31
10
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T77511 |
TRPA1-IN-2
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
TRPA1-IN-2 是一种有效且具有口服活性的 TRPA1 抑制剂,IC50 值为 0.04 µM。TRPA1-IN-2 具有抗炎活性。 | |||
T40822 |
TRPA1 Antagonist 3
TRPA1 Antagonist 3 |
||
TRPA1 Antagonist 3 is a compound with photoswitchable properties that acts as an agonist on the TRPA1 channel, providing the ability for optical control. | |||
T39935 |
TRPA1-IN-1
TRPA1-IN-1 |
||
TRPA1-IN-1 is a potent, selective antagonist of the TRPA1 channel, demonstrating significant oral bioavailability as a small molecule. | |||
T13212 | TRPA1 Antagonist 1 | TRP/TRPV Channel | Membrane transporter/Ion channel |
TRPA1 Antagonist 1 is an antagonist of TRPA1(IC50: 8 nM) and is a methylene phosphate prodrug which converts to its active parent drug. | |||
T6617 |
Optovin
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Optovin 是可逆的光活化 TRPA1配体,可实现光介导的神经元兴奋。它通过与氧化还原敏感的半胱氨酸残基产生结构依赖性光化学反应激活 TRPA1。 | |||
T64337 |
PF-04745637
PF4745637,PF 4745637,PF 04745637,PF-4745637 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
PF-04745637 是TRPA1的选择性拮抗剂,对人 TRPA1 的IC50为 17 nM。 | |||
T15628 |
JT010
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
JT010 是一种有效的 TRPA1 激动剂 (EC50 = 0.65 nM)。 | |||
T4385 |
PF-4840154
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
PF4840154 是有效的大鼠和人TrpA1通道选择性激动剂,EC50分别为 97 和 23 nM。PF-4840154 可以诱导 TrpA1 介导的小鼠伤害行为。 | |||
T7430 |
AM-0902
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
AM-0902 是有效的瞬时受体电位 A1 选择性拮抗剂,作用于rTRPA1和hTRPA1的IC50分别为 71 和 131 nM。 | |||
T7205 |
A-967079
(1E,3E)-1-(4-氟苯基)-2-甲基-1-戊烯-3-酮肟 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
A 967079是一种有效的TRPA1受体选择性拮抗剂,对人和大鼠 TRPA1 受体的IC50分别为 67 nM 和 289 nM。A 967079具有良好的CNS 穿透性。 | |||
T21543 |
AP 18
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
AP-18 是选择性的 TRPA1 抑制剂。AP-18 可以抑制 50 μM 肉桂醛诱导的 TRPA1 激活,在小鼠和人中的 IC50 分别为 4.5 μM 和 3.1 μM。AP-18 可以逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 可以浓度依赖的方式减弱 30 μM AITC 诱导的 Yo-Pro 摄取(IC50= 10.3 μM)。 | |||
T6530 |
HC-030031
2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺,HC030031,TOSLAB 829227 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
HC-030031 (TOSLAB 829227) 是一种有效的TRPA1选择性抑制剂,拮抗福尔马林和AITC 诱发的钙流入,IC50分别为5.3±0.2和6.2±0.2μM。 | |||
T8410 |
ASP7663
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
ASP7663 是口服有效的TRPA1选择性激动剂。ASP7663具有抗便秘和抗腹痛的功效。 | |||
T29968 |
AMG-0347
UNII-CD7L9290QR |
TRP/TRPV Channel | Membrane transporter/Ion channel |
