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39

抑制剂 & 化合物

8

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12608 QX-314 chloride

Sodium Channel Membrane transporter/Ion channel
QX-314 chloride 是钠离子通道电荷阻滞剂,具有膜不渗透性。
T8960 MONNA

Chloride channel Membrane transporter/Ion channel
MONNA 是 TMEM16A (Anoctamin-1)阻滞剂,IC50为 80 nM。它在氯离子存在或不存在的情况下诱导啮齿动物抵抗动脉的血管舒张。
T15192 Eact

Chloride channel Membrane transporter/Ion channel
Eact 是一种选择性和有效的 TMEM16A 激活剂,可直接激活感觉伤害感受器中的 TRPV1 通道,还会产生瘙痒、急性伤害感受和热过敏。
T7638 NPPB

Chloride channel Membrane transporter/Ion channel
NPPB 是外向整流氯化物通道阻断剂,IC50 为 80 nM。
T10979 DCPIB

Potassium Channel; Chloride channel Membrane transporter/Ion channel
DCPIB 是选择性可逆体积调节性阴离子通道抑制剂,抑制肿胀激活氯电流,在 CPAE 细胞中,IC50值为 4.1 μM。它能够电压依赖性激活钾离子通道 TREK1 和 TRAAK,抑制 TRESK、TASK1 和 TASK3的 IC50值分别为 0.14、0.95 和 50.72 μM。
T7538 Tetraethylammonium chloride

Potassium Channel Membrane transporter/Ion channel
Tetraethylammonium chloride 是非选择性钾通道阻滞剂。它是有机阳离子转运蛋白的良好底物,并具有抗肿瘤特性。
T23213 QX-222 chloride

QX 222,Lidocaine N-Methyl Hydrochloride

Sodium Channel Membrane transporter/Ion channel
QX-222 chloride (Lidocaine N-Methyl Hydrochloride) 是 Lignocaine 的一种三甲基类似物,是有效的 Na+通道阻滞剂。
T8391 Cesium chloride

氯化铯,CsCl

Potassium Channel Membrane transporter/Ion channel
Cesium chloride (CsCl) 是一种钾通道抑制剂,可以防止 Alloxan 引起的 Na+转运减少。Cesium chloride 可以诱发心律失常。
T0979 Dequalinium chloride

Dequafungan,地喹氯铵,Danical,Decabis

Potassium Channel; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel
Dequalinium chloride (Decabis) 是一种apamin 敏感型的钾离子通道选择性阻断剂。
T16346 NS1652

Chloride channel Membrane transporter/Ion channel
NS1652 是可逆阴离子电导抑制剂,在人和小鼠的红细胞中,可以抑制氯离子通道,IC50值为 1.6 μM。
T13059 T16Ainh-A01

Chloride channel Membrane transporter/Ion channel
T16Ainh-A01 是氨基苯基噻唑,是有效的跨膜蛋白 16A 的抑制剂,抑制 TMEM16A 介导的氯离子电流,IC50约为1 µM。TMEM16A (ANO1)起钙激活氯离子通道(CaCC)的作用。
T15233 Endovion

NS3728

Chloride channel Membrane transporter/Ion channel
Endovion (NS3728) 是阴离子通道抑制剂 和 Anoctamin-1 (ANO 1) 通道抑制剂,也是特异性的 VRAC/VSOAC 阻断剂。
T7191 Diphenyleneiodonium chloride

二苯基氯化碘盐,DPI

NOS; Reactive Oxygen Species; NADPH; TRP/TRPV Channel Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB
Diphenyleneiodonium chloride (DPI) 是 NADPH 氧化酶抑制剂,也是 TRPA1激活剂,EC50为 1 - 3 μM 。它选择性抑制胞内活性氧。
T0858 Flufenamic acid

Arlef,Nichisedan,氟灭酸,氟芬那酸,Achless

Potassium Channel; Calcium Channel; Chloride channel; COX; AMPK; Parasite Chromatin/Epigenetic; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; PI3K/Akt/mTOR signaling
Flufenamic acid (Arlef) 是一种非甾体类抗炎剂,是一种邻氨基苯甲酸衍生物,具有镇痛、抗炎和解热的特性。 它用于肌肉骨骼和关节疾病。
T0275 Meticrane

美替克仑,Fontiliz,Arresten,蒲硫杂茶磺胺

Chloride channel; Sodium Channel Membrane transporter/Ion channel
Meticrane (Arresten) 是一种磺胺类衍生物,具有类似噻嗪类利尿剂的活性,可于研究原发性高血压。
T2498 Adjudin

