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23

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2355 CFTR(inh)-172

CFTRinh 172,CFTR Inhibitor-172,CFTRinh-172,CFTRinh172

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
CFTR(inh)-172 (CFTR Inhibitor-172) 是一种不依赖电压的选择性 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。
T1874 PPQ-102

PPQ102,CFTR Inhibitor,PPQ 102

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
PPQ-102 (CFTR Inhibitor) 是一种CFTR 抑制剂,可以完全抑制CFTR 氯化物电流,IC50为90 nM。
T5312 CFTR corrector 2

FDL169

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
CFTR corrector 2 (FDL169) 是一种新型有效的囊性纤维化跨膜电导调节因子(CFTR)调节剂,用于治疗携带 F508del 突变的囊性纤维化患者。
T2451 GlyH-101

GlyH 101

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
GlyH-101 是一种可渗透入细胞的 CFTR 阻断剂,Ki 为1.4 uM。
T3135 KM11060

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
KM11060 是 F508del-CFTR 运输缺陷的新型校正剂,可纠正 F508del-CFTR 运输,增加质膜上功能性 CFTR 的数量。它可用于 F508del-CFTR 加工缺陷的研究和囊性纤维化治疗剂的开发。
T1805 Ataluren

PTC124

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
Ataluren (PTC124) 是一种可口服的 CFTR-G542X 无义等位基因抑制剂。
T14935 Elexacaftor

VX-445

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
Elexacaftor (VX-445) 是一种囊性纤维化跨膜电导调节因子 (CFTR) 校正剂。它促进CFTR 的加工和转运,增加细胞表面CFTR 的数量。
T16681 Nesolicaftor

PTI-428

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
Nesolicaftor (PTI-428) 特异性增强囊性纤维化跨膜电导调节蛋白合成。
T9499 Icenticaftor

QBW251

CFTR Membrane transporter/Ion channel
Icenticaftor (QBW251) 是一种具有口服活性CFTR 通道增强剂,可用于慢性阻塞性肺疾病 (COPD) 和囊性纤维化研究,对F508del 和G551D CFTR 的EC50分别为 79 和 497 nM。
T7083 GLPG1837

ABBV-974

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
GLPG1837 (ABBV-974) 是一种有效的 CFTR 增强剂,对其 F508del 和 G551D 的 EC50 分别为 3 nM 和 339 nM。
T2486 IOWH-032

IOWH032,IOWH 032

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
IOWH-032 (IOWH032) 是一种合成 CFTR 抑制剂,可用于研究治疗霍乱、腹泻和分泌性腹泻,在T84和CHO-CFTR 细胞实验中IC50为1.01 uM。
T10591 BPO-27 racemate

BPO-27 (racemate)

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
BPO-27 racemate (BPO-27(racemate)) 是一种CFTR 抑制剂,IC50为8 nM。
T2588 Ivacaftor

Ivacaftor (VX-770),VX-770,依伐卡托

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
Ivacaftor (VX-770) 是一种 CFTR 增强剂,靶向G551D-CFTR 和F508del-CFTR 的EC50分别为100 和 25 nM。
T2595 Lumacaftor

鲁玛卡托,VX-809,VRT 826809

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
Lumacaftor (VRT 826809) 是一种 CFTR 调节剂,可纠正 CFTR 蛋白的折叠和运输。它增强了 FRT 细胞中 F508del-CFTR 蛋白的成熟,EC50为100 nM。
T1634 Glibenclamide

格列本脲,Glyburide

Potassium Channel; Mitochondrial Metabolism; CFTR; P-gp; Autophagy Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience
Glibenclamide (Glyburide) 是一种具有口服活性的 ATP 敏感的 K+通道抑制剂,可研究糖尿病和肥胖。它抑制 P-糖蛋白,可直接结合并阻断 KATP 的 SUR1亚基并抑制囊性纤维化跨膜传导调节蛋白。它通过诱导膜离子通透性干扰线粒体生物能,可诱导自噬。
T2263 Tezacaftor

VX661,1-(2,2-二氟-1,3-苯并二氧戊环-5-基)-N-[1-[(2R)-2,3-二羟基丙基]-6-氟-2-(2-羟基-1,1-二甲基乙基)-1H-吲哚-5-基]-环丙烷甲酰胺

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
Tezacaftor (VX661) 是一种小分子,可用作囊性纤维化跨膜电导调节器基因功能的校正剂。
T26955 Cavosonstat

N91115,N 91115,N-91115

GSNOR; CFTR Membrane transporter/Ion channel; Metabolism
Cavosonstat (N91115) 是一种口服活性 S-亚硝基谷胱甘肽还原酶(GSNOR)抑制剂,可促进囊性纤维化跨膜传导调节器(CFTR)成熟和质膜稳定。
T10591L (R)-BPO-27

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
(R)-BPO-27 是一种具有口服活性和高效性的 ATP 竞争性 CFTR 抑制剂(IC50:4 nM),可用于研究腹泻和多囊肾。
T61702 SRI-37240

SRI-37240 is a powerful inhibitor of premature termination codons (PTCs). It effectively suppresses CFTR nonsense mutations and induces changes in cellular translation termination at PTCs in HEK293T cells. Additionally, when combined with G418, SRI-37240 restores CFTR function in primary bronchial epithelial cells [1].
T70232 3,4-Dephostatin

