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Cat. No. | Product Name | Target | Signaling Pathways |
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T23101 |
o-3M3FBS
|
Others | Others |
o-3M3FBS 是 m-3M3FBS 的阴性对照。它以独立于 PLC 的机制及拮抗方式抑制内向和外向电流。它以与 m-3M3FBS 竞争的方式增加 [Ca2+]i 增加。 | |||
T22408 |
Proflavine
吡啶-3,6-二胺,3,6-Diaminoacridine |
Antibacterial | Microbiology/Virology |
Proflavine (3,6-Diaminoacridine) 是吖啶染料,可用作抗菌剂。它是 DNA 嵌入剂,能够阻滞Kir3.2孔。它用作与 Kir3.2 相关的神经系统疾病的研究。 | |||
T0438 |
Proflavine Hemisulfate
3,6-Diaminoacridine hemisulfate,Proflavin hemisulfate,硫酸原黄素 |
Others; Potassium Channel; DNA; Thrombin; Antibacterial; Autophagy | Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Others; Proteases/Proteasome |
Proflavine Hemisulfate (3,6-Diaminoacridine hemisulfate) 是一种 DNA 嵌入剂,也是一种吖啶染料。它是抗菌剂,也可作为 Kir3.2孔阻滞剂,可研究与 Kir3.2 相关的神经系统疾病。 | |||
T21263 |
Amlodipine maleate
Amlodipine (+-)-form maleate,Amvaz |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Amlodipine maleate (Amvaz) 是一种具有口服活性的二氢吡啶类钙通道阻滞剂,通过阻滞电压依赖性 L 型钙通道,从而抑制钙离子内流。Amlodipine maleate 可用于研究高血压和癌症。 | |||
T27205 |
DPI 201-106
DPI-201-106 |
Sodium Channel | Membrane transporter/Ion channel |
DPI 201-106对电压门控钠通道的有心脏选择性调节活性,从而产生正性肌力作用。DPI 201-106 具有协同肌膜和细胞内作用机制。 | |||
T4542 |
Clonixin
Clonixic acid,氯尼辛 |
Others | Others |
Clonixin (Clonixic acid) 是一种非甾体抗炎药,具有口服活性。 | |||
T0207 |
Ranolazine dihydrochloride
盐酸雷诺嗪,雷诺嗪二盐酸盐,RS 43285,Ranolazine 2HCl |
Calcium Channel; Sodium Channel; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism |
Ranolazine dihydrochloride (Ranolazine 2HCl) 是一种抗心绞痛和抗缺血剂,可通过抑制内向钠电流的后期作用来发挥功效,而不会影响心率或血压。它对 INa 和 IKr 的 IC50值分别为 6 μM 和 12 μM。它还是脂肪酸氧化的部分抑制剂。 | |||
T22361 |
Mepivacaine
Carbocaine |
Sodium Channel | Membrane transporter/Ion channel |
Mepivacaine (Carbocaine) 是一种可用于局部麻醉的酰胺类化合物,可使人或动物短暂的失去自知觉。Mepivacaine 通过与神经细胞膜上特定的电压门控钠离子通道结合,抑制钠离子内流和膜去极化来发挥作用。Mepivacaine 适用于神经阻滞和硬膜外麻醉。 | |||
T36033 |
DETA NONOate
NOC-18,Diethylamine NONOate |
NO Synthase | Immunology/Inflammation |
DETA NONOate (NOC 18)是外源性一氧化氮 (NO) 供体,具有血管舒张和抗抑郁活性。DETA NONOate 可用于激活神经元中的内向电流,可加速MRSA感染伤口的愈合。 | |||
T0866 |
Propafenone
Rythmol,普罗帕酮,Propafenonum |
Potassium Channel; MRP; Sodium Channel | Immunology/Inflammation; Membrane transporter/Ion channel |
Propafenone (Propafenonum) 是钠通道阻滞剂,它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ,具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡,从而抑制食管癌增殖。 | |||
T15555 |
IK1 inhibitor PA-6
|
Potassium Channel | Membrane transporter/Ion channel |
IK1 inhibitor PA-6 是一种喷他脒类似物,是选择性的 IK1(KIR2.x 离子通道携带向内整流电流) 抑制剂,对人和老鼠中 KIR2.x 电流的 IC50值为 12-15 nM。它可上调 KIR2.1 的蛋白表达,诱导细胞内 KIR2.1 的蛋白的积累。它在房颤和心律失常的研究中具有潜力。 | |||
T6541 |
Ibutilide Fumarate
Corvert Fumarate,U70226E,富马酸伊布利特 |
