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14
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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T74742 |
TRPV1 activator-2
|
Others | Others |
TRPV1 activator-2 (compound 9)为辣椒素类似物,特异性与脂-水通道残基相互作用。 | |||
T61788 |
TRPV1 antagonist 3
|
Others | Others |
TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1]. | |||
T74741 |
TRPV1 activator-1
|
Others | Others |
TRPV1 activator-1 (compound 8),一种颈部结构经过改变的辣椒素类似物,特异性与T551残基相互作用。 | |||
T83701 |
TRPV1-Tat TFA
Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat |
||
TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时,它能增加大鼠后爪机械痛阈。 | |||
T22360 |
MDR-652
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
MDR-652是瞬时受体电位香草酸亚型 1 的选择性激动剂,对 hTRPV1 和 rTRPV1 的Ki 分别为 11.4 和 23.8 nM,EC50分别为 5.05 和 93 nM。MDR-652在缓解疼痛方面有研究的价值。 | |||
T23322 |
SB 452533
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
SB 452533 是TRPV1的选择性拮抗剂,pKb 为 7.8。 | |||
T15758 |
Linopirdine
利诺吡啶,DuP 996 |
Potassium Channel; TRP/TRPV Channel | Membrane transporter/Ion channel |
Linopirdine (DuP 996) 是一种口服有效的,选择性 M 型 K+电流 (IM;Kv7;KCNQ Channels) 抑制剂,IC50为 2.4 μM。Linopirdine 是TRPV1激活剂。Linopirdine 是一种公认的认知增强药物,可增加大鼠脑组织中乙酰胆碱的释放。 | |||
T7526 |
JNJ-17203212
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
JNJ-17203212 是一种竞争性 TRPV1选择性拮抗剂。它被开发用于疼痛处理的研究。 | |||
T8562 |
A 425619
1-(4-(TRIFLUOROMETHYL)BENZYL)-3-(ISOQUINOLIN-5-YL)UREA |
TRP/TRPV Channel | Membrane transporter/Ion channel |
A 425619 (1-(4-(TRIFLUOROMETHYL)BENZYL)-3-(ISOQUINOLIN-5-YL)UREA) 是一种有效的 TRPV1 拮抗剂。 | |||
T6977 |
SB-366791
SB366791 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
SB366791 是一种有效的 vanilloid receptor (VR1/TRPV1)选择性拮抗剂 (IC50=5.7 nM)。SB-366791 在炎症方面有研究价值。 | |||
T6379 |
AMG 517
AMG517,N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺,AMG-517 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
AMG 517是一种有效的香草素受体-1 (TRPV1) 拮抗剂,IC50为0.5 nM。 | |||
T7189 |
AMG9810
(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
AMG9810是高效的,竞争性的香草素受体1选择性拮抗剂,对人类和大鼠TRPV1的IC50分别为24.5 和 85.6 nM。 | |||
T12306 |
OMDM-5
|
Cannabinoid Receptor; Endogenous Metabolite; TRP/TRPV Channel | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂,Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂,EC50为 75 nM,显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。 | |||
T6660 |
SB-705498
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
SB705498 是一种口服有效的 TRPV1选择性拮抗剂,pIC50值为 7.1。 | |||
T39349 |
Vocacapsaicin hydrochloride
CA-008 hydrochloride |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Vocacapsaicin hydrochloride (CA-008 hydrochloride) 是非阿片类 TRPV1 激动剂,是辣椒素的原料,可用于缓解疼痛。 | |||
T12307 |
OMDM-6
|
Cannabinoid Receptor; Endogenous Metabolite; TRP/TRPV Channel | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
OMDM-6 是 TRPV1(EC50 = 75 nM) 和 CB1 (Ki = 3.2 μM) 的双重激动剂。 OMDM-6 抑制 anandamide 细胞摄取,Ki 为 7.0 μM。 | |||