AMG-0347 (UNII-CD7L9290QR)是一种靶向TRPA1(瞬时受体电位锚蛋白1)离子通道的小分子抑制剂,是一种在感觉神经元中发现的受体,参与疼痛和环境刺激物的检测。AMG-0347通过阻断TRPA1的功能起作用,具有镇痛作用。 | |||
T2711 |
Chembridge-5861528
TCS 5861528 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Chembridge-5861528 (TCS 5861528) 是有效的 TRPA1离子通道阻断剂。 | |||
T22920 |
LE135
LE 135 |
Retinoid Receptor | Metabolism |
LE135 是一种有效的 RAR 拮抗剂,可选择性结合 RARα (Ki 为 1.4 μM) 和 RARβ (Ki 为 220 nM),对 RARβ 具有更高的亲和力。LE135 对 RARγ,RXRα,RXRβ 和 RXRγ 具有高度选择性。LE135 还是一种有效的 TRPV1 和 TRPA1 受体激活剂,EC50 分别为 2.5 μM 和 20 μM。 | |||
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。 | |||
T2007 |
RQ-00203078
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
RQ00203078是一种口服有效的TRPM8高选择性拮抗剂,对大鼠和人类TRPM8通道的IC50分别为 5.3 nM 和 8.3 nM。它对 TRPV1,TRPA1,TRPV4 或 TRPM2 通道基本没有抑制作用。 | |||
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。 | |||
T21623 |
AS1269574
AS 1269574 |
GPR; TRP/TRPV Channel | Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel |
AS1269574 是口服有效的GPR119激动剂,在表达人 GPR119 的 HEK293 细胞中EC50为 2.5 μM。它激活 TRPA1 阳离子通道,刺激胰高血糖素样肽-1分泌。它仅在高糖条件下特异性诱导胰腺 β 细胞分泌葡萄糖依赖性胰岛素。它在 2 型糖尿病的研究中具有价值。 | |||
T25078 |
AMG9090
AMG 9090,AMG-9090 |
||
AMG9090 is a transient receptor potential ankyrin 1 (TRPA1) antagonist. | |||
T78082 |
Supercinnamaldehyde
|
||
Supercinnamaldehyde是一种有效的瞬时受体电位锚蛋白1(TRPA1)激活剂,具有0.8 μM的EC50值。它通过对半胱氨酸的共价修饰作用来激活TRPA1离子通道。 | |||
T39408 |
GDC-0334
|
||
GDC-0334 is a TRPA1 antagonist useful in treatment TRPA1-mediated diseases, such as pain or asthma. | |||
T69987 |
AMG2504
|
||
AMG2504 is a TRPA1 inhibitor. | |||
T79875 |
GDC-6599
|
||
GDC-6599 (Example 8)为口服活性TRPA1抑制剂,适用于研究TRPA1介导的病症,包括疼痛等。 | |||
T73432 |
BAY-390
|
||
BAY-390 是一种选择性的,跨物种活跃的,可穿透大脑的 TRPA1抑制剂。BAY-390 抑制 hTRPA1 FLIPR,hTRPA1 Ephys,rTRPA1 FLIPR 和 rDRG Ephys,IC50值分别为 16,82,63 和 35 nM。BAY-390 可用于炎症的研究。 | |||
T80843 |
Wasabi Receptor Toxin
WaTx |
||
Wasabi Receptor Toxin通过延长TRPA1通道的开放时间并降低其Ca2+渗透性,从而激活该通道。该化合物被应用于急性与持续性疼痛研究领域。 | |||
T38372 |
2-Fluoro-4-iodo benzonitrile
|
||
2-Fluoro-4-iodo benzonitrile is a building block.1,2It has been used in the synthesis ofL. infantumtrypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors.12-Fluoro-4-iodo benzonitrile has also been used in the synthesis of transient receptor potential ankyrin 1 (TRPA1) antagonists.2 1.Revuelto, A., Ruiz-Santaquiteria, M., de Lucio, H., et al.Pyrrolopyrimidine vs imidazole-phenyl-thiazole scaffolds in nonpeptidic dimerization inhibitors of Leishmania infantum trypan... | |||
T69359 | Ludartin | ||
Ludartin is a TRPA1 channel activator that has been found to produce anticancer effects by inducing DNA damage and a reduction of mitochondrial membrane potential. | |||
