trpc6

TRPC6-PAM-C20 是一种选择性 TRPC6 正变构调节剂。 TRPC6-PAM-C20 在表达 TRPC6 的 HEK 细胞中诱导胞内 Ca2+ 瞬时增加，EC50 为 2.37 μM。 TRPC6-PAM-C20 增强 OAG 诱导的血小板聚集。

D-GsMTx4 TFA 是一种具有选择性的蜘蛛毒液肽，是一种TRPC1 6和Piezo2抑制剂，可抑制属于 Piezo 和 TRP 通道家族的阳离子可渗透的机械敏感性通道 （MSCs），阻断阳离子选择性的拉伸激活通道 （SAC），减弱溶血磷脂酰胆碱 （LPC） 诱导的星形胶质细胞毒性和小胶质细胞反应性。D-GsMTx4 TFA 在小鼠缺血 再灌注模型中预防心肌梗死，可用于鉴定兴奋性 MSC 在正常生理学和病理学中的作用。

SAR7334 (TRCP6-IN-1) 是 TRPC6特异性抑制剂，抑制 TRPC6 电流的 IC50为 7.9 nM。

2-Aminoethyl diphenylborinate (2-APB) 是细胞通透性的 IP3R 和 TRP 通道抑制剂，还抑制 store-operated Ca2+(SOC)通道。

TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

TRPC6-IN-2 是一种 TRPC 蛋白质抑制剂，尤其能够抑制TRPC6蛋白质。

TRPC6-IN-3 (compound 17) 是一种口服具有活力的瞬时受体电位 C6 离子通道 (TRPC6) 抑制剂。TRPC6-IN-3 能够调节细胞内钙浓度，也能够调节包括钙离子和钠离子在内的阳离子通量来调节膜电位。TRPC6-IN-3 可以用于研究呼吸系统。

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。

SAR7334 hydrochloride, a potent and specific inhibitor of TRPC6 (IC50 of 7.9 nM), effectively targets and inhibits the TRPC6 channel.

Larixyl acetate 是一种生物活性化学物质。

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].

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.

GFB-8438 是有效的TRPC5选择性抑制剂，对 hTRPC5 和 hTRPC4 的IC50分别为 0.18 和 0.29 μM。它对 TRPC6、其他 TRP 家族成员、NaV1.5 具有良好的选择性，对 hERG 通道的活性也有限。它对小鼠足细胞的保护作用。

ML204 是有效的TRPC4 TRPC5通道选择性抑制剂，相比于 TRPC6 ，对TRPC4 TRPC5通道的选择性高出 19 倍，不影响其他的 TRP 通道和电压门控的钠、钾或 Ca2+通道。

DS88790512, IC50 at 11 nM, is an effective, selective, oral bioeffective TRPC6 inhibitor.

GSK1702934A 是一种特异性 TRPC3 激动剂，具有促心律失常和正性肌力作用，通过刺激由孔螺旋和跨膜螺旋 S6 形成的细胞外腔的机制直接激活 TRPC6。GSK1702934A 可用于研究糖尿病。

Hyperforin dicyclohexylammonium salt is a transient receptor canonical 6 channel activator with antidepressant effect. It modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels.

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。

PPZ1 is a novel DAG-activated TRPC3 TRPC6 TRPC7 channels activator.

PPZ2 is a novel DAG-activated TRPC3 TRPC6 TRPC7 channels activator.

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.

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 leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

Hyp9为特异性激动剂，针对瞬时受体电位阳离子通道6（TRPC6），应用于脊髓损伤（SCI）的研究。

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。