Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T60003 |
AC1-IN-1
|
Adenylyl cyclase | Neuroscience |
AC1-IN-1 是 1 型腺苷酸环化酶的选择性抑制剂(AC1,IC50 = 0.54 µM)。 | |||
T14844 |
BX430
|
P2X Receptor; Calcium Channel | Membrane transporter/Ion channel; Metabolism; Neuroscience |
BX430 是一种有效的选择性非竞争性变构人 P2X4 受体通道拮抗剂,IC50 为 0.54 μM。它具有物种特异性,可用于治疗慢性疼痛和心血管疾病。 | |||
T8711 |
PF-05186462
PF-05150122 |
Sodium Channel | Membrane transporter/Ion channel |
PF-05186462 (PF-05150122)是选择性的人Nav1.7电压依赖性钠通道抑制剂,IC50为 21 nM,与其他钠通道 (Nav 1.1、1.2、1.3、1.4、1.5、1.6 和 1.8) 相比,它对 Nav1.7显示出显著的选择性。PF-05186462在急性或慢性疼痛中具有研究价值。 | |||
T7416 |
WS-12
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
WS-12 是有效的TRPM8激动剂,EC50为 39 nM。 | |||
T1780 |
Parecoxib
SC 69124,帕瑞昔布,Vorth-P,Valus-P |
COX | Immunology/Inflammation; Neuroscience |
Parecoxib (SC 69124) 是一种有效的选择性 COX-2 抑制剂,是 Valdecoxib 的前药。 | |||
T15781 |
LP-935509
|
Serine/threonin kinase; AAK1 (AP2 associated kinase 1) | Cell Cycle/Checkpoint; Metabolism; Neuroscience |
LP-935509 是一种选择性的、具有脑渗透的、小分子的衔接蛋白-2 相关激酶1 (AAK1) ATP 竞争性抑制剂,其 IC50=3.3 nM,Ki=0.9 nM。它是一种 BIKE 的有效抑制剂 (IC50=14 nM) 和中度的 GAK 抑制剂 (IC50=320 nM)。它能够逆转 SNL 手术后的疼痛。 | |||
T8333 |
Aurintricarboxylic acid
ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056 |
Apoptosis; P2X Receptor; Influenza Virus; Topoisomerase | Apoptosis; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Aurintricarboxylic acid (NSC-4056) 是高效的αβ-亚甲基-ATP 敏感选择性P2X1Rs 和P2X3Rs 变构拮抗剂。 它是核糖核酸酶和拓扑异构酶 II 的有效抑制剂,可阻止核酸与酶结合。 | |||
T31208 |
Dasolampanel
NGX-426,NGX 426,NGX426 |
GluR; iGluR | Membrane transporter/Ion channel; Neuroscience |
Dasolampanel (NGX-426) 是一种可口服的离子型谷氨酸受体 AMPA 和 Kainate 受体拮抗剂,可用于研究慢性疼痛疾病,包括神经性疼痛和偏头痛。 | |||
T34308 |
Rezatomidine
AGN-203818,AGN203818,AGN 203818 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Rezatomidine (AGN203818) 是 α2-肾上腺素能受体的选择性拮抗剂,可用于慢性疼痛研究,包括神经性疼痛。 | |||
T0916 |
Butamben
Butyl 4-aminobenzoate,4-氨基苯甲酸丁酯 |
Potassium Channel; Calcium Channel; Sodium Channel | Membrane transporter/Ion channel; Metabolism |
Butamben (Butyl 4-aminobenzoate) 是一种长效局部麻醉剂,用于治疗慢性疼痛。 | |||
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。 | |||
T78652 |
p38α inhibitor 4
|
p38 MAPK | MAPK |
p38α inhibitor 4 是一种选择性 MAPK p38α抑制剂,看而用于研究糖尿病、疼痛和慢性炎症。 | |||
T50082 |
Org 25543
|
Chloride channel | Membrane transporter/Ion channel |
Org 25543 是一种 N-酰基氨基酸的开发,它选择性地抑制甘氨酸转运蛋白 2 以在大鼠慢性疼痛模型中产生镇痛作用。 | |||
T1197 |
Trimebutine maleate
Debridat,Polibutin,马来酸曲美布汀 |
Calcium Channel; Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Trimebutine maleate (Polibutin) 是一种外周 μ、δ 和 kappa 阿片受体激动剂,用作治疗慢性和急性腹痛的解痉药物。 | |||
T3699 |
Bay 59-3074
|
Cannabinoid Receptor | GPCR/G Protein |
Bay 59-3074 是选择性的CB1/CB2受体的部分激动剂,其在 CB1 受体 (Ki:48.3 nM) 和 CB2 受体 (Ki:45.5 nM)。它可用于缓解疼痛的研究。 | |||
T19812 |
Propentofylline
HWA-285,Karsivan,Propentophylline,Hextol,HWA 285,HWA285 |
PDE | Metabolism |
Propentofylline (Hextol) 是一种甲基黄嘌呤衍生物,具有神经保护、抗增殖和抗炎活性,可增强的突触腺苷信号传导,可用于研究阿尔茨海默病、血管性痴呆、认知障碍、痴呆和慢性疼痛。 | |||
T80641 |
Bupivacaine hydrochloride monohydrate
|
Potassium Channel; Calcium Channel; Sodium Channel; NMDAR | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Bupivacaine hydrochloride monohydrate 是一种 NMDA 受体抑制剂,对钠、L-钙和钾通道有抑制作用。Bupivacaine hydrochloride monohydrate 对 SCN5A 通道有抑制作用,常用于研究慢性疼痛。 | |||