T29522L |
(S)-ABT 102
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea 是一种有效的TRPV1拮抗剂,其IC50为123 nM,可阻断capsaicin 对TRPV1的激活。 | |||
T33429 |
MK-2295
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
MK-2295 是一种有效的 TRPV1 拮抗剂。 MK-2295 可用于治疗慢性疼痛的研究。 | |||
T8440 |
LASSBio-1135
|
TNF; TRP/TRPV Channel | Apoptosis; Membrane transporter/Ion channel |
LASSBio-1135 是一种口服有效的 TRPV1 拮抗剂和 TNF-α 生成抑制剂。 | |||
T23118 |
PALDA
|
Others | Others |
PALDA potentiates TRPV1-mediated effects of NADA. | |||
T7102 |
BCTC
N-(4-叔丁苯基)-4-(3-氯吡啶-2-基)哌嗪-1-甲酰胺 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
BCTC 是有效的、特异性的瞬时受体阳离子通道M8(TRPM8)抑制剂。 | |||
T62530 |
N-Arachidonyldopamine
NADA |
Cannabinoid Receptor | GPCR/G Protein |
N-Arachidonyldopamine (NADA) 是一种选择性的、强效的内源性 CB1 受体激动剂 (Ki: 250 nM)。N-Arachidonyldopamine 也是一种有效的、选择性 TRPV1 激动剂,其 EC50 值 ~50 nM。 | |||
T16014 |
Mavatrep
JNJ-39439335 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Mavatrep (JNJ-39439335) 是一种特异性的 TRPV1 拮抗剂,Ki 为 6.5 nM,可用于炎症性疼痛的研究。 | |||
T29522 |
ABT 102
ABT102,CHEMBL398338,ABT-102 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
ABT 102 (CHEMBL398338) 是瞬时受体电位香草素 1 (TRPV1) 受体的选择性拮抗剂。 | |||
T9818 |
NGD-8243
NGD8243,N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine |
TRP/TRPV Channel | Membrane transporter/Ion channel |
NGD-8243 (N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine) 是一种 TRPV1 抑制剂,可用于预防和治疗心脏肥大的研究。 | |||
T15192 |
Eact
|
Chloride channel | Membrane transporter/Ion channel |
Eact 是一种选择性和有效的 TMEM16A 激活剂,可直接激活感觉伤害感受器中的 TRPV1 通道,还会产生瘙痒、急性伤害感受和热过敏。 | |||
T14087 |
ABT-239
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂,也是一种TRPV1拮抗剂。 | |||
T28118 |
MSP3
MSP-3,MSP 3 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
MSP3 是瞬时受体电位香草素 1 型的激动剂 (EC50 = 0.87 μM) ,具有镇痛和神经保护作用。 | |||
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。 | |||
T4693 |
2-Aminoethyl diphenylborinate
2-Aminoethoxydiphenyl borate,二苯基酸,2-APB |
Calcium Channel; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
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。 | |||
T9247 |
Vanilloid receptor antagonist 1
4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) 是香草酸受体的有效拮抗剂。 | |||
T36064 |
N-Oleoyl Glutamine
Oleoyl-L-glutamine |
TRP/TRPV Channel | Membrane transporter/Ion channel |
N-Oleoyl Glutamine (Oleoyl-L-glutamine) 是参与 PM20D1 调控的N-酰基氨基酸,拮抗瞬时受体电位 (TRP) 钙通道的 TRPV1。 | |||
T37097 |
SET 2
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
SET 2 是瞬时受体电位香草酸 2 型 (TRPV2) 的拮抗剂,IC50 为 0.46 μM。 SET 2 显示了对 TRPV1、TRPV3 和 TRPV4 的选择性。 | |||
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。 | |||
T22124 |
Oleoyl Serotonin
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Oleoyl Serotonin 是 hTRPV1 的拮抗剂,IC50(Human TRPV1) 为 2.57 μM。 | |||
T34081 |
Piromelatine
NEU-P-11,NEU-P 11,NEU-P11 |
