Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T61407 |
TRPC3/6-IN-1
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TRPC3/6-IN-1 is a highly potent and selective inhibitor that specifically blocks the activity of the canonical transient receptor channels TRPC3 and TRPC6. It exhibits a significant blocking potency against the human isoforms hTRPC3 and hTRPC6, with IC50 values of 1260 nM and 500 nM, respectively. This compound, TRPC3/6-IN-1, is particularly valuable for conducting research on chronic models of heart failure [1]. | |||
T79054 |
TRPC3/6-IN-2
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TRPC3/6-IN-2为针对TRPC3及TRPC6的高效抑制剂,IC50分别为16 nM对TRPC3与29.8 nM对TRPC6。 | |||
T16686 |
Pyr10
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Pyr10 是吡唑衍生物,是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。 | |||
T16687 |
Pyr3
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Pyr3 是一种选择性瞬时受体电位经典通道 3 抑制剂。 Pyr3 以剂量依赖性方式抑制 TRPC3 介导的 Ca2+ 内流 (IC50 = 700 nM)。 | |||
T16688 |
Pyr6
N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide)是选择性的 TRPC3抑制剂,IC50值为0.49uM。 | |||
TP2158 |
TRV-120027 TFA
TRV-120027 TFA (1234510-46-3 free base) |
RAAS; Arrestin | Endocrinology/Hormones; GPCR/G Protein |
TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂,可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂,可与 ß-arrestins 结合,同时阻断 G 蛋白信号传导。 它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌,并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。 | |||
T16532 |
Pico145
HC-608 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Pico145 (HC-608) 是有效的瞬时受体电位通道蛋白 1/4/5 (TRPC1/TRPC4/TRPC5) 抑制剂,在细胞中,抑制 (-)-englerin A 活化TRPC4/TRPC5 通道的IC50分别为 0.349 和 1.3 nM。 | |||
T10537 |
BI-749327
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
BI-749327是高选择性、口服有效的TRPC6拮抗剂,对小鼠、人、豚鼠 TRPC6 作用的IC50值分别为 13 nM、19 nM 和 15 nM。BI-749327对小鼠 TRPC6 选择性比 TRPC3 高出 85 倍, 比TRPC7高出42 倍。 | |||
T8784 |
IGS-1.76
|
Others | Others |
IGS-1.76对hNCS-1有显著的亲和力,并有效调节hNCS-1与Ric8a之间的相互作用。此外,IGS-1.76还能熟练抑制由human NCS-1和Ric8a形成的复合物。 | |||
T28444 |
PPZ1
PPZ 1,PPZ-1 |
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PPZ1 is a novel DAG-activated TRPC3/TRPC6/TRPC7 channels activator. | |||
T28445 |
PPZ2
PPZ-2,PPZ 2 |
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PPZ2 is a novel DAG-activated TRPC3/TRPC6/TRPC7 channels activator. | |||
T33814 |
OptoDArG
Opto-DArG,Opto DArG |
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OptoDArG is a diacylglycerol (DAG) photoswitch, which enables efficient control of TRPC3 by light. | |||
T38780 |
GSK2332255B
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GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels. | |||
T37698 |
OptoBI-1
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OptoBI-1 是一种光敏分子,是光致变色的TRPC3激动剂,可用作控制神经元放电的光药理学工具。 | |||
T15425 |
GSK1702934A
|
Others | Others |
GSK1702934A is a selective TRPC3 agonist. It modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3. | |||
T37823 | M 084 hydrochloride | ||
TRPC4/5 channel blocker (IC50 values are 3.7-10.3 and 8.2 μM, respectively). Also weakly blocks TRPC3 channels. Exhibits rapid antidepressant and anxiolytic effects in vivo. Zhu et al (2015) Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels. Br.J.Pharmacol. 172 3495 PMID:25816897 |Yang et al (2015) Acute treatment with a novel TRPC4/C5 channel inhibitor produces antidepressant and anxiolytic-like effects in mice. PLoS One 10 e0136... | |||
T41232 |
GSK 2833503A
|
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GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes. | |||
T71303 |
Flufenamic Acid-d4
|
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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... | |||
T13213 | TRPC6-IN-1 | Others | Others |
TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM). | |||
T23148 |
Phenamil methanesulfonate
Phenamil |
Others | Others |
TRPP3 channel inhibitor |