T72023 |
JB002
|
Myosin | Cytoskeletal Signaling |
JB002为一种肌球蛋白 II 抑制剂,IC50值不大于10 μM。适用于研究肌肉痉挛、慢性肌肉骨骼疼痛及肥厚型心肌病。 | |||
T0030L |
Bupivacaine
AH 250,AH-250,AH250,Bupivacaina,Exparel,Anekain |
NMDAR | Neuroscience |
Bupivacaine (AH-250) 是一种 NMDA 受体抑制剂。Bupivacaine 可以阻断钠、L-钙和钾通道。Bupivacaine 有效阻断 SCN5A 通道,IC50 为 69.5 μM。Bupivacaine 可用于慢性疼痛的研究。 | |||
T21013 |
Clomipramine
Chlorimipramine,Anafranil,Clomicalm,Anafranil (free base),Clomipramina,氯米帕明 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Clomipramine (Clomicalm) 是一种三环类抗抑郁药,能够有效阻断 5-HT 再摄取 (IC50:1.5 nM) ,可用于研究强迫症 (OCD) 及抑郁症。 | |||
T16836 |
SAFit2
|
FKBP | Apoptosis; Autophagy; Immunology/Inflammation |
SAFit2是一种高效、具有选择性的fk506结合蛋白51(FKBP51)抑制剂(Ki:6 nM)。SAFit2能增强AKT2-AS160的结合,参与体内糖皮质激素释放的下游反应,是治疗肥胖、慢性疼痛、抑郁和焦虑的候选化合物。 | |||
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。 | |||
T67952 |
JB062
|
Myosin | Cytoskeletal Signaling |
JB062是一种针对非肌肉肌球蛋白(nonmusclemyosin)的抑制剂,其IC50值对骨骼肌肌球蛋白为1.6μM、心肌肌球蛋白为5.4μM,而对平滑肌肌球蛋白II大于100μM。此化合物对人类癌细胞显示出细胞毒性,对正常细胞则无此作用。JB062在肌肉痉挛、慢性肌肉骨骼疼痛及肥厚型心肌病研究中有潜在应用价值。 | |||
T3354 |
BIA 10-2474
BIA10-2474 |
FAAH; Autophagy | Autophagy; Metabolism; Neuroscience |
BIA 10-2474 是一种长效可逆的脂肪酸酰胺水解酶抑制剂,与人类内源性大麻素系统相互作用,可增加中枢神经系统和外周组织,对大鼠大脑不同区域的 IC50值为50至70mg/kg。它用于治疗焦虑症、帕金森氏病和多发性硬化症、高血压或肥胖症的慢性疼痛。 | |||
T30236L | Axelopran sulfate | ||
Axelopran sulfate is used in Oral Therapies for Opioid-induced Bowel Dysfunction in Patients with Chronic Noncancer Pain. | |||
T27481 |
GSK-554418A
GSK554418A |
||
GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model. | |||
T70730 |
Oxycodegol phosphate
|
||
Oxycodegol phosphate is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain | |||
T29084 |
V116517
V-116517,V 116517 |
||
V-116517, a TRPV1 antagonist, is used potentially for the treatment of severe pain due to osteoarthritis and chronic pain due postherpetic neuralgia (PHN). | |||
T32722 |
Lexanopadol
GRT-13106G,GRT6006,GRT 13106G,GRT-6006,GRT 6006,GRT13106G |
||
Lexanopadol (GRT6006) is a potent ORL-1 agonist (opioid receptor-like-1), suitable for the treatment of moderate to severe chronic pain, including neuropathic pain. | |||
T28106 |
MRS5698
MRS 5698,MRS-5698 |
||
MRS5698 is a high affinity and selective agonist of A3 adenosine receptor (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors | |||
T11439 | GNE-616 | Others | Others |
GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor (Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7) for the treatment of chronic pain. | |||
T71225 |
Oxicodegol HCl
|
||
Oxicodegol HCl is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain | |||
T71224 |
Oxicodegol trifluoroacetate
|
||
Oxicodegol trifluoroacetate is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain | |||
T26796 |
BI-44370
|
||
BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain. | |||
T27474 |
GSK-345931A
GSK-345931A free acid,GSK 345931A free acid,GSK 345931A |
||
GSK-345931A, an EP(1) receptor antagonist, shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain. | |||
T38912 | Vicasinabin | ||
Vicasinabin, a potent agonist of cannabinoid receptor 2 (CB2), exhibits promising potential for researching chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and related human diseases. | |||
