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  2. Membrane Transporter/Ion Channel Autophagy
  3. CFTR Autophagy
  4. GLPG1837

GLPG1837 是一種有效的，可逆的 CFTR 增強劑，對 CFTR 的 突變體 F508del 和 G551D 的 EC50 值分別為 3 nM 和 339 nM。

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GLPG1837 Chemical Structure

GLPG1837 Chemical Structure

CAS No. : 1654725-02-6

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1 mg ￥394
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5 mg ￥900
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10 mg ￥1500
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25 mg ￥2475
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50 mg ￥4100
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Customer Review

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

IC50 & Target

EC50: 3 nM (F508del CFTR), 339 nM (G551D CFTR)[1]
體外研究
(In Vitro)

GLPG1837 is a potent CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM[1]. GLPG1837 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2～2 μM[2].

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

348.42

Formula

C16H20N4O3S
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 250 mg/mL (717.52 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8701 mL 14.3505 mL 28.7010 mL
5 mM 0.5740 mL 2.8701 mL 5.7402 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻
Cell Assay
[1]

CFBe41o- cells are cultured in Eagle’s Minimal Essential Medium (MEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, 1%?l-glutamine, and 500 μg/mL hygromycin B. The cells are grown on culture flasks coated with 0.01% bovine serum albumin (BSA), 30 μg/mL Purecol, and 0.001% human fibronectin. CFBe41o- cells are transduced with adenoviruses containing F508del CFTR and YFP (H148Q/I152L/F47L). HEK293 cells are cultured in Dulbecco’s Modified Eagle Medium (DMEM) supplemented with 10% FBS and 1% penicillin/streptomycin. HEK293 cells are transfected with plasmids containing G551D, G178R, S549N, R117H, CFTR, and YFP (H148Q/I152L/F47L). Directly after transfection, the HEK293 cells are seeded in black 96-well plates coated with poly-d-lysine at a density of 70000 cells per well. The next day, cells are incubated for 24 h at 27°C (CFBE41o?) or 37°C (HEK293). Then cells are treated for 10 min with 10 μM forskolin and the desired concentration of potentiator at room temperature.

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

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8701 mL 14.3505 mL 28.7010 mL 71.7525 mL
5 mM 0.5740 mL 2.8701 mL 5.7402 mL 14.3505 mL
10 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
15 mM 0.1913 mL 0.9567 mL 1.9134 mL 4.7835 mL
20 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
25 mM 0.1148 mL 0.5740 mL 1.1480 mL 2.8701 mL
30 mM 0.0957 mL 0.4783 mL 0.9567 mL 2.3917 mL
40 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
50 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4350 mL
60 mM 0.0478 mL 0.2392 mL 0.4783 mL 1.1959 mL
80 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8969 mL
100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7175 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.

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產(chǎn)品名稱：
GLPG1837
目錄號：
HY-111099
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