2. Membrane Transporter/Ion Channel
  3. CFTR
  4. PG01

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。

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PG01 Chemical Structure

PG01 Chemical Structure

CAS No. : 853138-65-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4448
In-stock
1 mg ￥1550
In-stock
5 mg ￥4600
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

PG01 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin[1][2].

IC50 & Target

CFTR[1]
体外研究
(In Vitro)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PG01 相关抗体:
体内研究
(In Vivo)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

439.55

Formula

C28H29N3O2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 43.96 mg/mL (100.01 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2751 mL 11.3753 mL 22.7505 mL
5 mM 0.4550 mL 2.2751 mL 4.5501 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥98.0%

COA (285 KB)

产品使用指南 (1538 KB)
参考文献

PG01 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 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 0.4550 mL 2.2751 mL 4.5501 mL 11.3753 mL
10 mM 0.2275 mL 1.1375 mL 2.2751 mL 5.6876 mL
15 mM 0.1517 mL 0.7584 mL 1.5167 mL 3.7918 mL
20 mM 0.1138 mL 0.5688 mL 1.1375 mL 2.8438 mL
25 mM 0.0910 mL 0.4550 mL 0.9100 mL 2.2751 mL
30 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8959 mL
40 mM 0.0569 mL 0.2844 mL 0.5688 mL 1.4219 mL
50 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1375 mL
60 mM 0.0379 mL 0.1896 mL 0.3792 mL 0.9479 mL
80 mM 0.0284 mL 0.1422 mL 0.2844 mL 0.7110 mL
100 mM 0.0228 mL 0.1138 mL 0.2275 mL 0.5688 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PG01853138-65-5PG 01PG-01CFTRCystic fibrosis transmembrane conductance regulatorCysticfibrosisCl-channelpotentiatorforskolin-activatedcurrentE193KG970RcAMPInhibitorinhibitorinhibit

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目录号：
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