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BAPTA-AM

现货
Catalog No.
B4758
钙螯合剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
现货
10mg
¥ 670.00
现货
50mg
¥ 2,370.00
现货

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Background

BAPTA-AM is a selective calcium chelator [1].

Ca2+ is one of the most ubiquitous and versatile intracellular signaling molecules that control numerous cellular processes such as neurotransmitter release, contraction of all muscle cell types and fertilization [4].

BAPTA-AM is a selective and membrane permeable calcium chelator. In the human leukemia cell lines HL-60 and U937, BAPTA/AM (10 μM) induced internucleosomal DNA cleavage and classic apoptotic morphology. Also, BAPTA/AM increased Ca2+ in intracellular and downregulated c-jun [1]. In bovine chromaffin cells, APTA-AM (50 μM) rapidly and reversibly inhibited Ca2+-activated K+ (I(KCa)) and voltage-gated K+ (I(K)) by 50% [2]. In HEK 293 cells, BAPTA-AM inhibited hERG (Kv11.1), hKv1.3 and hKv1.5 channels with IC50 values of 1.3, 1.45 and 1.23 μM respectively in a concentration dependent way, which was dependent on channel opening [3].

In swiss mice, BAPTA-AM inhibited locomotor stimulation produced by ethanol and reversed ethanol-induced hypnotic effects. In male C57BL/6J mice, BAPTA-AM reduced ethanol consumption in a dose-dependent way [4].

References:
[1].  Grant S, Freemerman AJ, Gregory PC, et al. Induction of apoptotic DNA fragmentation and c-jun downregulation in human myeloid leukemia cells by the permeant Ca2+ chelator BAPTA/AM. Oncol Res, 1995, 7(7-8): 381-392.
[2].  Urbano FJ, Buño W. BAPTA-AM blocks both voltage-gated and Ca2+-activated K+ currents in cultured bovine chromaffin cells. Neuroreport, 1998, 9(15): 3403-3407.
[3].  Tang Q, Jin MW, Xiang JZ, et al. The membrane permeable calcium chelator BAPTA-AM directly blocks human ether a-go-go-related gene potassium channels stably expressed in HEK 293 cells. Biochem Pharmacol, 2007, 74(11): 1596-1607.
[4].  Baliño P, Monferrer L, Pastor R, et al. Intracellular calcium chelation with BAPTA-AM modulates ethanol-induced behavioral effects in mice. Exp Neurol, 2012, 234(2): 446-453.

文献引用

1. Li S, Lu D, et al. "Electrical Stimulation Activates Fibroblasts through the Elevation of Intracellular Free Ca(2+): Potential Mechanism of Pelvic Electrical Stimulation Therapy." Biomed Res Int. 2019 Apr 21;2019:7387803. PMID:31139648
2. Wang J, Yang C, et al. "T-2 Toxin Exposure Induces Apoptosis in TM3 Cells by Inhibiting Mammalian Target of Rapamycin/Serine/Threonine Protein Kinase(mTORC2/AKT) to Promote Ca(2+)Production." Int J Mol Sci. 2018 Oct 27;19(11). pii: E3360. PMID:30373220
3. Wang Y, Lu S, et al. "Sonic hedgehog induces GLT-1 degradation via PKC delta to suppress its transporter activities." Neuroscience. 2017 Oct 6;365:217-225. PMID:28993237

Chemical Properties

StorageDesiccate at -20°C
M.Wt764.68
Cas No.126150-97-8
FormulaC34H40N2O18
Solubility≥16.3mg/mL in DMSO with gentle warming
SDFDownload SDF
Canonical SMILESO=C(CN(CC(OCOC(C)=O)=O)C1=CC=CC=C1OCCOC2=CC=CC=C2N(CC(OCOC(C)=O)=O)CC(OCOC(C)=O)=O)OCOC(C)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1, 2]:

细胞系

人白血病细胞系HL-60和U937,牛嗜铬细胞

溶解方法

该化合物在DMSO中的溶解度大于16.3 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

10 μM,50 μM,6 h

应用

在人白血病细胞系HL-60和U937中,BAPTA/AM(10 μM)诱导产生经典的凋亡形态,BAPTA/AM(50 μM)诱导产生一些非典型特征,例如细胞肿胀及染色质聚集。BAPTA-AM(50 μM)的灌注引起IKCa和IK快速(<60s)及可逆阻滞(~50%)。用BAPTA/AM(50 μM,30分钟)或用BAPTA的非通透活性形式(在移液管溶液中10 mM)进行预孵育,永久阻断IKCa。在BAPTA加载或BAPTA-AM预培养后,BAPTA-AM超灌注(50 μM)阻断IK(~53%)。

动物实验 [3]:

动物模型

Swiss (RjOrl)小鼠,雄性C57BL/6J小鼠

给药剂量

0–10 mg/kg,30 min

应用

在Swiss (RjOrl)小鼠中,用BAPTA-AM(0-10 mg/kg,30分钟)预处理在不改变基础运动的条件下阻止了乙醇产生的运动刺激。BAPTA-AM逆转乙醇诱导的催眠作用。在黑暗喝酒方法之后,给予雄性C57BL/6J小鼠20%v/v乙醇、自来水或0.1%甜味水。BAPTA-AM预处理(0-5 mg/kg)以剂量依赖性方式降低乙醇消耗,而对水和甜水摄入不受影响。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Grant S, Freemerman AJ, Gregory PC, et al. Induction of apoptotic DNA fragmentation and c-jun downregulation in human myeloid leukemia cells by the permeant Ca2+ chelator BAPTA/AM. Oncol Res, 1995, 7(7-8): 381-392.

[2]. Urbano FJ, Buo W. BAPTA-AM blocks both voltage-gated and Ca2+-activated K+ currents in cultured bovine chromaffin cells. Neuroreport, 1998, 9(15): 3403-3407.

[3] Balio P, Monferrer L, Pastor R, et al. Intracellular calcium chelation with BAPTA-AM modulates ethanol-induced behavioral effects in mice. Exp Neurol, 2012, 234(2): 446-453.

生物活性

Description BAPTA-AM是一种选择性的细胞膜可透过的钙螯合剂.
靶点            
IC50            

质量控制

化学结构

BAPTA-AM

相关生物数据

BAPTA-AM

相关生物数据

BAPTA-AM

相关生物数据

BAPTA-AM