AF-2364

Chloride channel; Mitochondrial Metabolism Membrane transporter/Ion channel; Metabolism
Adjudin (AF-2364) 是广泛研究的男性避孕试剂,可通过抑制 NF-κB 通路来减弱小胶质细胞的活化。
T4330 CaCCinh-A01

Chloride channel Membrane transporter/Ion channel
CaCCinh-A01 是钙激活氯离子通道和TMEM16A 抑制剂,IC50值分别为 10 和 2.1 μM。
T0693 Niflumic acid

氟尼酸,Nifluril,Forenol,Landruma

Others; Phospholipase; Chloride channel; COX; Monocarboxylate transporter; UGT Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
Niflumic acid (Nifluril) 是钙离子激活的氯离子通道阻断剂,用于治疗类风湿性关节炎的镇痛剂和抗炎剂。
T1049 Oxybutynin chloride

Oxybutynin hydrochloride,盐酸奥昔布宁,Oxybutynin HCl

Potassium Channel; AChR Membrane transporter/Ion channel; Neuroscience
Oxybutynin chloride (Oxybutynin HCl) 是一种抗胆碱能药物,用于缓解泌尿和膀胱困难。它抑制血管 Kv 通道,IC50为 11.51 μM。
T13536 Afoxolaner

Chloride channel; GABA Receptor; Parasite Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Afoxolaner 是一种异恶唑啉杀虫剂/杀螨剂,可对抗犬的肩胛硬蜱。 它作用于昆虫的 γ-氨基丁酸(GABA)受体谷氨酸受体,抑制 GABA 和谷氨酸调节的氯离子吸收,导致过度的神经元刺激和节肢动物死亡。
T4503 Talniflumate

Somalgen,他尼氟酯

Chloride channel; COX; N-Acetylglucosaminyltransferase; Anion Exchanger Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
Talniflumate (Somalgen) 是一种钙激活氯离子通道 (hCLCA1/mCLCA3) 阻滞剂,可减少动物模型和细胞培养中的粘蛋白合成和释放。它通过抑制环氧合酶,并抑制 Cl-/HCO3- 交换活性,具有抗炎作用。它还增加了远端肠梗阻综合征囊性纤维化小鼠模型的存活率。
T22330 Fenamic acid

N-苯基邻氨基苯甲酸,2-Anilinobenzoic acid,Diphenylamine-2-carboxylic acid,2-(Phenylamino)benzoic acid,N-Phenylanthranilic acid

Chloride channel Membrane transporter/Ion channel
Fenamic acid (N-Phenylanthranilic acid) 是氯通道阻滞剂。
T4059 Selamectin

UK-124114,司拉克丁,塞拉菌素

Chloride channel; P-gp; Parasite Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Selamectin (UK-124114) 是半合成的大环内酯,是一种驱虫剂,可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。它还是抗寄生虫剂,可激活神经元和咽肌中的谷氨酸门控氯离子通道,以预防恶丝虫,淋巴丝虫和线虫感染。它还是 P-糖蛋白底物和抑制剂,IC50为 120 nM。
T6307 Lubiprostone

芦比前列酮,SPI-0211,RU-0211,鲁比前列酮

Chloride channel Membrane transporter/Ion channel
Lubiprostone (RU-0211) 是一种 ClC-2 氯化物通道的激活剂,用于治疗特发性慢性便秘。
T15212 Emamectin Benzoate

MK-244,甲胺基阿维菌素苯甲酸盐

Apoptosis; Reactive Oxygen Species; GABA Receptor; Parasite Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
Emamectin Benzoate (MK-244) 是口服有效的神经系统毒物,其通过结合昆虫中的 GABA 受体发挥作用。它是阿维菌素的半合成衍生物之一,具有广谱的杀虫和杀螨活性。它诱导ROS 介导的 DNA 损伤和细胞凋亡。
T5454 N-(p-amylcinnamoyl) Anthranilic Acid

2-(3-(4-戊基苯基)丙烯酰胺基)苯甲酸,ACA

Phospholipase; TRP/TRPV Channel Membrane transporter/Ion channel; Metabolism
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) 是一种广谱磷脂酶 A2(PLA2) 抑制剂,也是TRP channel 的阻滞剂。ACA 也可逆的抑制钙离子激活氯通道 (calcium-activated chloride channels) ,在心律失常方面具有研究的潜力。
T0124 UK-124114