3,4-Dephostatin is an inhibitor of the interactions of CFTR-associated ligand (CAL) and PSD-95/Dlg1/ZO-1 (PDZ) domain.
T69658 Ethyl-3,4-dephostatin

Ethyl-3,4-dephostatin is a novel inhibitor of the interactions of CFTR-associated ligand and PSD-95/Dlg1/ZO-1 domain.
T35883 RNF5 inhibitor inh-02

RNF5 inhibitor inh-02

RNF5 inhibitor inh-02, a potent E3 ubiquitin ligase RNF5/RMA1 inhibitor, demonstrates significant efficacy in rescuing F508del-CFTR with an EC50 of 2.2 uM in bronchial epithelial cells homozygous for the F508del mutation. This compound is valuable for cystic fibrosis research[1].
T71303 Flufenamic Acid-d4

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear...

化合物

CFTR(inh)-172
Cat.No: T2355
Synonym: CFTRinh 172,CFTR Inhibitor-172,CFTRinh-172,CFTRinh172
Target: CFTR, Autophagy
PPQ-102
Cat.No: T1874
Synonym: PPQ102,CFTR Inhibitor,PPQ 102
Target: CFTR, Autophagy
CFTR corrector 2
Cat.No: T5312
Synonym: FDL169
Target: CFTR, Autophagy
GlyH-101
Cat.No: T2451
Synonym: GlyH 101
Target: CFTR, Autophagy
KM11060
Cat.No: T3135
Synonym:
Target: CFTR, Autophagy
Ataluren
Cat.No: T1805
Synonym: PTC124
Target: CFTR, Autophagy
Elexacaftor
Cat.No: T14935
Synonym: VX-445
Target: CFTR, Autophagy
Nesolicaftor
Cat.No: T16681
Synonym: PTI-428
Target: CFTR, Autophagy
Icenticaftor
Cat.No: T9499
Synonym: QBW251
Target: CFTR
GLPG1837
Cat.No: T7083
Synonym: ABBV-974
Target: CFTR, Autophagy
IOWH-032
Cat.No: T2486
Synonym: IOWH032,IOWH 032
Target: CFTR, Autophagy
BPO-27 racemate
Cat.No: T10591
Synonym: BPO-27 (racemate)
Target: CFTR, Autophagy
Ivacaftor
Cat.No: T2588
Synonym: Ivacaftor (VX-770),VX-770,依伐卡托
Target: CFTR, Autophagy
Lumacaftor
Cat.No: T2595
Synonym: 鲁玛卡托,VX-809,VRT 826809
Target: CFTR, Autophagy
Glibenclamide
Cat.No: T1634
Synonym: 格列本脲,Glyburide
Target: Potassium Channel, Mitochondrial Metabolism, CFTR, P-gp, Autophagy
Tezacaftor
Cat.No: T2263
Synonym: VX661,1-(2,2-二氟-1,3-苯并二氧戊环-5-基)-N-[1-[(2R)-2,3-二羟基丙基]-6-氟-2-(2-羟基-1,1-二甲基乙基)-1H-吲哚-5-基]-环丙烷甲酰胺
Target: CFTR, Autophagy
Cavosonstat
Cat.No: T26955
Synonym: N91115,N 91115,N-91115
Target: GSNOR, CFTR
(R)-BPO-27
Cat.No: T10591L
Synonym:
Target: CFTR, Autophagy
SRI-37240
Cat.No: T61702
Synonym:
Target:
3,4-Dephostatin
Cat.No: T70232
Synonym:
Target:
Ethyl-3,4-dephostatin
Cat.No: T69658
Synonym:
Target:
RNF5 inhibitor inh-02
Cat.No: T35883
Synonym: RNF5 inhibitor inh-02
Target:
Flufenamic Acid-d4
Cat.No: T71303
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2S1837 Steviol

甜菊醇,NSC 226902,Hydroxydehydrostevic acid

Others Others
Steviol (NSC-226902) 是一种甜菊糖甙的主要代谢物。它能降低 AQP2 的表达,并促进 AQP2 的降解,从而减缓肾囊肿的生长。
TN1834 Kobusin

去甲槟郎碱,自旋七叶素

Others; NOS; NF-κB Immunology/Inflammation; NF-κB; Others
Kobusin, a Calmodulin inhibitor, shows mild antiplasmodial,anti-inflammatory, and cytotoxic activities; it may be beneficial for the treatment of neuro-inflammatory diseases through the inhibition of iNOS expression and peroxynitrite scavenging potential. Kobusin can mildly reduce gastrointestinal motility in mice, it activates CFTR and CaCCgie chloride channel activities in mouse colonic epithelia and shows inhibitory effects toward ANO1/CaCC-mediated short-circuit currents in ANO1/CaCC-express...

天然产物

Steviol
Cat.No: T2S1837
Synonym: 甜菊醇,NSC 226902,Hydroxydehydrostevic acid
Target: Others
Kobusin
Cat.No: TN1834
Synonym: 去甲槟郎碱,自旋七叶素
Target: Others, NOS, NF-κB
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