T60284 | 4-(Phenyldiazenyl)benzoic acid | ||
4-(Phenyldiazenyl)benzoic acid 是一种光敏和可控的 TRPA1激动剂,可作为研究疼痛信号传导的药理学工具。 | |||
T31995 |
GRC-17536
GRC17536,GRC 17536 |
||
GRC-17536 is an orally available, potent, and selective transient receptor potential anchor protein 1 (TRPA1) inhibitor that has been shown to be highly effective in the treatment of inflammation and neuropathic pain in animal models. The selectivity of G |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8307 |
Hydroxy-α-sanshool
羟基-α-山椒素,Hydroxy-α-sanshool |
Endogenous Metabolite; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
Hydroxy-α-sanshool 是分离自胡椒的烷基酰胺,作为 TRPA1的共价激动剂和 TRPV1的非共价激动剂,EC50分别为69和 1.1 µM。 | |||
T12514 |
Podocarpic acid
|
Others; TRP/TRPV Channel | Membrane transporter/Ion channel; Others |
Podocarpic acid 是一种天然产物,是一种新型 TRPA1 激活剂。 | |||
TQ0001 |
1,4-Cineole
Isocineole,1,4-桉叶素 |
Endogenous Metabolite; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
1,4-Cineole (Isocineole) 是天然广泛分布的含氧单萜烯,存在于桉树油中,可激活人TRPM8和TRPA1。 | |||
TN3575 |
(±)-Cannabichromene
Cannabichromene,大麻色原烯,Cannabichrome |
Cannabinoid Receptor | GPCR/G Protein |
(±)-Cannabichromene 是一种发现于大麻的 2,2-dimethyl-2H-chromene 衍生物。 | |||
TN1927 |
Methyl Kakuol
1-(6-methoxy-1,3-benzodioxol-5-yl)propan-1-one |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Methyl Kakuol 是 TRPA1 的激动剂,EC50 为 0.27 µM,可用于作为 MBST 成分 Asiasari Radix 的活性成分的研究。 | |||
T3727 |
Methyl syringate
Syringic Acid Methyl Ester,丁香酸甲酯 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Methyl syringate (Syringic Acid Methyl Ester) 是水仙花蜜的化学标记物,是有效的细菌和真菌漆酶酚介质。它也是TRPA1激动剂。 | |||
TCS0102 |
Pulegone
胡薄荷酮,(+)-Pulegone,蒲勒酮,胡薄荷酮,长叶薄荷酮 |
Calcium Channel; Endogenous Metabolite; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
Pulegone ((+)-Pulegone) 是 Calamintha nepeta (L.) Savi 的精油的主要化学成分,也是禽类驱虫剂之一。它在禽类物种中驱避作用的分子靶点是伤害感受性 TRP 锚蛋 1。它刺激鸡感觉神经元中的 TRPM8 和 TRPA1 通道,并在高浓度下抑制前者但不抑制后者。 | |||
T7177 |
Capsazepine
|
Apoptosis; TRP/TRPV Channel | Apoptosis; Membrane transporter/Ion channel |
Capsazepine 是一种 TRPV1 受体的拮抗剂, IC50值为 562 nM。 它可阻断由激活 TRPV1 离子通道的辣椒素引起的热痛感,是辣椒素拮抗剂。 | |||
T2994 |
(E)-Cardamonin
Alpinetin chalcone,Cardamomin,小豆蔻明,Cardamonin,(E)-Cardamoni,豆蔻明 |
Apoptosis; TRP/TRPV Channel | Apoptosis; Membrane transporter/Ion channel |
(E)-Cardamonin (Alpinetin chalcone) 是一种新型hTRPA1阳离子通道拮抗剂,IC50值为454 nM。 | |||
T13953 | Umbellulone | Others | Others |
Umbellulone is a natural product isolated from Umbellularia californica, and stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism. |