UNII-A2669OWX9N,西拉菌素,Selamectin

Others Others
UK-124114 (Selamectin) 是伊维菌素的大环内酯衍生物,伊维菌素是一种驱虫剂,可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。在 H. contortus 幼虫发育试验中,赛拉菌素 (0.1 µg/ml) 显示出生长抑制作用。
T1240 Flumazenil

Ro 15-1788,氟马西尼

GABA Receptor Membrane transporter/Ion channel; Neuroscience
Flumazenil (Ro 15-1788) 是一种有竞争性的GABAA 受体拮抗剂,以剂量依赖的方式逆转苯二氮卓类药物诱导的作用,包括镇静、精神运动缺陷、健忘和换气不足。
T69610 Taplucainium chloride

Taplucainium chloride is a sodium channel blocker with applications as a pain reliever.
T69550 NS-3736

NS-3736 is a chloride channel inhibitor that has been shown to prevent osteoclastic acidification and resorption.
T35734 Doramectin monosaccharide

Doramectin monosaccharide is an acid degradation product of doramectin , a disaccharide-containing anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. Doramectin undergoes acid-catalyzed hydrolysis to form doramectin monosaccharide.
T37748 Ivermectin B1b

Ivermectin B1b is the minor component . It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.
T61818 DFBTA

DFBTA is a highly effective and orally active inhibitor of ANO1, specifically the calcium-activated chloride channel anoctamin-1. It exhibits potent inhibitory activity, with an IC 50 of 24 nM. Notably, DFBTA demonstrates significant analgesic efficacy in treating inflammatory pain [1].
T40750 12,14-Dichlorodehydroabietic acid

12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, exhibits potent calcium-activated potassium (BK) channel opening activity. It effectively inhibits GABA-dependent chloride influx in the mammalian brain, functioning as a non-competitive antagonist of GABA A receptors. Moreover, 12,14-Dichlorodehydroabietic acid induces an elevation in cytosolic free calcium levels and promotes the release of neurotransmitters.
TP1285 Chlorotoxin(linear)

Chlorotoxin(linear) is a linear 36 amino-acid peptide which can be used in Chlorotoxin related research. Chlorotoxin is a chloride channel blocker which has been found in the venom of the Egyptian scorpion Leiurus quinquestriatus.
T35733 Doramectin aglycone

Doramectin aglycone is an acid degradation product of doramectin , a disaccharide-containing anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes, and its acid-catalyzed hydrolysis product doramectin monosaccharide . Doramectin undergoes one round of acid-catalyzed hydrolysis to form doramectin monosaccharide which is then hydrolyzed again to remove the remaining saccharide unit and form doramectin aglycone.
T37756 Phloxine B

Phloxine B is a red dye, the USP grade of which is used as a color additive for food, drugs, and cosmetics. It has also been used as an alternative to Gram staining, to differentiate between Gram-negative and Gram-positive bacteria. At 100 μg/ml, it can inhibit methicillin-resistant S. aureus growth in vitro. Phloxine B has also been shown to modulate channel activity of wild-type cystic fibrosis transmembrane conductance regulator chloride channels (CFTR; Ki = 38 μM) and mutant delta F508 CFTR ...
T79578 CFTR corrector 12

CFTR Membrane transporter/Ion channel
CFTRcorrector 12(compound 17C)作为一种双噻唑衍生物,本身是CFTR校正剂。它具有校正控制氯离子跨膜运输通道的特定折叠缺陷突变的功能,并能够在带有突变的细胞中恢复α-肌聚糖(α-SG)的含量。
T35746 Milbemycin A3

Milbemycin A3 is a member of a complex family of macrocyclic lactones that contain a characteristic spiroketal group produced from the fermentation of soil bacterium S. hygroscopicus subsp. aureolacrimosus. As a compound that potentiates glutamate and GABA-gated chloride-channel opening, milbemycin A3 is used as a nematocide and insecticide. The acaricidal and nematocidal activity of a mixture of milbemycin A3 and milbemycin A4 against adult spider mites, spider mite eggs, and C. elegans are rep...

