中文名称:

离子载体(钙镁盐混合物)

中文同义词:

A23187(游离酸);钙离子载体A23187;抗生素 A 23187;钙离子载体 A23187 混合钙镁盐;钙离子载体 A23187, 来源于链霉菌属;离子载体(钙镁盐混合物);CALCIMYCIN游离态

英文名称:

A23187

英文同义词:

A23187 (CalciMycin);CALCIUM IONOPHORE III;CALCIUM IONOPHORE A23187;CALCIMYCIN;CALCIMYCIN A23187;IONOPHORE A-23187;5-(Methylamino)-2-[[(2R,3R,6S,8S,9R,11R)-3,9,11-trimethyl-8-[(1S)-1-methyl-2-oxo-2-(1H-pyrrol-2-yl)-ethyl]-1,7-dioxaspiro[5.5]undec-2-yl]methyl]-4-benzoxazolecarboxylic acid;Bis[5-methylamino-2-[[(6S)-3β,9α,11β-trimethyl-8α-[(S)-1-methyl-2-oxo-2-(1H-pyrrol-2-yl)ethyl]-1,7-dioxaspiro[5.5]undec-2β-yl]methyl]-4-benzoxazolecarboxylic acid]calcium salt

CAS号:

52665-69-7

分子式:

C29H37N3O6

分子量:

523.62

EINECS号:

258-084-1

相关类别:

微生物代谢物;荧光探针，标记，颗粒和染色;Signalling;antibiotic;Calcium channel

Mol文件:

52665-69-7.mol

熔点 

187-190 °C

比旋光度 

D25 -56° (c = 1 in chloroform)

沸点 

710.3±55.0 °C(Predicted)

密度 

1.28±0.1 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

Soluble in DMSO with warming or sonication. Also soluble in ethanol or ethyl acetate

形态

Solid

酸度系数(pKa)

pKa1 6.9 in 90% DMSO

颜色

white to light yellow

Merck 

13,1639

BRN 

1096801

生物活性

Calcimycin (A-23187) 是一种抗生素和独特的二价阳离子离子载体 (divalent cation ionophore)，如钙离子和镁离子。Calcimycin 通过增加细胞内钙浓度诱导 Ca2+ 依赖性细胞死亡。Calcimycin 抑制革兰氏阳性细菌和一些真菌的生长，还抑制 ATP 酶的活性并解耦哺乳动物细胞的氧化磷酸化 (OXPHOS)，诱导细胞凋亡。

体外研究

Calcimycin (A-23187) mediates mycobacterial killing by inducing intracellular calcium-regulated autophagy in a P2RX7 dependent manner.

体内研究

Calcimycin (A-23187) (2.5 or 7.5 nM; intrapleurally) induces protein leakage. Animal Model: Mice (ICR, 25-30 g) Dosage: 2.5 or 7.5 nM Administration: Intrapleurally Result: Two hours after 2.5 nM, or three hours after 7.5 nM, challenge the protein levels in the pleural cavity were equivalent to about a half of their corresponding peak values.

Animal Model:

Mice (ICR, 25-30 g)

Dosage:

2.5 or 7.5 nM

Administration:

Intrapleurally

Result:

Two hours after 2.5 nM, or three hours after 7.5 nM, challenge the protein levels in the pleural cavity were equivalent to about a half of their corresponding peak values.

用途 

高选择性钙离子载体增强对NMDA非使君子氨酸的响应。在细胞培养中，通过钙调素依赖结构型一氧化氮合酶刺激一氧化氮的生成。

危险品标志 

Xi,Xn

危险类别码 

36/37/38-20/21/22

安全说明 

26-36

WGK Germany 

3

RTECS号

DM4676000

F 

8

海关编码 

29349990

毒性

LD50 i.p. in mice: 10 mg/kg (Gale)