71
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2710 |
TCS 1102
|
OX Receptor | GPCR/G Protein; Neuroscience |
TCS 1102 是双食欲素受体拮抗剂,对 OX1和OX2受体的Ki 分别为3和 0.2 nM。 | |||
T77676 |
(Z)-Metanicotine 2HCl
(Z)-Metanicotine 2HCl(1129-68-6 Free base) |
Others | Others |
(Z)-Metanicotine 2HCl 具有镇痛活性,可用于治疗中枢系统疾病。 | |||
T0702 |
Gabapentin
Neurontin,Gabapentine,加巴喷丁,Aclonium |
Calcium Channel; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Gabapentin (Neurontin) 是GABA 类似物,是一种抗癫痫药,可用于缓解神经性疼痛。 | |||
T1413 |
Pentetrazol
Metrazole,Pentylenetetrazole,Pentylenetetrazol,戊四唑,PTZ,pentamethylenetetrazol,Cardiazol |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Pentetrazol 是一种 GABA(A) 受体拮抗剂,具有中枢神经系统和呼吸兴奋剂的活性。 | |||
T1946 |
Felbamate
W-554,ADD-03055,非尔氨酯,非巴马特 |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
Felbamate (W-554) 是非镇静性抗痉挛剂,可通过降低中枢神经系统紊乱的电活动起作用。 | |||
T77731 |
ERK5-IN-6
|
ERK | MAPK |
ERK5-IN-6 是一种有效的 ERK5 激酶抑制剂。ERK5-IN-6 具有抗增殖活性、抗惊厥活性和抗肿瘤活性,可用于研究中枢神经系统相关疾病。 | |||
T68127 |
Picenadol
LY-150720,LY150720,LY 150720 |
Others | Others |
Picenadol (LY 150720) 是N-甲基-4-苯基哌啶衍生物的外消旋混合物,具有激动剂 - 拮抗剂阿片性质。Picenadol 具有中枢镇痛活性。 | |||
T6445 |
Cilomilast
SB-207499,西洛司特,Ariflo |
PDE | Metabolism |
Cilomilast (SB-207499) 是选择性的、口服具有活性的磷酸二酯酶 4 抑制剂。 它对 PDE4 的选择性高于 PDE1,PDE2,PDE3 和 PDE5 (IC50=74,65,>100,83 µM)。它具有抗炎和免疫调节功能,可用于研究哮喘和慢性阻塞性肺疾病。 | |||
T6649 |
(S)-(+)-Rolipram
(S)-Rolipram,(+)-Rolipram,盐酸环胞苷,S- (+)-Rolipram |
Apoptosis; PDE | Apoptosis; Metabolism |
(S)-(+)-Rolipram ((+)-Rolipram) 是一种 cAMP 依赖性磷酸二酯酶 4 (PDE4) 抑制剂,IC50=1100 nM。它能够抑制人单核细胞产生的肿瘤坏死因子 α (TNFα)。 | |||
T0440 |
Oxcarbazepine
GP 47680,奥卡西平 |
Apoptosis; Sodium Channel | Apoptosis; Membrane transporter/Ion channel |
Oxcarbazepine (GP 47680) 是一种钠通道阻滞剂,有效抑制胶质母细胞瘤细胞生长并诱导胶质母细胞瘤细胞凋亡或 G2/M 停滞,具有抗癌和抗惊厥作用。 | |||
T2407 |
Tiagabine
噻加宾,TGB,NO050328,Gabitril,NO328 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Tiagabine (NO050328) 是具有抗惊厥特性的选择性 GABA 再摄取抑制剂,在突触体、神经元和神经胶质中,能够抑制 [3H]GABA 的重摄取,IC50值分别为 67、446 和 182 nM。 | |||
T0680 |
Lamotrigine
LTG,BW430C,拉莫三嗪 |
5-HT Receptor; Sodium Channel; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Lamotrigine (BW430C) 是一种抗癫痫剂和情绪稳定剂,可研究癫痫、局灶性癫痫等。。它选择性地阻断电压门控钠离子通道,稳定突触前神经元膜,抑制谷氨酸释放。 | |||
T2156 |
WP1066
|
Apoptosis; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
WP1066 是一种新型JAK2和STAT3抑制剂,对 STAT5 和 ERK1/2 也起作用。它用于研究黑色素瘤、脑癌、实体瘤和中枢神经系统肿瘤治疗。 | |||
T60707 |
Quinupramine
|
||
Quinupramine 具有口服活性的抗抑郁剂,其抗抑郁活性与中枢血清素系统有关,与 β- 肾上腺素能系统无关。Quinupramine 能够渗入中枢神经系统并且影响某些神经传递的过程。 | |||
T16115 |
MLi-2
|
LRRK2 | Autophagy |
MLi-2 是一种结构新颖、高效、选择性的 LRRK2 激酶抑制剂,具有中枢神经系统活性,IC50为 0.76 nM,有潜力用于帕金森氏病。 | |||
