| CAS NO: | 524-95-8 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 225.1 |
| Cas No. | 524-95-8 |
| Formula | C14H16BNO |
| Solubility | insoluble in H2O; ≥27.85 mg/mL in EtOH; ≥9.4 mg/mL in DMSO |
| Chemical Name | 2-((diphenylboryl)oxy)ethanamine |
| Canonical SMILES | NCCOB(C1=CC=CC=C1)C2=CC=CC=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 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。溶液形式一般不宜长期储存，请尽快用完。 |
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.
| 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. | |
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