化合物

QX-314 chloride
Cat.No: T12608
Synonym:
Target: Sodium Channel
MONNA
Cat.No: T8960
Synonym:
Target: Chloride channel
Eact
Cat.No: T15192
Synonym:
Target: Chloride channel
NPPB
Cat.No: T7638
Synonym:
Target: Chloride channel
DCPIB
Cat.No: T10979
Synonym:
Target: Potassium Channel, Chloride channel
Tetraethylammonium chloride
Cat.No: T7538
Synonym:
Target: Potassium Channel
QX-222 chloride
Cat.No: T23213
Synonym: QX 222,Lidocaine N-Methyl Hydrochloride
Target: Sodium Channel
Cesium chloride
Cat.No: T8391
Synonym: 氯化铯,CsCl
Target: Potassium Channel
Dequalinium chloride
Cat.No: T0979
Synonym: Dequafungan,地喹氯铵,Danical,Decabis
Target: Potassium Channel, PKC
NS1652
Cat.No: T16346
Synonym:
Target: Chloride channel
T16Ainh-A01
Cat.No: T13059
Synonym:
Target: Chloride channel
Endovion
Cat.No: T15233
Synonym: NS3728
Target: Chloride channel
Diphenyleneiodonium chloride
Cat.No: T7191
Synonym: 二苯基氯化碘盐,DPI
Target: NOS, Reactive Oxygen Species, NADPH, TRP/TRPV Channel
Flufenamic acid
Cat.No: T0858
Synonym: Arlef,Nichisedan,氟灭酸,氟芬那酸,Achless
Target: Potassium Channel, Calcium Channel, Chloride channel, COX, AMPK, Parasite
Meticrane
Cat.No: T0275
Synonym: 美替克仑,Fontiliz,Arresten,蒲硫杂茶磺胺
Target: Chloride channel, Sodium Channel
Adjudin
Cat.No: T2498
Synonym: AF-2364
Target: Chloride channel, Mitochondrial Metabolism
CaCCinh-A01
Cat.No: T4330
Synonym:
Target: Chloride channel
Niflumic acid
Cat.No: T0693
Synonym: 氟尼酸,Nifluril,Forenol,Landruma
Target: Others, Phospholipase, Chloride channel, COX, Monocarboxylate transporter, UGT
Oxybutynin chloride
Cat.No: T1049
Synonym: Oxybutynin hydrochloride,盐酸奥昔布宁,Oxybutynin HCl
Target: Potassium Channel, AChR
Afoxolaner
Cat.No: T13536
Synonym:
Target: Chloride channel, GABA Receptor, Parasite
Talniflumate
Cat.No: T4503
Synonym: Somalgen,他尼氟酯
Target: Chloride channel, COX, N-Acetylglucosaminyltransferase, Anion Exchanger
Fenamic acid
Cat.No: T22330
Synonym: N-苯基邻氨基苯甲酸,2-Anilinobenzoic acid,Diphenylamine-2-carboxylic acid,2-(Phenylamino)benzoic acid,N-Phenylanthranilic acid
Target: Chloride channel
Selamectin
Cat.No: T4059
Synonym: UK-124114,司拉克丁,塞拉菌素
Target: Chloride channel, P-gp, Parasite
Lubiprostone
Cat.No: T6307
Synonym: 芦比前列酮,SPI-0211,RU-0211,鲁比前列酮
Target: Chloride channel
Emamectin Benzoate
Cat.No: T15212
Synonym: MK-244,甲胺基阿维菌素苯甲酸盐
Target: Apoptosis, Reactive Oxygen Species, GABA Receptor, Parasite
N-(p-amylcinnamoyl) Anthranilic Acid
Cat.No: T5454
Synonym: 2-(3-(4-戊基苯基)丙烯酰胺基)苯甲酸,ACA
Target: Phospholipase, TRP/TRPV Channel
UK-124114
Cat.No: T0124
Synonym: UNII-A2669OWX9N,西拉菌素,Selamectin
Target: Others
Flumazenil
Cat.No: T1240
Synonym: Ro 15-1788,氟马西尼
Target: GABA Receptor
Taplucainium chloride
Cat.No: T69610
Synonym:
Target:
NS-3736
Cat.No: T69550
Synonym:
Target:
Doramectin monosaccharide
Cat.No: T35734
Synonym:
Target:
Ivermectin B1b
Cat.No: T37748
Synonym:
Target:
DFBTA
Cat.No: T61818
Synonym:
Target:
12,14-Dichlorodehydroabietic acid
Cat.No: T40750
Synonym:
Target:
Chlorotoxin(linear)
Cat.No: TP1285
Synonym:
Target:
Doramectin aglycone
Cat.No: T35733
Synonym:
Target:
Phloxine B
Cat.No: T37756
Synonym:
Target:
CFTR corrector 12
Cat.No: T79578
Synonym:
Target: CFTR
Milbemycin A3
Cat.No: T35746
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1221 Acetylcholine chloride