T0806 |
Flunarizine dihydrochloride
Flunarizine 2HCl,KW-3149,R14950,盐酸氟桂利嗪 |
Calcium Channel; Dopamine Receptor; Sodium Channel | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Flunarizine dihydrochloride (R14950) 是 Na+/Ca2+(T 型) 通道双重阻滞剂。它也是 D2多巴胺受体拮抗剂。它具有用于扩张外周血管和预防偏头痛的潜力。 | |||
T10893 |
CS-722 Free base
|
Others | Others |
CS-722 Free base是一种合成的中枢作用肌肉松弛剂,它展现出肌肉松弛效果并抑制脊髓反射。可能通过限制钠和钙流动,从而在海马培养物中减少自发的抑制性和兴奋性突触后电流。 | |||
T1790 |
Fosaprepitant dimeglumine
福沙匹坦二甲葡胺,L785298,福沙吡坦二甲葡胺,MK-0517,Fosaprepitant dimeglumine salt |
Neurokinin receptor | GPCR/G Protein; Neuroscience |
Fosaprepitant dimeglumine (MK-0517) 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂,可用于预防化疗引起的恶心呕吐。 | |||
T1483 |
Citalopram hydrobromide
Lu 10-171,Nitalapram HBr,Bonitrile HBr,XU-62-320,Lu 10-171 HBr,氢溴酸西酞普兰,Citalopram HBr |
5-HT Receptor; Serotonin Transporter; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Citalopram hydrobromide (XU-62-320) 是一种选择性 5-羟色胺再摄取抑制剂,可选择性地抑制 CNS 神经元对 5-羟色胺的再摄取,从而增强中枢神经系统中的 5-羟色胺能活性,也具有抗抑郁活性。它抑制兔血小板中 5-HT 的摄取,IC50为 14 nM。 | |||
T26778 |
Besipirdine
HP 749 free base,P-867493,P867493,HP 749,HP749,P 867493 |
Sodium Channel; Adrenergic Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Besipirdine (HP 749 free base)是一种非受体依赖性拟胆碱化合物,具有α-肾上腺素能活性和心血管活性。Besipirdine 抑制电压依赖性钠钾通道,抑制生物胺的摄取。Besipirdine 可减少大鼠的时间表诱导的烦渴,增强中枢神经系统中的胆碱能和肾上腺素能神经传递。 | |||
T7656 |
Apelin-13
|
||
Apelin-13 是存在于中枢和外周神经系统由13个氨基酸组成的多肽序列,是 G 蛋白偶联受体angiotensin II protein J (APJ) 的内源性配体,对 APJ 的 EC50 值为 0.37 nM。Apelin-13 具有扩张血管和降压活性,可用于研究 2 型糖尿病综合征。 | |||
T3716 |
Rolapitant
罗拉吡坦,SCH619734,罗拉匹坦 |
Neurokinin receptor | GPCR/G Protein; Neuroscience |
Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂,Ki 值为0.66 nM。 | |||
T6426 |
Buclizine dihydrochloride
盐酸安其敏,Longifene,Buclina,Buclizine HCl,UCB-4445 |
5-HT Receptor; AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Buclizine dihydrochloride (Buclina) 是可口服的一种哌嗪组胺 H1 受体拮抗剂,主要具有止吐和抗眩晕活性。 | |||
T13330 |
WAY-213613 hydrochloride
WAY-213613 hydrochloride (868359-05-1 free base) |
transporter | Metabolism |
WAY-213613 hydrochloride 是一个有效,选择性的,非底物再摄取 GLT-1/EAAT2抑制剂,具有有效的 EAAT2 抑制活性,IC50值为 85 nM,它是阐明 EAAT2 功能的潜在工具,可用于中枢神经系统的研究。 | |||
T61025 |
GSK-1482160
|
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
GSK-1482160是一种CNS-渗透的P2X7受体负变构调节剂,具有口服活性。P2X7受体参与中枢和外周免疫细胞产生促炎细胞因子,因此GSK-1482160具有研究炎症性疾病的潜力。GSK-1482160具有出色的体外效价(在包括人类在内的多种物种的重组和初始P2X7受体的功能和电生理测试中)和交叉靶标选择性。 | |||
T23440 |
TC-N 22A
|
GluR | Neuroscience |
TC-N 22A 是一种作用力强的、可选择的、口服具有活性的、可以通过血脑屏障的 mGlu4 正向别构调节剂 (PAM)。TC-N 22A 在表达人 mGlu4 的 BHK 细胞中 EC50 表现为 9 nM。TC-N 22A 在激动和正向别构模型中对 mGlu 1、2、3、5 和 7 受体的活性表现很低 (EC50 >10 μM)。TC-N 22A 可以用于中枢神经系统疾病的研究。 | |||