P2X Receptor; 5-HT Receptor; MT Receptor; Sodium Channel; TRP/TRPV Channel | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂,也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性,对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用,可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。 | |||
T8425 |
Linoleoyl Ethanolamide
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Linoleoyl ethanolamide 是脂肪酸乙醇酰胺。它可弱结合 CB1 和 CB2 受体,并分别抑制[3H]CP-55,940的结合,Ki 分别为 10 和 25μM。它在引起小鼠过氧化氢酶方面的效力是 anandamide 的4倍,且对睡眠时间无延长效果。 | |||
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。 | |||
T7502 |
PF 05089771 tosylate
|
Sodium Channel | Membrane transporter/Ion channel |
PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。 | |||
T1109 |
(Z)-Capsaicin
Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素 |
TRP/TRPV Channel; HSV | Membrane transporter/Ion channel; Microbiology/Virology |
(Z)-Capsaicin (Zucapsaicin) 是天然辣椒素的合成顺式异构体,用于治疗膝骨关节炎。它是一种可口服的 TRPV1激动剂,可研究神经性疼痛。 | |||
T23106 |
Olvanil
N-Vanillyloleamide,奥伐尼,N-Vannilyloleoylamide |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Olvanil (N-Vannilyloleoylamide) 是一种vanilloid 受体激动剂,EC50为0.7nM。 | |||
T22515 |
5'-Iodoresiniferatoxin
|
Others | Others |
TRPV1 (VR1) receptor antagonist | |||
T14067 |
A-1165442
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM. | |||
T15634 |
JYL 1421
SC 0030 |
TRP/TRPV Channel | Membrane transporter/Ion channel |
JYL 1421 (SC 0030) 是 TRPV1 的拮抗剂 (IC50 = 8 nM)。 | |||
T23778 |
BCTP
|
Others | Others |
BCTP is a polymodal inhibitor of TRPV1. It has a reduced liability for hyperthermia. | |||
T68256 |
JNJ-38893777
|
Others | Others |
JNJ-38893777 is a potent and selective transient receptor potential vanilloid 1 (TRPV1) channel antagonist. | |||
T68271 |
AZD1386
|
Others | Others |
AZD1386 is a TRPV1 antagonist. AZD1386 acts as a competitive antagonist at the channel's capsaicin binding site. | |||
T84630 |
N-Linolenoylethanolamine
α-Linolenoyl ethanolamide,18:3 NAE |
Others | Others |
N-Linolenoylethanolamine (18:3 NAE) 为一种内源性大麻素,同时也是香草素受体(TRPV1)的激动剂。 | |||
T28876 |
SU-200
SU 200 |
Others | Others |
SU-200 is a TRPV1 agonist. | |||
T24504 |
MSK-195
MSK 195,MSK195 |
Others | Others |
MSK-195 is an effective TRPV1 agonist. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1062 |
Capsaicin
Qutenza,8-Methyl-N-vanillyl-trans-6-nonenamide,天然辣椒素,Vanilloid,辣椒素,(E)-Capsaicin,Zostrix |
Apoptosis; TRP/TRPV Channel; Autophagy | Apoptosis; Autophagy; Membrane transporter/Ion channel |
Capsaicin ((E)-Capsaicin) 属于天然产物,提取自辣椒,是一种 TRPV1 激动剂 (EC50=0.29 μM)。Capsaicin 具有抗肿瘤、抗炎、抗氧化、神经保护等活性。 | |||
TN2429 |
Capsiate
|
Antioxidant; TRP/TRPV Channel | Membrane transporter/Ion channel; oxidation-reduction |
Capsiate 是一种具有口服活性的 TRPV1 激动剂,是非刺激性辣椒素类似物,可作为抗过敏剂,具有抗炎、抗氧、降糖和抑制血管生成活性。 | |||
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。 | |||
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。 | |||
T21165 |
Pellitorine
