23
2
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... |
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... |