Calcium Channel; Sodium Channel | Membrane transporter/Ion channel; Metabolism |
Ibutilide Fumarate (U70226E) 是一种 III 类抗心律失常药物,可作用于急性心梗阻塞。 | |||
T13387L |
Zatebradine hydrochloride
UL-FS-49CL,UL-FS-49 |
Others; HCN Channel | Membrane transporter/Ion channel; Others |
Zatebradine hydrochloride (UL-FS-49CL) 是一种高效的 、有效的HCN Channel 抑制剂( IC50 :1.96 µM)。 HCN Channel 是一种有效的超极化激活环核苷酸门控通道。 Zatebradine hydrochloride 阻止通过人类 HCN1,HCN2,HCN3 和 HCN4 通道的缓慢内向电流,其 IC50 值分别为 1.83 µM,2.21 µM,1.90 µM 和 1.88 µM。 | |||
T2535 |
Ivabradine hydrochloride
盐酸伊伐布雷定,S 16257-2,Ivabradine HCl |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Ivabradine hydrochloride (S 16257-2) 是一种可口服的,超极化激活的环核苷酸门控离子通道通道阻滞剂。 | |||
T19839 |
Oxatomide
Oxatomida |
P2X Receptor; Calcium Channel; 5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Oxatomide (Oxatomida) 是一种有效且具有口服活性的双重 H1 组胺受体 和 P2X7 受体双重拮抗剂,具有抗组胺和抗过敏活性。Oxatomide 可用于阻断人 P2X7 受体中 ATP 诱导的电流 ,IC50 为 0.95 μM。Oxatomide 对 ATP 诱导的 Ca2+ 内流具有抑制作用,IC50 值为 0.43 μM。Oxatomide 对 5-羟色胺具有抑制作用。Oxatomide可用于治疗免疫系统疾病和研究超敏反应。 | |||
T71406 |
SA 2572
|
Others | Others |
SA 2572 is a newly synthesized Ca2+ antagonist having a inhibitory effect on the fast Na+ inward channel. | |||
T23012 |
MNI caged kainic acid
|
Others | Others |
Generates large inward currents at resting membrane potential | |||
T24948 |
VU625
VU007625,VU 625,VU 007625,VU-625,VU-007625 |
Others | Others |
VU625 is an effective inhibitor of Aedes aegypti inward rectifier potassium channels. | |||
T5336L |
Zacopride
Racemic zacopride |
Others | Others |
Zacopride is a selective agonist of inward rectifier potassium current (I K1) channel, inhibiting ventricular arrhythmias without affecting atrial arrhythmias. | |||
T80510 |
Tertiapin-RQ
|
Potassium Channel | Membrane transporter/Ion channel |
Tertiapin-RQ为抗抑郁特性的内向整流K+通道阻滞剂肽。 | |||
T68361 |
Asocainol hydrochloride
|
Others | Others |
Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also interferes with the fast inward Na+ current. | |||
T70063 |
GYKI 52466 HCl
|
Others | Others |
GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general... | |||
TP1967 |
Phrixotoxin 3
|
||
Potent blocker of voltage-gated sodium channels (IC50 values are 0.6, 42, and 72 nM for NaV1.2, NaV1.3 and NaV1.5 respectively). Blocks inward sodium currents in a voltage-dependent manner. | |||
T17240 |
VU041
|
Others | Others |
VU041 is an inhibitor of Anopheles gambiae and Aedes aegypti inward rectifier potassium 1 channels (IC50: 2.5 μM and 1.7 μM, respectively). VU041 inhibits appreciably is mammalian Kir2.1 (IC50: 12.7 μM) and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. | |||
T37093 |
4,9-Anhydrotetrodotoxin
4,9-Anhydrotetrodotoxin,4,9-anhydro-TTX |
Others | Others |
4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1] | |||