T39000 |
Zaloglanstat
GRC-27864,ISC-27864 |
||
Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases. | |||
T41091 |
JTS-653
|
||
JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs. | |||
TQ0002L |
A-317491 sodium
A-317491,A 317491,A317491 |
||
A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on peripheral receptors. | |||
TP1559 |
Ziconotide
|
||
Ziconotide is an atypical analgesic agent for the amelioration of severe and chronic pain. Derived from Conus magus, a cone snail, it is the synthetic form of an ω-conotoxin peptide. | |||
T38595 |
EP4 receptor antagonist 3
EP4 receptor antagonist 3 |
||
EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor. It is intended for research purposes in studying EP4 receptor-mediated diseases such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer. | |||
T74739 | Oleoyl-D-lysine | ||
Oleoyl-D-lysine是一种脂质基选择性GlyT2 (甘氨酸转运体-2) 抑制剂,具有逆转小鼠神经性疼痛及抗慢性神经性疼痛嗜睡作用,安全有效,不引发呼吸抑制。 | |||
T71155 | NP-1815-PX | P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
NP-1815-PX是一种选择性P2X4R拮抗剂,显示出抗炎活性并可缓解慢性疼痛模型的疼痛症状。此外,NP-1815-PX能够抑制豚鼠气管/支气管平滑肌(TSM和BSM)的收缩。 | |||
T24692 |
QAQ dichloride
|
||
QAQ dichloride is a photoswitchable compound that blocks voltage-gated Na v and K v channels. Its channel-blocking activity is observed in the trans form of the azobenzene photoswitch, while the cis form does not exhibit this effect. This compound is membrane-impermeant and selectively enters pain-sensing neurons expressing endogenous import channels. QAQ dichloride functions as a light-sensitive analgesic and provides a valuable tool for investigating signaling mechanisms involved in acute and ... | |||
T7772 |
Fast Green FCF
C.I. 42053,固绿 FCF,Food green 3,FD&C Green No. 3 |
Others | Others |
Fast Green FCF (FD&C Green No. 3) 是海绿色三芳基甲烷食用染料,最大吸收在625nm 处,将在电泳过程中的蛋白质染色,。 | |||
T61130 |
SSTR4 agonist 3
|
||
SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor. The SSTR4 receptor is highly expressed in the hippocampus and neocortex, which are regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of pain, both acute and chronic, by reducing peripheral nociception and inflammation. Considering its potential application in pain research, SSTR4 agonist 3 is of interest[1]. | |||
T80485 |
μ-Conotoxin SxIIIC
|
Sodium Channel | Membrane transporter/Ion channel |
μ-Conotoxin SxIIIC是从条纹芋螺(Conus striolatus)提取的不可逆NaV通道(NaV channel)抑制剂,适用于慢性疼痛等神经系统疾病研究。 | |||
T75710 |
Ziconotide TFA
|
||
Ziconotide TFA (SNX-111 TFA),一种肽类化合物,作为高效且选择性的N型钙通道拮抗剂,能减少突触传递,适用于慢性疼痛的研究。 | |||
T62422 | Nav1.8-IN-2 | ||
Nav1.8-IN-2 (compound 35A) 是一种 Nav1.8 的有效抑制剂 (IC50: 0.4 nM)。Nav1.8-IN-2 能够用于疼痛障碍、咳嗽、急性和慢性瘙痒症的研究。 | |||
T68297 | Dilmapimod tosylate | ||
Dilmapimod tosylate is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor. It was investigated for its anti-inflammatory effect in non-head injury trauma patients at risk for developing acute respiratory distress syndrome. IL-1β was identified as a gene regulated by dilmapimod that could influence c-reactive protein levels. Dilmapimod had been in phase III clinical trials by GlaxoSmithKline for the treatment of rheumatoid arthritis, neuropathic pain, coronary artery disease (CAD) and... |