Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PG01是一种有效的CFTR Cl-通道增效剂,PG01对 ΔF508(Ka 为 0.3 μM)有效。PG01 对 E193K,G970R 和 G551D (CFTR 突变体)也 有效,Kd 值分别为 0.22 μM,0.45 μM 和 1.94 μM 。PG01在加入Forskolin 后可增加ΔF508-CFTR Cl-电流,纠正CFTR 突变体的门控缺陷。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,210 | 现货 | ||
5 mg | ¥ 3,430 | 现货 | ||
10 mg | ¥ 4,900 | 现货 | ||
25 mg | ¥ 7,830 | 现货 | ||
50 mg | ¥ 10,500 | 现货 | ||
100 mg | ¥ 14,200 | 现货 | ||
500 mg | ¥ 28,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,480 | 现货 |
产品描述 | PG01 is a potent CFTR Cl-channel potentiator, effective against ΔF508 (Ka 0.3 μM), and also against E193K, G970R and G551D (CFTR mutants), with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively.PG01 increases ΔF508-CFTR Cl- currents upon addition of forskolin. F508-CFTR Cl-current upon addition of Forskolin, correcting the gating defect of CFTR mutants. |
靶点活性 | E193K:0.22 μM(Kd), G970R:0.45 μM(Kd), CFTR (G551D):1.94 μM(Kd) |
体外活性 | PG01 produces large currents in both G551D- and G1349D-CFTR expressing cells. PG01 itself does not activate ∆F508-CFTR, produces substantial ∆F508-CFTR Cl- current after the addition of 0.5 and 2 μM Forskolin. PG01 (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. The currents are sensitive to CFTRinh-172 and are not seen in nontransfected cells.[1] |
体内活性 | Microsome metabolism studies and rat pharmacokinetic analysis suggest a significantly more rapid metabolism of PG01 than SF-03. 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 the volume of distribution 4 L.[1] |
别名 | Phenylglycine-01 |
分子量 | 439.55 |
分子式 | C28H29N3O2 |
CAS No. | 853138-65-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (68.25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2751 mL | 11.3753 mL | 22.7505 mL | 56.8764 mL |
5 mM | 0.455 mL | 2.2751 mL | 4.5501 mL | 11.3753 mL | |
10 mM | 0.2275 mL | 1.1375 mL | 2.2751 mL | 5.6876 mL | |
20 mM | 0.1138 mL | 0.5688 mL | 1.1375 mL | 2.8438 mL | |
50 mM | 0.0455 mL | 0.2275 mL | 0.455 mL | 1.1375 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PG01 853138-65-5 Membrane transporter/Ion channel CFTR PG 01 PG-01 Phenylglycine-01 Inhibitor inhibitor inhibit