T84683 |
NPBA
|
Others | Others |
NPBA为K2P通道TASK-3 (KCNK9)的激动剂,并对串联孔域弱内向整流K+通道(TWIK2)具有阻断作用。此外,NPBA能够抑制巨噬细胞中NLRP3炎性体的激活。 | |||
TP2114 |
Tertiapin-Q
|
||
A high affinity blocker for inward-rectifier K+ channels, this compound is a stable derivative of the bee venom toxin tertiapin. Binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and | |||
T41209 |
DPNB-ABT 594
|
Others | Others |
DPNB-ABT 594 is a nitrobenzyl-caged ABT 594, a selective α4β2 nAChR agonist. One-photon uncaging evokes large inward currents and Ca2+transients on cell bodies and dendrites of medial habenular neurons in mouse brain slices. Two-photon uncaging induces fast nAChR-mediated currents. Photolyzed with high quantum yield of 0.20. Effective photolysis occurs using one- or two-photon excitation; one-photon uncaging requires illumination at 410 nm for 1.5-3 ms; two-photon uncaging requires illumination ... | |||
T63445 |
Amlodipine mesylate
|
Others | Others |
Amlodipine mesylate 是口服具有活力的二氢吡啶钙通道(calcium channel)阻滞剂,能够阻断电压依赖性的 L 型钙通道,并抑制钙离子内流,是一种抗心绞痛药。Amlodipine mesylate 能够用于研究高血压和癌症。 | |||
T36740 |
Guanosine 5’-diphosphate (sodium salt hydrate)
|
Others | Others |
Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)... | |||
T37199 |
Bilaid C
|
||
Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Siana... | |||
T70987 |
AT-1001
|
Others | Others |
AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal prepar... | |||
TP2016 |
Huwentoxin-IV
Huwentoxin IV |
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Selective NaV1.7 channel blocker. Preferentially inhibits neuronal NaV1.7, 1.2 and 1.3 (IC50 values are 26, 150 and 338 nM respectively), compared to muscle subtypes NaV1.4 and 1.5 (IC50 = >10 μM). Inhibits the channel by binding at the neurotoxin recepto | |||
T85192 |
AF-353 hydrochloride
P2X3 Purinergic Receptor Antagonist, AF353, P2X2/3 Purinergic Receptor Antagonist, AF353 |
Others | Others |
This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The ... | |||
T75855 |
Phrixotoxin 3 TFA
|
||
Phrixotoxin 3 TFA 是一种高效的电压门控钠通道阻滞剂,对NaV1.2、NaV1.3、NaV1.4、NaV1.1及NaV1.5的IC50值分别为0.6、42、72、288和610 nM。该化合物通过改变门控动力学的去极化并阻断钠电流的内向流,调控电压门控钠通道,表现出类似典型门控修饰毒素的作用机制。 | |||
T84928 |
2-Chloroadenosine 5-triphosphate sodium
2-chloro ATP |
Others | Others |
2-Chloroadenosine 5-triphosphate (2-chloro ATP), an analog of ATP and adenine nucleotide, functions as an antagonist of the purinergic P2Y1 receptor, inhibiting ADP-induced intracellular calcium mobilization in Jurkat cells with a Ki value of 2.3 µM. Additionally, 2-chloro ATP acts as an agonist of purinergic P2X receptors, demonstrated by inducing inward currents in HEK293 cells expressing either human bladder smooth muscle or rat PC12 receptor forms, with EC50 values of 0.5 and 2.5 µM, respect... | |||
