89
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6393 |
ARQ 621
|
Kinesin | Cytoskeletal Signaling |
ARQ 621 是一种变构和选择性 Eg5 有丝分裂运动蛋白抑制剂,具有抗肿瘤活性。 | |||
T11689 |
ITI-214
ITI214 |
PDE | Metabolism |
ITI-214 是一种中枢神经系统活性抑制剂,具有口服生物活性的PDE1抑制剂 (Kiof 58 pM),对其他 PDE 家族成员和一系列酶、受体、转运体和离子通道具有良好的选择性,在各种运动和认知功能的动物模型中显示出有效性。 | |||
T22103 |
ML-193
CID 1261822 |
Cannabinoid Receptor | GPCR/G Protein |
ML-193 (CID 1261822) 是一种有效的选择性GPR55拮抗剂,IC50值为 221 nM,对 GPR55 的选择性比 GPR35、CB1 和 CB2 高 27 倍以上,可改善帕金森病 (PD) 大鼠的运动和感觉运动缺陷。 | |||
T13554 |
Arimoclomol maleate
BRX-220 |
HSP | Cytoskeletal Signaling; Metabolism |
Arimoclomol maleate (BRX-220) 是一种热休克蛋白 (HSP) 的共诱导剂。它通过增强 Hsp 表达来保护运动神经元,进而通过蛋白酶体-泛素系统直接影响蛋白质聚集和错误折叠装配体的清除 | |||
T1030 |
Triprolidine hydrochloride monohydrate
盐酸曲普利啶,盐酸曲普利啶一水合物,Triprolidine hydrochloride |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Triprolidine hydrochloride monohydrate 是一种组胺 H1 拮抗剂,用于过敏性鼻炎、哮喘。 | |||
T4641 |
Branaplam
LMI 070,NVS-SM1 |
Others; Potassium Channel; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Others |
Branaplam (LMI 070) 是一种高效、选择性和口服活性的小分子 SMN2 剪接调节剂,对 SMN 的 EC50为 20 nM。它可提高全长 SMN 蛋白并延长其生存期,也抑制 hERG,IC50为 6.3 μM。 | |||
T13553 |
Arimoclomol
阿瑞洛莫,BRX-220 free base |
HSP | Cytoskeletal Signaling; Metabolism |
Arimoclomol (BRX-220 free base) 是热休克蛋白 (HSP) 的共诱导剂,可用于治疗肌萎缩侧索硬化症的研究。 | |||
T24047 |
Etilevodopa hydrochloride
Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester |
Others; Dopamine Receptor; Drug Metabolite | GPCR/G Protein; Metabolism; Neuroscience; Others |
Etilevodopa hydrochloride (L-DOPA ethyl ester) 是 Levodopa 的前药,在胃肠道中被非特异性酯酶快速水解产生 Levodopa 和乙醇。Levodopa 是多巴胺的前体,有助于中枢神经系统的渗透和传递多巴胺。Etilevodopa HCl 可用于帕金森病 (PD)的相关研究。 | |||
T3336 |
Rg3039
PF-06687859 |
Others | Others |
Rg3039 (PF-06687859) 是一种具有口服活性、能够透过血脑屏障的DcpS 抑制剂,其IC50=0.069 nM。 | |||
T27084 |
Crisdesalazine
AAD2004,AAD 2004,AAD-2004 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Crisdesalazine (AAD 2004) 是微粒体前列腺素 E2 合酶 1 (mPGES-1) 的抑制剂。 Crisdesalazine 可减少自噬体形成、轴索病变和运动神经元变性,改善运动功能并延长寿命。 | |||
T6209 |
CW-069
CW069 |
Kinesin; Microtubule Associated | Cytoskeletal Signaling |
CW-069 是一种微管运动蛋白 HSET 的变构选择性抑制剂,IC50值为 75 μM,对 KSP 具有显着的特异性。 | |||
T16757 |
Risdiplam
RO7034067,RG7916 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Risdiplam (RO7034067) 是一种中枢和外周分布的 SMN2 前 mRNA 剪接修饰剂,可增加运动神经元存活 (SMN) 蛋白水平。 | |||
T8631 |
pyridostigmine
Regonol,Mestinon-SR,UNII-19QM69HH21,PyridostigmineBromine,Pyridostigminum |
Others | Others |
Pyridostigmine(Regonol) 是一种乙酰胆碱酯酶抑制剂,可通过增加突触后运动终板的乙酰胆碱来治疗重症肌无力。 | |||
T4029 |
BTB-1
BTB 1,NSC156750 |
Microtubule Associated | Cytoskeletal Signaling |
BTB-1 (NSC156750) 是一种新型的有丝分裂运动蛋白 Kif18A 的小分子抑制剂,IC50值为1.69 μM。 | |||
T3525 |
PD150606
|
Cysteine Protease | Proteases/Proteasome |
PD150606 是一种具有选择性的非肽 calpain 抑制剂,具有神经保护活性,抑制 μ-calpains 和 m-calpains ,抑制红藻氨酸诱导的 Ca2+ 内流,干扰兴奋性毒性依赖性运动神经元死亡。 | |||
T2039 |
GSK-923295
|
Apoptosis; Kinesin | Apoptosis; Cytoskeletal Signaling |
