2. Membrane Transporter/Ion Channel
  3. CFTR
  4. I1421

I1421 是囊性纤维化跨膜传导调节器 (CFTR) 的激活剂，对 WT CFTR 电流的 EC50 为 64 nM。I1421 还可以变构激活多种导致囊性纤维化 (CF) 的突变体，具有较好的体内效力，其在小鼠中的口服生物利用度为 60%，对应的半衰期为 75 min。I1421 与 Elexacaftor (HY-111772) 有协同作用，可共同增强 CFTR 电流。

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I1421 Chemical Structure

I1421 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
1 mg ￥1600
7 - 9 周
5 mg ￥4000
7 - 9 周
10 mg 现货 7 - 9 周
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

I1421 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents[1].

IC50 & Target

EC50: 64 nM (WT CFTR)[1]
体内研究
(In Vivo)

I1421 (10 mg/kg; ip, po, sc; 单剂量) 在 C57BL/6 小鼠中的吸收速率快，进行 3 种不同给药方式后，腹膜内和口服给药后 15 min 观察到的最大血浆浓度 (Cmax) 分别为 7.4 μM 和 3.4 μM，同时腹膜内给药后的血浆水平高于其他两种给药途径[1]。
I1421 (3 mg/kg; iv, po; 单剂量) 在进行口服和静脉注射的小鼠中，生物利用度为 60%，但口服 T1/2 较短（75 min）[1]。

C57BL/6 小鼠中的药代动力学分析[1]

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) T1/2 (h) CL (mL/min/kg) Vss (1/kg) F (%)
IP 10 0.25 2617 2145 2.16 - - -
PO 10 0.25 1181 1211 1.24 - - 60
SC 10 0.50 625 1512 1.36 - - -
IV 3 - 2354 610 1.78 81.51 2.49 -

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

343.35

Formula

C18H18FN3O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Animal Administration

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

I1421 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

I1421I 1421I-1421CFTRCystic fibrosis transmembrane conductance regulatorABC transporteranion channelinhibitorslarge-scale dockingligand discoverypotentiatorsInhibitorinhibitorinhibit

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目录号：
HY-158991
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