TP1513 |
Egg Laying Hormone, aplysia
|
||
Egg-laying hormone (ELH) is a neuropeptide synthesized by the bag cell neurons, Egg-laying hormone (ELH) induces egg laying and its correlated behavior in Aplysia californica. Egg-laying hormone (ELH) has been purified to homogeneity and Egg-laying hormon | |||
T83749 |
Tertiapin LQ TFA
TPNLQ |
||
Tertiapin LQ是源自蜜蜂毒素肽tertiapin的肽衍生物,同时也是向内整流钾(Kir)通道的抑制剂。它能够抑制由G蛋白激活的向内整流钾通道1(GIRK1)和GIRK4(即Kir3.1和Kir3.4)组成的异源多聚钾通道,以及向内整流钾通道1(Kir1.1)。在活体内,tertiapin LQ抑制在雪貂中对条件刺激的Purkinje细胞暂停响应。 | |||
T84871 |
Emetine hydrochloride
NSC 33669 |
Others | Others |
Emetine hydrochloride (NSC 33669),一种从ipecac根部提取的生物碱,用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4,抑制细胞自噬,并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8195 |
Lotusine
|
Others | Others |
Lotusine 是一种提取自Nelumbo nucifera Gaertn 的绿色种胚中的纯生物碱。它能够作用于心肌中动作电位及心脏浦肯野纤维缓慢内向电流。 | |||
T8040 |
Cholesterol myristate
胆甾烯基豆蔻酸酯,Cholesteryl myristate,胆固醇肉豆蔻酸,Cholesteryl tetradecanoate |
Others; Potassium Channel; GABA Receptor; Endogenous Metabolite; AChR | Membrane transporter/Ion channel; Metabolism; Neuroscience; Others |
Cholesterol myristate (Cholesteryl myristate) 是粗吻海龙中的一种类固醇,可与多种离子通道结合,例如nAChR、GABAA 受体和内向整流钾离子通道。 | |||
T78489 |
Lotusine hydroxide
|
Others | Others |
Lotusine (hydroxide)为纯生物碱,源自Nelumbo nucifera Gaertn绿色种胚提取。该化合物能够影响心肌动作电位和心脏浦肯野纤维的缓慢内向电流。 | |||
T74193 |
(R)-IDHP
|
Others | Others |
(R)-IDHP为IDHP异构体,属于丹参代谢物。该化合物能通过抑制血管平滑肌细胞电压依赖性钙通道与受体操作钙通道的Ca2+释放和Ca2+内流,发挥血管松弛作用,适用于心脑血管疾病研究。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01889 |
KCNK3 Protein, Human, Recombinant (His & Myc)
Potassium channel subfamily K member 3,TWIK-related acid-sen... |
Human | E. coli |
pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward. KCNK3 Protein, Human, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 50.5 kDa and the accession number is O... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIH-0087 |
Amlodipine-d4 Maleate (Racemic)
|
||
Amlodipine-d4 Maleate (Racemic) 是 Amlodipine Maleate (Racemic) 的氘代化合物。Amlodipine Maleate (Racemic) 的 CAS 号为 88150-47-4。Amlodipine maleate是一种具有口服活性的二氢吡啶类钙通道阻滞剂,通过阻滞电压依赖性L型钙通道,从而抑制钙离子内流。Amlodipine maleate可用于研究高血压和癌症。 | |||
T69600 |
Spermidine-d6
|
||
Spermidine-d6 is intended for use as an internal standard for the quantification of spermidine by GC- or LC-MS. Spermidine is an endogenous polyamine. It is formed from putrescine by spermidine synthase. Spermidine (25 µM) inhibits the activity of the human inward-rectifying potassium channel Kir2.3 in a patch-clamp assay. It induces autophagy in HeLa cells when used at a concentration of 100 µM and increases the lifespan of D. melanogaster, yeast, and C. elegans. Spermidine (30 mM in the drinki... |