GSK923295 是一种特异性的变构着丝粒相关蛋白-E 驱动蛋白 ATPase 活性抑制剂,作用于人类和犬类此酶,Ki 分别为 3.2±0.2 nM 和 1.6±0.1 nM。 | |||
T23331 |
SC 51089
SC 51089 free base |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
SC 51089 是一种选择性的前列腺素受体 PGE2 拮抗剂,对前列腺素受体亚型具有选择性,具有抗伤害活性,可改善亨廷顿病 R6/1 小鼠模型中的运动缺陷并挽救记忆力下降。 | |||
T34399 |
Rovatirelin
KPS-0373,S0373,S-0373,S 0373 |
AChE | Neuroscience |
Rovatirelin (S-0373) 是一种新合成的促甲状腺激素释放激素(TRH)类似物,通过乙酰胆碱和多巴胺神经传递改善胞嘧啶阿拉伯糖苷诱导的脊髓小脑变性大鼠模型的运动功能障碍。 | |||
TP1852L |
Myomodulin acetate(110570-93-9 free base)
|
Potassium Channel; Calcium Channel; Sodium Channel | Membrane transporter/Ion channel; Metabolism |
Myomodulin acetate(110570-93-9 free base) 存在于两个已识别的海兔神经元中,它们包含肌调节蛋白 A、ARC 运动神经元 B16 和腹部神经元 L10。 | |||
T77586 | Eg5-IN-1 | Kinesin | Cytoskeletal Signaling |
Eg5-IN-1 是一种有效的驱动蛋白家族运动蛋白 (Eg5) 抑制剂,对 Eg5 的 IC50 值为 1.97 µM。Eg5-IN-1 可用于研究癌症。 | |||
T10659 |
Ca2+ channel agonist 1
|
Calcium Channel; CDK | Cell Cycle/Checkpoint; Membrane transporter/Ion channel; Metabolism |
Ca2+channel agonist 1 是 N-型钙离子通道激动剂和Cdk2的抑制剂,EC50分别为 14.23 μM 和 3.34 μM,可用作运动神经末梢功能障碍的潜在治疗方法。 | |||
T7352 |
Pridopidine
ACR16,ASP2314,FR310826,4-[3-(甲磺酰基)苯基]-1-丙基哌啶 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Pridopidine (FR310826) 是多巴胺稳定剂,是一种低亲和力的多巴胺 D2 受体拮抗剂。它高亲和力作用于 sigma 1受体,Ki=70-80 nM,比其对 D2R 的亲和力高约 100 倍。 | |||
T8741 |
MitoBloCK-10
3-fluoro-N'-[(E)-(5-nitrothiophen-2-yl)m |
Others | Others |
MitoBloCK-10 (3-fluoro-N'-[(E)-(5-nitrothiophen-2-yl)m) 是第一个能够减弱PAM 复合体活性的小分子调节剂,对 C 末端结构域的Tim44与前体和 Hsp70 结合具有抑制作用。 | |||
T14965 |
Ciliobrevin D
|
ATPase; Hedgehog/Smoothened | GPCR/G Protein; Membrane transporter/Ion channel; Stem Cells |
Ciliobrevin D 是细胞渗透性,可逆和特异性的 AAA + ATPase 运动细胞质动力蛋白抑制剂。它在体外抑制依赖于动力蛋白的微管滑动和 ATPase 活性。它抑制Hedgehog 信号和初级纤毛形成。 | |||
TP2047L |
CRF (6-33) acetate(120066-38-8 free base)
|
CRFR | GPCR/G Protein |
CRF (6-33) acetate(120066-38-8 free base) 是促肾上腺皮质激素释放因子结合蛋白 (CRFBP) 抑制肽;从 CRFBP 中替换 CRF。在体内抑制肥胖大鼠的体重增加并增加运动活动。 | |||
T16398 |
Opicapone
BIA 9-1067 |
Transferase | Metabolism |
Opicapone (BIA 9-1067) 是第三代儿茶酚-O-甲基转移酶 (COMT)抑制剂,能够降低细胞 ATP 含量,IC50=98 μM。它有用于帕金森病和运动波动的研究潜力。 | |||
T13248 |
UK-240455
|
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
UK-240455是一种有效的且具有选择性的 N-甲基 D-天冬氨酸 (NMDA) 甘氨酸受体拮抗剂,具有神经保护作用和改善帕金森病模型的运动的功能,是治疗帕金森病的潜在候选化合物。 | |||
T0166 |
Pancuronium dibromide
Pancuronium bromide,Pavulon,泮库溴铵 |
AChR | Neuroscience |
Pancuronium dibromide (Pavulon) 是一种双季基类固醇,是一种神经肌肉松弛剂。它通过与乙酰胆碱竞争 nACh 受体上的结合位点来抑制神经肌肉传递。它还可抑制心脏毒蕈碱受体并具有拟交感神经作用。 | |||
T24754 |
Hh-Ag1.5
SAG-1.5,SAG1.5,SAG 1.5 |
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
Hh-Ag1.5 (SAG-1.5) 是一种高效的 Hedgehog (Hh) 激动剂(EC50: 1 nM)和Smoothened (Smo)受体激动剂,对Smo的 EC50 为 1 nM、 Ki值在 0.5 和 2.3 nM 之间。Hh-Ag1.5 介导的重编程打破了非损伤肝脏干细胞的静止状态,从而挽救了肝衰竭。Hh-Ag1.5 诱导 hiPSCs 分化为皮肤前体细胞、脊髓运动神经元和脊髓感觉神经元。 | |||
TP1325L |
Gastrin-Releasing Peptide, human(TFA)
|
Others | Others |
