货号	规格	价格	上海	北京	珠海	重庆	武汉
T80805-5mg促销	99.80%	￥1500.00 ￥1200.00 T80805-5mg ￥1200.00 现货	6 6	-	-	-	-
T80805-10mg促销	99.80%	￥2400.00 ￥1920.00 T80805-10mg ￥1920.00 现货	6 6	-	-	-	-
T80805-25mg促销	99.80%	￥4500.00 ￥3600.00 T80805-25mg ￥3600.00 现货	5 5	-	-	-	-
T80805-100mg促销	≥98%	￥8520.00 ￥6810.00 T80805-100mg ￥6810.00 3-5天	0 货期：3-5天	-	-	-	-

大包装询价收藏产品

加入购物车

产品描述：

PG01 是一种有效的 CFTR Cl- 通道增效剂。PG01 对 E193K，G970R 和 G551D (CFTR突变体) 有效，Kd 值分别为 0.22 μM，0.45 μM 和 1.94 μM。PG01对 ΔF508（Ka 为 0.3 μM）也有效。PG01 在添加 Forskolin 后增加 ΔF508-CFTR Cl- 电流。

靶点：

CFTR

体外研究：

PG01 itself does not activate ∆F508-CFTR, produces substantial ∆F508-CFTR Cl- current after the addition of 0.5 and 2 μM Forskolin. PG01 at 100 nM strongly stimulates channel activity with multiple channel openings observed. The apparent Kd for PG01 for G551D-CFTR activation is 1 μM, approximately 100-fold better than that of genistein. The potency for activation G1349D-CFTR by PG01 is even better at 40 nM. PG01 produces large currents in both G551D- and G1349D-CFTR expressing cells. The currents are sensitive to CFTRinh-172 and are not seen in nontransfected cells.

体内研究：

Pharmacokinetic analysis of PG01 in rats is done by serial measurements of plasma concentrations after single bolus infusions (5 mg/kg). PG01 pharmacokinetics fitted a two-compartment model with half-times of ＜5 min and 130 min with volume of distribution 4 L. Microsome metabolism studies and rat pharmacokinetic analysis suggests significantly more rapid metabolism of PG01 than SF-03.

参考文献：

1. Pedemonte N, et al. Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol Pharmacol. 2005 May;67(5):1797-807.

2. Caputo A, et al. Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J Pharmacol Exp Ther. 2009 Sep;330(3):783-91.

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.275 ml	11.375 ml	22.75 ml
5 mM	0.455 ml	2.275 ml	4.55 ml
10 mM	0.228 ml	1.138 ml	2.275 ml
50 mM	0.046 ml	0.228 ml	0.455 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置