英文名 ]:
(S)-(-)-Bay K 8644

[英文别名 ]:

Tocris-1544
(S)-(-)-Bay K8644
Lopac-B-112
Bay-K-8644 ((S)-(-)-)

生物活性

[ 描述 ]:

Bay-K-8644 (S)-(-)- 是 L 型钙离子通道激动剂。Bay-K-8644 (S)-(-)- 激活 Ba2+电流 (IBa),EC50 为 32 nM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 心血管疾病

[ 靶点 ]

EC50: 32 nM (IBa)[1]

[体外研究]

(±)-Bay K 8644,Bay K 8644的常规外消旋混合物,广泛用作L型Ca 2+通道激动剂。每种光学异构体对IBa(R(+)- Bay K 8644作为拮抗剂和Bay-K-8644(S)-(-)-作为激动剂具有相反的作用.Bay-K-8644(S)-(-)-可以防止两种不同的环核苷酸途径对豚鼠胃窦肌细胞中IBa的抑制作用[1].3-30μMBay-K-8644(S)-(-)-增强Ca2 +通道活性L-型Ca2 +通道的激动剂[2]。在平滑肌L型Ca2 +通道上检测两种Ca2 +通道激活剂Bay-K-8644(S)-(-)-和FPL 64176的相互作用.FPL 64176( 300 nM)引起大鼠尾动脉条的持续收缩.Bay-K-8644(S)-(-)-(EC50 = 14 nM)使这种收缩反应受到约70％的抑制.Bay-K-8644(S )-(-)-(100 nM)增加A7r5平滑肌细胞中的全细胞Ca2 +电流,但有效阻断1μMFPL64176的进一步刺激[3]。

[参考文献]

[1]. Zhu HL, et al. Antagonistic actions of S(-)-Bay K 8644 on cyclic nucleotide-induced inhibition of voltage-dependent Ba(2+) currents in guinea pig gastric antrum. Naunyn Schmiedebergs Arch Pharmacol. 2008 Dec;378(6):609-15.

[2]. Mironov SL, et al. L-type Ca2+ channels in inspiratory neurones of mice and their modulation by hypoxia. J Physiol. 1998 Oct 1;512 ( Pt 1):75-87.

[3]. Rampe D, et al. Functional interactions between two Ca2+ channel activators, (S)-Bay K 8644 and FPL 64176, in smooth muscle. Mol Pharmacol. 1992 Apr;41(4):599-602.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.37g/cm3

[ 沸点 ]:
429.2ºC at 760mmHg

[ 分子式 ]:
C₁₆H₁₅F₃N₂O₄

[ 分子量 ]:
356.29700

[ 闪点 ]:
213.4ºC

[ 精确质量 ]:
356.09800

[ PSA ]:
84.15000

[ LogP ]:
4.19940

[ 储存条件 ]:
2-8°C，干燥密封

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319

[ 警示性声明 ]:
P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危险品运输编码 ]:
NONH for all modes of transport

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