Gastrin-Releasing Peptide, human(TFA) (93755-85-2 free base) 是一种调节性人类肽,可引发胃泌素释放并调节胃酸分泌和肠道运动功能。支配胃G 细胞的迷走神经节后纤维释放GRP,刺激G 细胞释放胃泌素。 | |||
T2546 |
Pimozide
R6238,匹莫奇特,匹莫齐特 |
Potassium Channel; Dopamine Receptor; Adrenergic Receptor; STAT | GPCR/G Protein; JAK/STAT signaling; Membrane transporter/Ion channel; Neuroscience; Stem Cells |
Pimozide (R6238) 是多巴胺受体拮抗剂,对多巴胺 D1、D2 和 D3 受体的 Ki 值分别为 588、1.4 和 2.5 nM。它也是STAT3和STAT5的抑制剂,对 α1 肾上腺素受体也有较高亲和性,Ki 值为 39 nM。 | |||
T67729 |
UCM-1306
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
UCM-1306 是具有口服活性的人多巴胺 D1 受体变构调节剂 (PAM)。UCM-1306 增加结合在人和小鼠 D1 受体的内源性多巴胺 (DA) 效应。UCM-1306可以改善运动症状,解决与长期帕金森病(PD) 相关的关键共病认知障碍。 | |||
T0939 |
Phenytoin
苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin |
Virus Protease; Sodium Channel | Membrane transporter/Ion channel; Microbiology/Virology |
Phenytoin (5,5-Diphenylhydantoin) 是一种有效的电压门控钠离子通道阻滞剂,可减少小鼠乳腺肿瘤的生长和转移,具有抗癫痫活性。 | |||
T37816 |
SB 243213
|
||
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1]. SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows... | |||
T28866 |
Stemazole
|
Apoptosis | Apoptosis |
Stemazole 是一种新型小分子人类干/祖细胞增殖激活剂 ,可促进人类胚胎干细胞的存活并保持干性 ,促进少突胶质细胞前体细胞在体外的存活。Stemazole 能显著提高细胞存活率和克隆形成数,并呈剂量依赖性,降低细胞凋亡率,促进运动功能障碍的恢复和髓鞘的修复。Stemazole 可作为脱髓鞘疾病的治疗剂,促进OPC 体外存活和体内再生。 | |||
T35689 |
MTP 131 acetate
|
Others | Others |
MTP 131 acetate 是一种小的线粒体靶向四肽。 | |||
T30167 |
ASP-5854
UNII-BJS8Y4IC5V,ASP 5854,C524699 |
||
ASP-5854 is an adenosine A(2A) receptor antagonist with the potential to improve motor deficits in Parkinson's disease. | |||
T71828 |
Syntelin
|
||
Syntelin is a selectively CENP-E inhibitor. Syntelin inhibited CENP-E motility in a dose-dependent manner with an IC50 value of 160 nM. Among an extensive list of mitotic kinesins examined, syntelin was found to be highly selective for CENP-E. Syntelin binds to different sites from those of GSK923295, a recently identified CENP-E ATPase inhibitor, as syntelin inhibits CENP-E mutants resistant to GSK923295 in a manner indistinguishable from that of wild type motor. Syntelin represents a novel cla... | |||
T21466 |
MK-212
MK 212,MK212 |
||
MK-212 is a 5HT2C-receptor agonist. Intraperitoneal injection of MK-212 in 0.5 and 1.0 mg/kg increased the blood level of corticosterone in mice and reduced their motor activity. In 0.1 and 0.2 mg/kg, the agonist reduced anxiety with no effect on motor ac | |||
T38828 |
Mesdopetam
IRL790 |
||
Mesdopetam (IRL790) is a dopamine D3 receptor antagonist with a Ki of 90 nM and an IC50 of 9.8 μM for the human recombinant D3 receptor. It exhibits psychomotor stabilizing properties and is utilized in the study of motor and psychiatric complications associated with Parkinson's disease. | |||
T63612 | ATX inhibitor 8 | ||
ATX inhibitor 8 是自分泌运动因子 Autotaxin (ATX) 抑制剂。 | |||
T34664 |
SMN2-Stablizer-27
SMN2-Stablizer 27,SMN2 Stablizer-27 |
||
SMN2-Stablizer-27 is a stablizer of survival of motor neuron 2 (SMN2), and a post-translationally stablizing SMN protein for the treatment of spinal muscular atrophy (SMA). | |||
