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31

抑制剂 & 化合物

10

天然产物

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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 71131 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 TRPV1TRPA1,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

化合物

TRPA1-IN-2
Cat.No: T77511
Synonym:
Target: TRP/TRPV Channel
TRPA1 Antagonist 3
Cat.No: T40822
Synonym: TRPA1 Antagonist 3
Target:
TRPA1-IN-1
Cat.No: T39935
Synonym: TRPA1-IN-1
Target:
TRPA1 Antagonist 1
Cat.No: T13212
Synonym:
Target: TRP/TRPV Channel
Optovin
Cat.No: T6617
Synonym:
Target: TRP/TRPV Channel
PF-04745637
Cat.No: T64337
Synonym: PF4745637,PF 4745637,PF 04745637,PF-4745637
Target: TRP/TRPV Channel
JT010
Cat.No: T15628
Synonym:
Target: TRP/TRPV Channel
PF-4840154
Cat.No: T4385
Synonym:
Target: TRP/TRPV Channel
AM-0902
Cat.No: T7430
Synonym:
Target: TRP/TRPV Channel
A-967079
Cat.No: T7205
Synonym: (1E,3E)-1-(4-氟苯基)-2-甲基-1-戊烯-3-酮肟
Target: TRP/TRPV Channel
AP 18
Cat.No: T21543
Synonym:
Target: TRP/TRPV Channel
HC-030031
Cat.No: T6530
Synonym: 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
Target: TRP/TRPV Channel
ASP7663
Cat.No: T8410
Synonym:
Target: TRP/TRPV Channel
AMG-0347
Cat.No: T29968
Synonym: UNII-CD7L9290QR
Target: TRP/TRPV Channel
Chembridge-5861528
Cat.No: T2711
Synonym: TCS 5861528
Target: TRP/TRPV Channel
LE135
Cat.No: T22920
Synonym: LE 135
Target: Retinoid Receptor
Pico145
Cat.No: T16532
Synonym: HC-608
Target: TRP/TRPV Channel
RQ-00203078
Cat.No: T2007
Synonym:
Target: TRP/TRPV Channel
Diphenyleneiodonium chloride
Cat.No: T7191
Synonym: 二苯基氯化碘盐,DPI
Target: NOS, Reactive Oxygen Species, NADPH, TRP/TRPV Channel
AS1269574
Cat.No: T21623
Synonym: AS 1269574
Target: GPR, TRP/TRPV Channel
AMG9090
Cat.No: T25078
Synonym: AMG 9090,AMG-9090
Target:
Supercinnamaldehyde
Cat.No: T78082
Synonym:
Target:
GDC-0334
Cat.No: T39408
Synonym:
Target:
AMG2504
Cat.No: T69987
Synonym:
Target:
GDC-6599
Cat.No: T79875
Synonym:
Target:
BAY-390
Cat.No: T73432
Synonym:
Target:
Wasabi Receptor Toxin
Cat.No: T80843
Synonym: WaTx
Target:
2-Fluoro-4-iodo benzonitrile
Cat.No: T38372
Synonym:
Target:
Ludartin
Cat.No: T69359
Synonym:
Target:
4-(Phenyldiazenyl)benzoic acid
Cat.No: T60284
Synonym:
Target:
GRC-17536
Cat.No: T31995
Synonym: GRC17536,GRC 17536
Target:
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.

天然产物

Hydroxy-α-sanshool
Cat.No: T8307
Synonym: 羟基-α-山椒素,Hydroxy-​α-​sanshool
Target: Endogenous Metabolite, TRP/TRPV Channel
Podocarpic acid
Cat.No: T12514
Synonym:
Target: Others, TRP/TRPV Channel
1,4-Cineole
Cat.No: TQ0001
Synonym: Isocineole,1,4-桉叶素
Target: Endogenous Metabolite, TRP/TRPV Channel
(±)-Cannabichromene
Cat.No: TN3575
Synonym: Cannabichromene,大麻色原烯,Cannabichrome
Target: Cannabinoid Receptor
Methyl Kakuol
Cat.No: TN1927
Synonym: 1-(6-methoxy-1,3-benzodioxol-5-yl)propan-1-one
Target: TRP/TRPV Channel
Methyl syringate
Cat.No: T3727
Synonym: Syringic Acid Methyl Ester,丁香酸甲酯
Target: TRP/TRPV Channel
Pulegone
Cat.No: TCS0102
Synonym: 胡薄荷酮,(+)-Pulegone,蒲勒酮,胡薄荷酮,长叶薄荷酮
Target: Calcium Channel, Endogenous Metabolite, TRP/TRPV Channel
Capsazepine
Cat.No: T7177
Synonym:
Target: Apoptosis, TRP/TRPV Channel
(E)-Cardamonin
Cat.No: T2994
Synonym: Alpinetin chalcone,Cardamomin,小豆蔻明,Cardamonin,(E)-Cardamoni,豆蔻明
Target: Apoptosis, TRP/TRPV Channel
Umbellulone
Cat.No: T13953
Synonym:
Target: Others
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