T0455 |
Clozapine
氯氮平,HF 1854,LX 100-129 |
Dopamine Receptor; Adrenergic Receptor; AChR | GPCR/G Protein; Neuroscience |
Clozapine (HF 1854) 是一种三环二苯二氮卓类药物,属于非典型抗精神病药物。它结合几种类型的中枢神经系统受体,并显示出独特的药理学特征。 它是一种血清素拮抗剂,与 5-HT 2A/2C 受体亚型具有强结合力。它还对几种多巴胺能受体表现出很强的亲和力,但对多巴胺 D2 受体仅表现出较弱的拮抗作用,这种受体通常被认为可调节精神抑制活性。 | |||
T68599 |
Orphenadrine
Orphenadrine (free base) |
Sodium Channel; NMDAR; AChR | Membrane transporter/Ion channel; Neuroscience |
Orphenadrine 是一种非竞争性的 N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,以浓度依赖性方式抑制克隆的 HERG 通道,在 HEK 细胞中产生0.85μM 的 IC。Orphenadrine 是中枢和外周毒蕈碱受体的拮抗剂,通过孔残基 Y652或 F656突变阻断衰减。 Orphenadrine 具有抗痉挛、镇痛和抗胆碱能活性,对在体外和体内对谷氨酸神经毒性具有保护作用。Orphenadrine 对钠离子通道具有抑制作用,可用来治疗帕金森。 | |||
T27379 |
FR-194921
FR194921 |
||
FR-194921 is a potent, selective, and orally active antagonist for central adenosine A1 receptors with cognitive-enhancing and anxiolytic activity. FR194921 has same binding affinity profile among human, rat, and mouse. | |||
T73342 |
Prenderol
2,2-Diethyl-1,3-propanediol |
||
Prenderol 是一种有效的中枢神经系统抑制剂。Prenderol 具有抗惊厥活性。 | |||
TP2194 |
Neuropeptide Y (scrambled)
|
Others | Others |
Neuropeptide Y (NPY) is a 36-amino acid neuropeptide that exerts its activity via G-protein-coupled receptors. NPY is widely distributed in the peripheral and central nervous systems. It modulates a variety of physiological processes, e.g. the central reg | |||
TP2139 |
AMY-101
Cp40 |
Others | Others |
AMY-101 is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). AMY-101 shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation. | |||
TP2139L |
AMY-101 TFA
Cp40 TFA |
Others | Others |
AMY-101 TFA (Cp40 TFA) is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). AMY-101 TFA shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation. | |||
T71160 |
Levomepromazine HCl
|
||
Levomepromazine HCl is a phenothiazine with pharmacological activity similar to that of both CHLORPROMAZINE and PROMETHAZINE. It has the histamine-antagonist properties of the antihistamines together with CENTRAL NERVOUS SYSTEM effects resembling those of chlorpromazine. | |||
T36644 | Rezivertinib | ||
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2]. | |||
T61427 | Lamivudine salicylate | ||
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI) that effectively inhibits the reverse transcriptase activity of both HIV 1/2 and hepatitis B virus. Moreover, it demonstrates the ability to penetrate the central nervous system [1] [2]. | |||
T38049 |
Glycerophospho-N-Palmitoyl Ethanolamine
|
||
