Membrane Transporters/Ion Channels
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Oct3/4 Inducer
O4I1在10 uM和20 uM下分别使HEK293细胞中的Oct3/4 mRNA水平增加2.5倍和4倍。
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Oct4 activator
OAC2是一种Oct4激活化合物，可通过Oct4基因启动子激活表达。
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Oct3/4 inducer
O4I2是Oct3/4的有效诱导剂。O4I2在执行Oct3/4表达方面显示出高活性。O4I2是一类适用于iPSC生成的新型小分子。
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NCX inhibitor
ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively.
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Na+/Ca2+ Exchanger 抑制剂
KB-R7943 mesylate是一种在表达NCX1的细胞中具有Na+/Ca2+交换反向模式的细胞渗透性强效选择性NCKX抑制剂。
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NCX 抑制剂
SEA0400是Na+-Ca2+交换剂的新型选择性抑制剂，IC50为5-33 nM（抑制培养的神经元，星形胶质细胞和小胶质细胞中Na+依赖的Ca2+吸收。
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- Wakana Shoda, .et al. Sodium-calcium exchanger 1 is the key molecule for urinary potassium excretion against acute hyperkalemia, PLoS One, 2020, 15(6): e0235360 PMID: 32603346
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Na+/Ca2+ exchange 抑制剂
CGP 37157是苯并硫氮平，可作为线粒体钠钙交换剂的选择性抑制剂（在分离的线粒体中IC50 = 0.36 μM）。
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Na+/Ca2+ exchanger (NCX) 抑制剂
ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively.
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BCRP 抑制剂
ko 143是有效的选择性乳腺癌耐药蛋白多药转运蛋白(BCRP)抑制剂，EC90值为26 nM。
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BCRP/ABCG2 抑制剂
YHO-13177是一种有效且特异性的乳腺癌抗性蛋白（BCRP/ABCG2）抑制剂。
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BCRP inhibitor
YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
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NHE3 抑制剂
Tenapanor充当钠-质子交换器NHE3的抑制剂。这种抗转运蛋白在肾脏和肠道中发现，通常起到调节机体吸收和分泌的钠水平的作用。
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- Xingjie Tan, .et al. The Na+/H+ exchanger NHE3 inhibitor tenapanor prevents intestinal obstructions in CFTR-deleted mice, Authorea, 2022, May 25
- Kunyan Zhou, .et al. Functional characterization of the sodium/hydrogen exchanger 8 and its role in proliferation of colonic epithelial cells, Am J Physiol Cell Physiol, 2021, Sep 1;321(3):C471-C488 PMID: 34288721
- Qinghai Tan, .et al. Inhibition of Na + /H + exchanger isoform 3 improves gut fluidity and alkalinity in cystic fibrosis transmembrane conductance regulator-deficient and F508del mutant mice, Br J Pharmacol, 2021, Mar;178(5):1018-1036 PMID: 33179259
- Y Liu, .et al. Deciphering Ion Transporters, Kinases and PDZ-adaptor Molecules That Mediate Guanylate Cyclase C Agonist-Dependent Intestinal Fluid Loss in Vivo, Biochem Pharmacol, 2020, May 16;178:114040 PMID: 32422138
- Yu Y, .et al. Expression, Localization and Functional Activity of the Major Na+/H+ Exchange Isoforms Expressed in the Intestinal Cell Line Caco-2BBe, Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thammayon N, .et al. Na+/H+ exchanger 3 inhibitor diminishes the amino-acid-enhanced transepithelial calcium transport across the rat duodenum, Amino Acids, 2017, Apr;49(4):725-734 PMID: 27981415
- Charoenphandhu N, .et al. Na+/H+ exchanger 3 inhibitor diminishes hepcidin-enhanced duodenal calcium transport in hemizygous β-globin knockout thalassemic mice, Mol Cell Biochem, 2017, Mar;427(1-2):201-208 PMID: 27995414
- Jantarajit W, .et al. CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels, Am J Physiol Cell Physiol, 2017, Jul 1;313(1):C118-C129 PMID: 28490422
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NHE-1 inhibitor
Rimeporide(EMD-87580)是Na+/H+交换剂（NHE-1）的有效和选择性抑制剂。
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NHE3 抑制剂
NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
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VMAT2 抑制剂
GZ-793A是囊泡单胺转运蛋白2 (VMAT2)的选择性抑制剂，它将单胺神经递质从细胞胞质溶胶转运到突触小泡中。
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VMAT2 抑制剂
Valbenazine是一种有效的选择性VMAT2抑制剂。
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VMAT2 inhibtior
NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM.
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