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  • Br-PBTC
Br-PBTC的可视化放大

Br-PBTC

Br-PBTC是一种有效的、2/4亚型选择性的nAChRs(烟碱乙酰胆碱受体)正变质调节剂,其α2β2、α2β4、α4β2、(α4β2)2α4 β2和(α4β2)2β2 EC50范围为0.1~0.6 μM。

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Br-PBTC的二维码
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  • 货号: ajcf25518
  • CAS: 1839519-57-1
  • 别名:
  • 分子式: C14H15BrN2OS
  • 分子量: 339.25
  • 纯度: >98%
  • 溶解度:
  • 储存: Store at -20°C
  • 库存: 现货

Background

Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.

Br-PBTC (0.01~10 μM; HEK cells) selectively affects 2 and 4 subunits. Br-PBTC (3 μM; oocytes) has greater effects on nAChRs with 2 subunits over those with 4 subunits. Br-PBTC (0.01~10 μM; 15 minutes; HEK cells) can increase channel activation by a maximal concentration of ACh. Br-PBTC (3 μM; 50 seconds; oocytes) increased ACh activation of α4β2 nAChRs by 385± 61 %. Br-PBTC (3 μM;oocytes) reactivates short term desensitized nAChRs expressed. Br-PBTC (3 μM; 500 seconds; HEK cells) reactivates short term desensitized (α4β2)2α4 and(α4β2)2β2 nAChRs expressed. Br-PBTC (0.1~100 μM;0~140 seconds; HEK cells) reactivates long term desensitized nAChRs[1].

参考文献:
[1]. Wang J, et al. A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an α Subunit. J Biol Chem. 2015;290(48):28834-28846.

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