N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. For example, arachidonoyl ethanolamide (AEA) is an endogenous neurotransmitter that evokes cellular responses by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). The different types of NAE are derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-palmitoyl ethanolamine (GP-NPEA) is the metabo... | |||
T40473 |
rCRAMP (rat)
|
||
rCRAMP (rat), the rat cathelin-related antimicrobial peptide, plays a crucial role in the antibacterial activity found in rat brain peptide/protein extracts. As a potential key player in the innate immune system of the rat central nervous system, rCRAMP (rat) serves to enhance immune response. | |||
T76440 |
Peptide E
|
||
Peptide E,作为kappa阿片受体激动剂,显示出显著的阿片受体结合活性,具IC50值为0.39 μM,适用于中枢神经系统研究。 | |||
T61784 |
GlcN-6-P Synthase-IN-1
|
||
GlcN-6-P Synthase-IN-1 (Compound 4d) is a potent inhibitor of Glucosamine-6-phosphate (GlcN-6-P) synthase, with an IC50 of 3.47 μM. This compound demonstrates remarkable antimicrobial activity and exhibits excellent penetration in the central nervous system. Additionally, GlcN-6-P Synthase-IN-1 is capable of inhibiting cytochrome P450, specifically the CYP3A4 isoform [1]. | |||
T37182 |
AX 048
|
||
The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of r... | |||
T29938 |
AM-3102
KDS-5104,AM 3102,Methyl oleoylethanolamide |
||
AM-3102 is an OEA analog that stimulates PPARα transcriptional activity and prolongs feeding latency. It is resistant to enzymatic hydrolysis and is as potent as OEA in enhancing transcriptional activity of PPARα and reducing food intake in free-feeding r | |||
T60445 |
Desipramine
|
||
Desipramine 是一种具有抗抑郁活性的三环类化合物。Desipramine 可抑制中枢神经系统的去甲肾上腺素再摄取受体,减少睡眠相关的腮舌肌活性丧失,可用于改善咽塌陷的研究。 | |||
T73655 | Frakefamide TFA | ||
Frakefamide TFA 是一种有效的止痛药物,作为μ 受体的选择性外围激动剂。该化合物不能穿透血脑屏障,因此不进入中枢神经系统。 | |||
T36591 |
ABD459
|
||
ABD459 is a neutral antagonist of the central cannabinoid 1 (CB1) receptor (Ki = 8.6 nM). It inhibits food consumption in nonfasted mice without affecting motor activity. ABD459 reduces active food seeking for 5-6 hours after treatment, with no rebound after washout. ABD459 also diminishes rapid eye movement (REM) sleep, with no alterations of wakefulness or non-REM sleep. | |||
T36813 | Lu AE98134 | ||
Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1]. | |||
TP2049 |
CRSP-1
|
||
Endogenous central calcitonin (CT) receptor agonist that stimulates cAMP formation at a potency 350-fold greater than CT (ED50 values are 0.2 and 71 nM respectively). Displays no activity at calcitonin-gene related peptide (CGRP) and adrenomedullin recept | |||
