Membrane Transporters/Ion Channels
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TRPM8 拮抗剂
AMG-333是有效的选择性TRPM8拮抗剂,IC50为13 nM。
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TRPM8 antagonist
AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
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TRPC6 inhibitor
SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
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TRPML3 ion channel activator
SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8??0.13 μM.
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TRPM8 agonist
D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
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TRPC3 inhibitor
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
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TRP 激动剂
Evodiamine (Isoevodiamine)是从Tetradium植物家族中提取的一种化学物质。 它主要起产热和刺激作用。
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TRPA1 channel blocker
A 967079是选择性TRPA1通道阻滞剂(人和大鼠TRPA1受体的IC50值分别为67和289 nM)。
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- L Jin, .et al. Acrolein but not its metabolite, 3-Hydroxypropylmercapturic acid (3HPMA), activates vascular transient receptor potential Ankyrin-1 (TRPA1): Physiological to toxicological implications, Toxicol Appl Pharmacol, 2021, Jul 13;426:115647 PMID: 34271065
- L. Jin, .et al. Crotonaldehyde-induced vascular relaxation and toxicity: Role of endothelium and transient receptor potential ankyrin-1 (TRPA1), Toxicology and Applied Pharmacology, 2020, 398(1),
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photoactive TRPA1 activator
Optovin是可逆光敏trpa1活化剂。
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TRPM8 and TRPA1 activator
Icilin是一种冷却剂,可激活新型的冷受体TRPM8(CMR1)和TRPA1(ANKTM1/TRPN1),它们是TRP离子通道家族的成员。在表达CMR1的HEK 293细胞中感应电流(EC50 = 0.36μM)。
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TRPA1 抑制剂
HC-030031是选择性TRPA1阻滞剂,可拮抗AITC和福尔马林诱导的TRPA1介导的钙内流(IC50分别为6.2和5.3 uM)。
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TRPA1 channel blocker
TCS 5861528是TRPA1通道阻滞剂和AITC和4-HNE诱发的钙流入的拮抗剂。
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ACA是一种通道阻滞剂,作用于多个瞬态受体电位(TRP)通道,包括TRPM2,TRPM8和TRPC6(IC50分别为1.7、3.8和2.3 uM)。
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TRPA1 activatior/TRPM8 blocker
Cannabichromene是一种主要的非精神植物大麻素,可抑制内源性大麻素失活并激活瞬时受体电位锚蛋白1(TRPA1)。内源性大麻素和TRPA1均可调节肠胃蠕动。
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TRPC4/C5 抑制剂
ML204是一种新型强效拮抗剂,可选择性调节天然TRPC4/C5离子通道。
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TRPM8 拮抗剂
RQ-00203078是一种高度选择性,有效且可口服的TRPM8拮抗剂(大鼠和人类通道的IC50值分别为5.3和8.3 nM),对TRPM8的选择性是TRPV4,TRPV1和TRPA1的> 350倍。
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GsMTX4是一种从Grammostola rosea(智利玫瑰)狼蛛毒液分离的34个氨基酸的肽基毒素,属于huwentoxin-1家族。
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- Yong Chen, .et al. Epithelia-Sensory Neuron Cross Talk Underlies Cholestatic Itch Induced by Lysophosphatidylcholine, Gastroenterology, 2021, Apr 2 PMID: 33819485
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TrpA1 channel 激动剂
PF-4840154是TrpA1通道的非亲电参考激动剂。基于TRPA1敲除小鼠在某些临床前发展模型中显示出几乎完全减轻了疼痛行为的事实,因此认为TRPA1通道是有吸引力的疼痛靶标。
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TRPM8 激动剂
WS 3是TRPM8受体激动剂(EC50 = 3.7 μM)和凉爽剂。
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TRPM8 激动剂
WS-12是有效的TRPM8激动剂,可作为凉爽剂(EC50 = 193 nM)。
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TRPC6 inhibitor
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
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TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
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TRPC1/4/5 channels inhibitor
Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
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TRPV1 拮抗剂
SB-705498是有效,选择性和口服生物利用的TRPV1拮抗剂,抑制TRPV1的Capsaicin,酸和热激活,IC50分别为3 nM, 0.1 nM和6 nM,该作用具有一定的电压依赖性,作用于TRPV1比作用于TRPM8选择性高100倍以上。
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TRPV1 拮抗剂
AMG 517是有效的选择性TRPV1拮抗剂。