AI3-19560,墙草碱,Pellitorin |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Pellitorine (Pellitorin) 是提取自 Piper nigrum 的根的一种化合物。它对 HL60 和 MCT-7 细胞系表现出显著的细胞毒活性。它可用于癌症疾病的研究。 | |||
TN6791 |
Palvanil
Hexadecanamide |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Palvanil (Hexadecanamide) 是一种快速脱敏的 TRPV1 激动剂。它可能是治疗 IBS 的有前途的药物,因为它可以调节肠道蠕动并减轻内脏疼痛。 | |||
T2845 |
Imperatorin
Ammidin,8-Isoamylenoxypsoralen,欧前胡素,8-Isopentenyloxypsoralene,Marmelosin,Pentosalen |
TRP/TRPV Channel; AChR; AChE; NOD | Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; NF-κB |
Imperatorin (8-Isopentenyloxypsoralene) 是NO synthesis 和BChE 的抑制剂,IC50分别为 9.2 μmol 和 31.4 μmol。它也是TRPV1的微弱激动剂,EC50为 12.6±3.2 μM。 | |||
TN1377 |
α-Spinasterol
Α-波菜甾醇,alpha-Spinasterol,菠甾醇 |
COX; Antibacterial; TRP/TRPV Channel | Immunology/Inflammation; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
α-Spinasterol 是一种从Spinacia oleracea 分离的瞬时受体电位香草酸 1 拮抗剂,具有抗菌、抗炎、抗抑郁、抗氧化和抗伤害作用。它抑制COX-1和COX-2活性,IC50值分别为 16.17 μM 和 7.76 μM。 | |||
T2807 |
Caffeic Acid
|
Lipoxygenase; Endogenous Metabolite; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
Caffeic acid 是5-脂氧合酶和 TRPV1离子通道的双重抑制剂。 | |||
T6S1684 |
8-Gingerol
|
Antioxidant; Antibacterial; TRP/TRPV Channel | Membrane transporter/Ion channel; Microbiology/Virology; oxidation-reduction |
8-Gingerol 分离自姜的根状茎,是口服有效的 TRPV1激活剂,EC50值为5.0 µM。8-Gingerol 抑制 COX-2,还能抑制体外 H. pylori 的生长。 | |||
T5786 |
TETRAHYDROPIPERINE
四氢胡椒碱,Cosmoperine |
P450; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
Tetrahydropiperine (Cosmoperine) 是胡椒碱的环己基类似物,也是一种天然芳基戊酰胺,从Piper longum 分离得到。它对细胞色素 P450 (CYP) 同工型 CYP1A1/芳基烃羟化酶 (AHH;IC50=23 µM)具有抑制作用。 | |||
T2163 |
Dihydrocapsaicin
CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide |
Others; TRP/TRPV Channel | Membrane transporter/Ion channel; Others |
Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素,是TRPV1的选择性激动剂,同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。 | |||
T60741 |
Dihydrocapsiate
|
Others | Others |
Dihydrocapsiate 可用于研究代谢疾病,是二氢 capsinoid 家族的一种化合物。Dihydrocapsiate 口服有效的 TRPV1激动剂。 | |||
T13582 |
Bisandrographolide C
|
Others | Others |
Bisandrographolide C is identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels (Kds: 289 and 341 μM) and protects cardiomyocytes from hypoxia-reoxygenation injury. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-02740 |
IL-31R alpha Protein, Mouse, Recombinant (His)
ZcytoR17,Interleukin-31 receptor subunit a... |
Mouse | E. coli |
Associates with OSMR to form the interleukin-31 receptor which activates STAT3 and to a lower extent STAT1 and STAT5. May function in skin immunity. Mediates IL31-induced itch, probably in a manner dependent on cation channels TRPA1 and TRPV1. Positively regulates numbers and cycling status of immature subsets of myeloid progenitor cells in bone marrow in vivo and enhances myeloid progenitor cell survival in vitro. IL-31R alpha Protein, Mouse, Recombinant (His) is expressed in E. coli expression... |