T38005 |
P11149
|
||
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer’s disease[1]. P11149 is a GAL analog that is rapidly hydrolyzed in vivo to yield the potent AChE inhibitor, 6-DMG[1].P11149 exhibits greater s.c. bioavailability than p.o. [1].Oral P11149 in mice pr... | |||
T74863 | Anthramycin | ||
Anthramycin, 一种属于苯并二氮杂卓(PBD)家族的有效抗生素(antibiotic),展现出显著的抗肿瘤(antitumor)活性。在小鼠中枢神经系统中,它也能作为胆收缩素(cholecystokinin)的有效拮抗剂。 | |||
T79297 | DZD1516 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
DZD1516为一选择性HER2抑制剂,IC50值为0.56 nM,且血脑屏障透过性佳。于中枢神经系统内及皮下异种移植的小鼠模型中,显示显著的抗肿瘤效果。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S0627 |
Mesaconitine
新乌碱,新乌头碱;中乌头碱 |
TNF | Apoptosis |
Mesaconitine 是乌头属植物的一种主要活性成分,通过循环 AMP 和刺激中枢 β-肾上腺素能系统具有镇痛活性,还有抗炎活性。 | |||
TN2322 |
Yangambin
|
Calcium Channel; PAFR | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
Yangambin 是从诸如番荔枝科植物中分离出来的呋喃木脂素,是选择性PAF 受体拮抗剂,通过调控Ca2+通道抑制 Ca2+流入,导致 [Ca2+]i 在血管平滑肌细胞和随后的外周血管舒张中减少,具有降压作用。 | |||
TN1516 |
Cnidicin
蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮 |
NOS; NO Synthase | Immunology/Inflammation |
Cnidicin 是一种香豆素,对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。 | |||
T6S1049 |
Wilforine
|
ATPase | Membrane transporter/Ion channel |
Wilforine 是一倍半萜吡啶化合物,T. wilfordii 植物中的重要生物活性化合物,可有效治疗特发性肺纤维化。它具有抗炎和杀虫活性。 | |||
T6S0721 |
Orientin
荭草苷,Lutexin,Luteolin-8-glucoside |
Others | Others |
Orientin (Luteolin-8-glucoside) 是天然存在的生物活性类黄酮,是一种有前景的神经保护剂,具有多种生物特性,如抗炎、抗肿瘤、抗氧化、保护心脏等。它有用于神经性疼痛研究潜力。 | |||
TMA0805 |
Lupanine
|
ATPase; Potassium Channel; Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Lupanine has a weak sedative effect on the central nervous system, interaction with specific drugs used for treatment of the CNS and for analgesic activity. Lupanine improves glucose homeostasis by influencing KATP-channels of pancreatic beta cells. | |||
TN4776 | Physalin D | TNF; Antifection | Apoptosis; Microbiology/Virology |
Physalin D shows antimalarial activity; it also exhibits a minimum inhibitory concentration value (MIC) against Mycobacterium tuberculosis H(37)Rv strain of 32 microg/mL. Physalin D displays considerable cytotoxicity against several cancer cell lines. It | |||
TN2766 |
2'-Hydroxydaidzein
|
Cannabinoid Receptor; Antioxidant | GPCR/G Protein; oxidation-reduction |
2'-Hydroxydaidzein 是一种在植物中发现的异黄酮类植物素,是一种天然化合物。2'-Hydroxydaidzein 具有抗氧化活性,主要由o -氢键解离焓(BDE)和氢原子转移(HAT)机制驱动。2'-Hydroxydaidzein 抑制炎症细胞中的化学介质,可能对治疗和预防与化学介质产生过多有关的中枢和外周炎症性疾病有作用。2'-Hydroxydaidzein 对大鼠中性粒细胞和formyl-Met-Leu-Phe/cytochalasin B(fMLP/CB)的释放具有抑制作用,IC(50)值分别为2.8+/-0.1和5.9+/-1.4 microM。 |