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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥545.00 | 现货 | |
10mg | ¥645.00 | 现货 | |
50mg | ¥2245.00 | 现货 |
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产品描述
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.
产品性质
物理外观 | A solid |
CAS号 | 524-95-8 |
分子式 | C14H16BNO |
分子量 | 225.1 |
小分子别名 | 2-Aminoethyl diphenylborinate |
化学名称 | 2-((diphenylboryl)oxy)ethanamine |
溶解度 | insoluble in H2O; ≥27.85 mg/mL in EtOH; ≥9.4 mg/mL in DMSO |
SMILES | NCCOB(C1=CC=CC=C1)C2=CC=CC=C2 |
存储条件 | 室温 |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. Hui Liu, Xuenan Li, et al. "Elaidic acid leads to mitochondrial dysfunction via mitochondria-associated membranes triggers disruption of mitochondrial calcium fluxes." Food Science and Human Wellness Volume 13 Issue 1, January 2024
- 2. Jiayin Chang, Shihai Yan, et al. "The interaction between Hsp90-mediated unfolded protein response and autophagy contributes to As3+/Se4+ combination-induced apoptosis of acute promyelocytic leukemia cells." Toxicol Appl Pharmacol. 2023 May 15:467:116511. PMID: 37031722
- 3. Ziping Cheng, Yangjie Liu, et al. "Lansoprazole-Induced Osteoporosis via IP3R and SOCE Mediated Calcium Signaling Pathway." Mol Med. 2022 Feb 19;28(1):21. PMID: 35183103
- 4. Yingying Zhang, Jiaqi Tang, et al. "Prenatal hypoxia induced ETBR activation and abnormal ROS signalling in pulmonary artery cells of rat offspring." Reprod Toxicol. 2021 Oct;105:91-100. PMID: 34478853
- 5. Yinghui Cui, Fenglan Chu, et al. "Role of serosal TRPV4-constituted SOCE mechanism in secretagogues-stimulated intestinal epithelial anion secretion." Front Pharmacol. 2021 Jul 14;12:684538. PMID: 34335254
- 6. Hong F, Wu S, et al. "TRPM7 Upregulate the Activity of SMAD1 through PLC Signaling Way to Promote Osteogenesis of hBMSCs." Biomed Res Int. 2020;2020:9458983. PMID: 32596398