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CFTR

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Oridonin (Isodonol)

Catalog No. A10675
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CFTR 抑制剂

Oridonin (Isodonol)是一种从鼠李木中分离出来的Entkaurane二萜类化合物，是一种重要的传统中草药。了解更多

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CFTRinh-172

Catalog No. A12897
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CFTR 抑制剂

CFTRinh-172是电压无关的选择性CFTR抑制剂。在2分钟内可逆地抑制CFTR短路电流的 Ki 值为300 nM。了解更多

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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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KM 11060

Catalog No. A15843
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F508del-CFTR trafficking corrector

KM 11060纠正了F508del-CFTR的运输，增加了质膜上功能性CFTR的量（?75％）并抑制了PDE5的活性。了解更多

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PG 01

Catalog No. A18315
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CFTR potentiator

PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. PG 01 is effective on G970R although with a significant decrease in potency relative to E193K and δF508. 了解更多

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CFTR corrector 2

Catalog No. A18528
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CFTR corrector

CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933. 了解更多

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GLPG2451

Catalog No. A18919
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CFTR potentiator

GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM. 了解更多

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Ivacaftor benzenesulfonate

Catalog No. A15132
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CFTR potentiator

Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment. 了解更多

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Ivacaftor hydrate

Catalog No. A15133
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CFTR potentiator

Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment. 了解更多

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PTC124 (Ataluren)

Catalog No. A10758
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CFTR 抑制剂

PTC124也称为Ataluren，是CFTR-G542X无意义等位基因抑制剂。了解更多

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- L Kadunc, .et al. Increased Gene Translation Stringency in Mammalian Cells by Nonsense Suppression at Multiple Permissive Sites With a Single Noncanonical Amino Acid, FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. A flow cytometry-based reporter assay identifies macrolide antibiotics as nonsense mutation read-through agents, J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
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VX-770 (Ivacaftor)

Catalog No. A10985
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CFTR activator

VX-770 (Ivacaftor)被称为CFTR增强剂，靶向作用于G551D-CFTR和F508del-CFTR，在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。了解更多

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- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
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VX-809 (Lumacaftor)

Catalog No. A10986
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CFTR modulator

VX-809 (Lumacaftor)是用于治疗囊性纤维化（CF）的第二种口服研究候选化合物，通过促进突变型CFTR(F508del-CFTR)的成熟，从而纠正囊性纤维症中常见的CFTR突变，在fisher大鼠甲状腺细胞中EC50为0.1 μM。了解更多

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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
- Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
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VX-661

Catalog No. A12519
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CFTR corrector

VX-661是另一种正在开发中的用于治疗囊性纤维化的囊性纤维化跨膜电导调节器（CFTR）校正器。了解更多

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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
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Glyburide

Catalog No. A10433
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K+ channel and CFTR Cl- channel blocker

Glyburide (Glibenclamide) 是一种抗糖尿病化合物，是一类磺脲类药物。了解更多

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IOWH032

Catalog No. A13511
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CFTR 抑制剂

IOWH032是CFTR抑制剂。了解更多

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CFTR-Inhibitor-II

Catalog No. A13723
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CFTR 抑制剂

CFTR inhibitor II,也称为GlyH-101，是一种甘氨酸酰肼，可选择性和可逆地阻断CFTR通道（Ki = 4.3 uM）。了解更多

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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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PPQ-102

Catalog No. A13000
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CFTR chloride channel 抑制剂

PPQ-102是一种化合物，其靶向cftr的胞内核苷酸结合结构域，并以电压依赖性和可逆的方式抑制cftr介导的氯离子电流。了解更多

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