2. Membrane Transporter/Ion Channel
  3. Chloride Channel
  4. ANO1-IN-5

ANO1-IN-5 是一种具有口服活性的 ANO1 抑制剂，IC50 为 4.57 μM。ANO1-IN-5 对 α1A-、α1B- 和 α1D-AR 的选择性分别是 ANO1 的 118 倍、642 倍和 10000 倍。ANO1-IN-5 对破骨细胞的分化和功能有显著的抑制作用。ANO1-IN-5 可用于骨质疏松症的研究。

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ANO1-IN-5

ANO1-IN-5 Chemical Structure

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ANO1-IN-5 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

ANO1-IN-5 is an orally active ANO1 inhibitor with an IC50 of 4.57 μM. J ANO1-IN-5 demonstrates 118-, 642-, and 10000-fold selectivity over α1A-,α1B-, andα1D-AR, respectively. ANO1-IN-5 exhibits significant inhibitory effects on osteoclast differentiation and function. ANO1-IN-5 can used for the study of osteoporosis[1].

体外研究
(In Vitro)

ANO1-IN-5 (Compound 10) (20 μM, 5 d) 显著抑制 TRAP+ 多核破骨细胞的形成[1]。
ANO1-IN-5 (Compound 10) (20 μM) 显著降低破骨细胞标志基因，例如 NFATc1、Acp5、Ctsk 和 Mmp9 的 mRNA 表达[1]。
ANO1-IN-5 通过抑制 ANO1 直接抑制破骨细胞的 Cl- 分泌功能[1]。

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

ANO1-IN-5 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. Tmax 0.083 h
Rat 10 mg/kg p.o. Tmax 4.00 h
Rat 1 mg/kg i.v. T1/2 1.62 h
Rat 10 mg/kg p.o. T1/2 2.76 h
Rat 1 mg/kg i.v. Cmax 2513 ng/mL
Rat 10 mg/kg p.o. Cmax 331.3 ng/mL
Rat 1 mg/kg i.v. AUC0-t 1520 ng·h/mL
Rat 10 mg/kg p.o. AUC0-t 2460 ng·h/mL
Rat 1 mg/kg i.v. AUC0-∞ 1520 ng·h/mL
Rat 10 mg/kg p.o. AUC0-∞ 2469 ng·h/mL
Rat 1 mg/kg i.v. ClF_obs 0.64 L/h/kg
Rat 10 mg/kg p.o. ClF_obs 4.11 L/kg
Rat 1 mg/kg i.v. Vz-F_obs 0.77 L/kg
Rat 10 mg/kg p.o. F 16.2 %
体内研究
(In Vivo)

ANO1-IN-5 (Compound 10) (3-30 mg/kg，灌胃，每日一次，持续 4 周) 可有效缓解卵巢切除术后的疼痛 (OVX) 引起的骨质流失，显著改善小鼠的骨小梁量和形态参数[1]。

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

Animal Model: OVX-induced bone loss model established in 6-8-week-old female mice[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Intragastrical administration (i.g.), once daily for 4 weeks
Result: Exhibited higher bone volume/total volume (BV/TV), trabecular number (Tb.N), and trabecular thickness (Tb.Th) values, but a lower trabecular separation (Tb.Sp) in a dose-dependent manner.
reduced the level of the bone resorption marker CTX-1 in the serum, and downregulated the expression of osteoclast marker genes in the bone tissue.
分子量

447.59

Formula

C23H33N3O4S
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

ANO1-IN-5 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:

ANO1-IN-5Chloride ChannelCl− ChannelsOsteoporosisTamsulosinOvariectomyTMEM16AInhibitorinhibitorinhibit

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