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- Jun Hai, .et al. Intragastric administration of AMG517, a TRPV1 antagonist, enhanced activity-dependent energy metabolism via capsaicin-sensitive sensory nerves in mice, Biosci Biotechnol Biochem, 2020, Jul 7;1-7 PMID: 32633621
- Hai J, .et al. Differences in the effects of TRPV1 antagonists on energy metabolism in mice, Biomed Res, 2018, 39(6):279-286 PMID: 30531157
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TRPV1 receptor 拮抗剂
A-889425是选择性TRPV1受体拮抗剂。A-889425阻断TRPV1通道,IC50为335 nM(大鼠)和34 nM(人)。
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Linoleyl ethanolamide是一种内源性大麻素,也与TRPV1结合(Ki = 5.60 uM)。
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TRPV1 modulator
MRS1477是TRPV1阳性变构调节剂。
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TRPV1 拮抗剂
Mavatrep是生物利用的TRPV1拮抗剂(Ki = 6.5 nM),对CYP亚型3A4、1A2和2D6的酶活性(IC50> 25μM)影响很小。
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TRPV1 receptor 拮抗剂
SB-366791是新颖,有效且选择性的肉桂酰胺TRPV1拮抗剂。
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TRPV1 receptor
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
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TRPV1 antagonist
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
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TRPV4 blocker
GSK2193874被确定为选择性的口服活性TRPV4阻滞剂,可通过重组TRPV4通道和天然内皮TRPV4电流抑制Ca(2+)流入。
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vanilloid receptor 激动剂
Resiniferatoxin是从大戟属(Euphorbia)属的一些植物中分离出的辣椒素的天然类似物(货号92350),包括E. resinifera。
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- Thieu X. Phan, .et al. TRPV1 in arteries enables a rapid myogenic tone, bioRxiv, 2021, February 27
- Thieu X Phan, .et al. TRPV1 expressed throughout the arterial circulation regulates vasoconstriction and blood pressure, J Physiol, 2020, Sep 17 PMID: 32944976
- Thieu X. Phan, .et al. TRPV1 expressed throughout the arterial circulation regulates vasoconstriction, bioRxiv, 2020, February 04
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TRPV4 Activator
GSK1016790A是一种新型有效的TRPV4激活剂(瞬态受体电位香草酸4),在脉络丛上皮细胞中的EC50为34nM。
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(+)-Camphor是蜡状,易燃,白色或透明的固体,具有强烈的香气,通常用于缓解疼痛,减少瘙痒和治疗真菌感染。它可以激活TRPV1和TRPV3。
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TRPV1 agonist
Zucapsaicin, also known as cis-Capsaicin, is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. It reduces pain, and improves articular functions.
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TRPV1 antagonist
NJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.
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EAAT1 抑制剂
UCPH 101是EAAT1的选择性非底物抑制剂(EAAT1,EAAT2和EAAT3的IC50分别为660,> 300000和> 300000 nM)。
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SNR 抑制剂
Sibutramine hydrochloride是5-HT和去甲肾上腺素再摄取抑制剂(SNRI)。
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Serotonin transporter 抑制剂
Imipramine Hydrochloride是一种三环抗抑郁药。抑制血清素和去甲肾上腺素转运蛋白,但对多巴胺转运蛋白几乎没有影响。
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serotonin reuptake 抑制剂
Azaphen dihydrochloride monohydrate是5-羟色胺再摄取的有效抑制剂。
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proton pump 抑制剂
Tenatoprazole是质子泵抑制剂(PPI)类的前药,可抑制质子转运,IC50为3.2 uM。
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Proton pump 抑制剂
Esomeprazole Magnesium trihydrate 是质子泵抑制剂,可通过抑制胃壁细胞中的H+/K+ ATPase来减少酸的分泌。
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M2 ion channel blocker能够抑制和阻断M2离子通道的活性。抗病毒药。
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Proton pump 抑制剂
Esomeprazole sodium是一种质子泵抑制剂,可通过抑制胃壁细胞中的H+/K+ ATPase来减少酸的分泌。
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proton pump 抑制剂
Rebeprazole sodium是质子泵抑制剂中的一种抗溃疡药。
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Chebulinic acid是结核分枝杆菌DNA促旋酶的有效天然抑制剂,也可以抑制SMAD-3磷酸化,抑制H+K+-ATPase活性。
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Proton pump 抑制剂
Lauric acid是质子泵抑制剂,可能用于治疗幽门螺杆菌感染。
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Oct4 Activator
OAC1通过增强Oct4和Nanog驱动的基因表达来增强iPSC重编程效率。
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