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2-APB

2-氨基乙氧基二苯基硼酸盐
Catalog No.
B6643
Ins(1,4,5)P3诱导Ca2+释放的拮抗剂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 545.00
现货
10mg
¥ 645.00
现货
50mg
¥ 2,245.00
现货

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A

背景

2-APB是Ins(1,4,5)P3诱导Ca2+释放的拮抗剂,其IC50值为42 μM[1]。

Myo-Ins(1,4,5)P3受体(IP3R)介导内部Ca2+动员。IP3R参与钙波和钙振荡的产生。

2-APB是Ins(1,4,5)P3诱导Ca2+释放的拮抗剂。2-APB抑制Ins(1,4,5)P3诱导的大鼠小脑微粒体Ca2+释放,其IC50值为42 μM。在人类血小板和中性粒细胞中,将2-APB加入到细胞外液中可以抑制凝血酶诱导的细胞内Ca2+增加。此外,2APB抑制血管紧张素Ⅱ(AⅡ)诱导的胸主动脉收缩[1]。在HEK-293细胞中,细胞外的2-APB阻断人TRPC5通道,其IC50值为20 μM。此外,2-APB阻断TRPC6和TRPC3通道。在过度表达TRPC5的细胞中,2-APB抑制细胞增殖[2]。在小鼠胰腺腺泡细胞中,低浓度的2-APB可以显著抑制钙库调控的钙内流。在透化的腺泡细胞中,高浓度的2-APB抑制直接刺激的Ca2+释放和InsP3诱导的Ca2+释放[3]。

在I/R引起睾丸损伤的大鼠中,2-APB显著增加超氧化物歧化酶(SOD)、总抗氧化能力(TAC)和谷胱甘肽(GSH),同时减少丙二醛(MDA)和DNA片段,这表明2-APR具有抗凋亡和抗氧化作用[4]。

参考文献:
[1].  Maruyama T, Kanaji T, Nakade S, et al. 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release. J Biochem, 1997, 122(3): 498-505.
[2].  Xu SZ, Zeng F, Boulay G, et al. Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol, 2005, 145(4): 405-414.
[3].  Choi KJ, Kim KS, Kim SH, et al. Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell. Korean J Physiol Pharmacol, 2010, 14(2): 105-111.
[4].  Sari E, Aksit H, Erken HA, et al. Protective effect of 2-APB on testicular ischemia-reperfusion injury in rats. J Urol, 2015, 193(3): 1036-1041.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at RT
M.Wt225.1
Cas No.524-95-8
FormulaC14H16BNO
Solubilityinsoluble in H2O; ≥27.85 mg/mL in EtOH; ≥9.4 mg/mL in DMSO
Chemical Name2-((diphenylboryl)oxy)ethanamine
SDFDownload SDF
Canonical SMILESNCCOB(C1=CC=CC=C1)C2=CC=CC=C2
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试验操作

Cell experiment:[1]

Cell lines

Mouse pancreatic acinar cells

Reaction Conditions

10 ~ 100 μM 2-APB

Applications

In mouse pancreatic acinar cells, 2-APB significantly inhibited store-operated Ca2+ (SOC) channel-mediated Ca2+ entry at low concentrations (~ 30 μM). At higher concentrations (~ 100 μM), 2-APB exerted multiple paradoxical effects including inhibition of InsP3-induced Ca2+ release and direct stimulation of Ca2+ release.

Animal experiment:[2]

Animal models

Adult male Sprague-Dawley rats, 250 ~ 300 g

Dosage form

2 or 4 mg/kg

Administered intraperitoneally

Applications

In rats with ischemia-reperfusion (I/R) induced testicular injury, 2-APB significantly increased mean levels of superoxide dismutase, total antioxidant capacity and glutathione, and reduced mean malondialdehyde and DNA fragmentation levels, which suggested the antiapoptotic and antioxidative effects of 2-APB.

Note

The technical data provided above is for reference only.

References:

1. Choi KJ, Kim KS, Kim SH, et al. Caffeine and 2-aminoethoxydiphenyl borate (2-APB) have different ability to inhibit intracellular calcium mobilization in pancreatic acinar cell. The Korean Journal of Physiology & Pharmacology, 2010, 14(2): 105-111.

2. Sari E, Aksit H, Erken HA, et al. Protective effect of 2-APB on testicular ischemia-reperfusion injury in rats. The Journal of Urology, 2015, 193(3): 1036-1041.

质量控制

化学结构

2-APB

相关生物数据

2-APB

相关生物数据

2-APB