ACh chloride,Pilofrin,氯化乙酰胆碱

Calcium Channel; Endogenous Metabolite; AChR Membrane transporter/Ion channel; Metabolism; Neuroscience
Acetylcholine chloride (Pilofrin) 是一种神经递质,是胆碱能激动剂,通过刺激烟碱乙酰胆碱受体调节多巴胺能神经元活性,在体外抑制 p53 突变肽的聚集。
TN1035 Irisolidone

尼泊尔鸢尾异黄酮,葛花苷元

IL Receptor; NF-κB; Chloride channel Immunology/Inflammation; Membrane transporter/Ion channel; NF-κB
Irisolidone 是葛根花中的一种异黄酮,具有较强的保肝活性。它是一种有效的体积调节阴离子通道 (VRAC) 电流抑制剂,有高效阻断作用,IC50 为 5-13 μM。
T1125 Shikonin

NSC 252844,Isoarnebin 4,(+)-Shikonin,紫草素,Alkanna Red,C.I. 75535,Anchusa acid

TNF; NF-κB; Chloride channel; HIV Protease; PKM Apoptosis; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome
Shikonin (Anchusa acid) 属于天然产物,是一种 TMEM16A 氯离子通道抑制剂 (IC50=6.5 μM) 和选择性 PKM2 抑制剂。Shikonin 具有抗肿瘤、抗炎和伤口愈合活性。
T16535 Picrotoxinin

Chloride channel; GABA Receptor Membrane transporter/Ion channel; Neuroscience
Picrotoxinin 是一种氯离子通道阻断剂和 GABAA 的非竞争性拮抗剂,对 α1β2γ2L GABAA 的 IC50 为 1.15 μM。 Picrotoxinin 具有惊厥作用。
T1131 Ivermectin

MK-933,伊维菌素

Mitophagy; GluCls; P2X Receptor; SARS-CoV; HIV Protease; Antibiotic; Parasite; Autophagy; HSV Autophagy; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome
Ivermectin (MK-933) 是谷氨酸门控氯离子通道激活剂,具有抗寄生虫活性。它特异性抑制Impα/β1 介导的核导入,还抑制牛疱疹病毒 1 复制并抑制BoHV-1DNA 聚合酶的核输入。它具有很强的抗病毒活性。它也是P2X4和 α7nAChRs 的正异构效应物。
T75722 Chlorotoxin TFA

Chlorotoxin TFA,一种从蝎子毒液中分离出的多肽,作为氯离子通道 (chloride channel) 的阻断剂,具备抗癌活性。
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...
TN3351 Aflatrem

GABA Receptor Membrane transporter/Ion channel; Neuroscience
Aflatrem is a tremorgenic mycotoxin with acute neurotoxic effects, a single low dose of aflatrem is able to induce degeneration of neuronal processes in hippocampal neurotransmitter systems. Aflatrem potentiates the gamma-aminobutyric acid (GABA)-induced

天然产物

Acetylcholine chloride
Cat.No: T1221
Synonym: ACh chloride,Pilofrin,氯化乙酰胆碱
Target: Calcium Channel, Endogenous Metabolite, AChR
Irisolidone
Cat.No: TN1035
Synonym: 尼泊尔鸢尾异黄酮,葛花苷元
Target: IL Receptor, NF-κB, Chloride channel
Shikonin
Cat.No: T1125
Synonym: NSC 252844,Isoarnebin 4,(+)-Shikonin,紫草素,Alkanna Red,C.I. 75535,Anchusa acid
Target: TNF, NF-κB, Chloride channel, HIV Protease, PKM
Picrotoxinin
Cat.No: T16535
Synonym:
Target: Chloride channel, GABA Receptor
Ivermectin
Cat.No: T1131
Synonym: MK-933,伊维菌素
Target: Mitophagy, GluCls, P2X Receptor, SARS-CoV, HIV Protease, Antibiotic, Parasite, Autophagy, HSV
Chlorotoxin TFA
Cat.No: T75722
Synonym:
Target:
Kobusin
Cat.No: TN1834
Synonym: 去甲槟郎碱,自旋七叶素
Target: Others, NOS, NF-κB
Aflatrem
Cat.No: TN3351
Synonym:
Target: GABA Receptor
TargetMol Loading
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