T68881 |
OL-135
|
||
OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism. | |||
T21393 |
Ethopropazine Hydrochloride
Lysivane,Parphezein,Dibutil,Parfezin,Profenamine HCl,Pardisol |
||
Ethoproprazine hydrochloride is an butyrylcholinesterase inhibitor. It reduces extrapyramidal motor effects and used as an antidyskinetic, characteristic of Parkinson′s disease. It also alleviates thermal hyperalgesia in rats. | |||
T28680 |
SB-215505
|
||
SB215505 is a potent 5-HT2B/2C receptor antagonist (pKi values are 8.3, 7.66 and 6.77 for 5-HT2B, 5-HT2C and 5-HT2A respectively). It Increases wakefulness and motor activity in rats. | |||
TP2047 |
CRF(6-33)(human)
CRF (6-33) |
||
CRF(6-33)(human) is a Corticotropin-releasing factor binding protein (CRFBP) inhibitor peptide; displaces CRF from CRFBP. Suppresses body weight gain and increases motor activity in obese rats in vivo. | |||
T30576 |
Brasofensine
BMS-204756,CID9554198,BMS204756,UNII-1YP2S94RVH,BMS 204756 |
||
Brasofensine is a monoamine reuptake blocker, which is a benztoalkane. In animal models of Parkinson's disease, Brasofensine is effective in stimulating LMA and reversing motor inactivity. Brasofensine is being developed to treat Parkinson's disease and A | |||
T35594 |
Cuspin-1
|
||
The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Ra... | |||
T69152 | Bromopride hydrochloride | ||
Bromopride hydrochloride is the salt form of Bromopride, a dopamine D2 receptor blocker. Bromopride exerts is a gastrointestinal prokinetic exploited clinically for the management of motor disorders of the upper gastrointestinal tract, including functional dyspepsia, gastric stasis of various origins and emesis. | |||
T12859 |
SB 243213 hydrochloride
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8).It has improved anxiolytic profile and has the potential for schizophrenia and motor disorders. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T20754 |
Deltamethrin
Butoss,RU-22974,Esbecythrin,溴氰菊酯,K-Othrin,Decamethrin,RU 22974 |
Others | Others |
Deltamethrin (RU 22974) 是一种具有神经毒性的拟除虫菊酯杀虫剂,在大鼠中能够产生一系列可逆的运动症状(如包括后肢僵硬、舞蹈性关节炎)。 | |||
TN1913 |
Marmin
|
Calcium Channel; Antifection; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
Marmin have anti-ulcer effects, which are ascribed primarily to the maintenance of the mucosal barrier integrity and inhibition of gastric motor activity and secondarily due to the prevention of the effects of endogenous acetylcholine and histamine. | |||
TN4519 |
Mesuaxanthone A
胡桐,海棠木 |
Others | Others |
Mesuaxanthone A and mesuaxanthone B are two yellow pigments.They produce varying degrees of C.N.S. depression characterised by ptosis, sedation, decreased spontaneous motor activity, loss of muscle tone, potentiation of pentobarbitone sleeping time and et | |||
T13123 |
Tentoxin
|
Endogenous Metabolite | Metabolism |
Tentoxin 是一种由植物致病真菌产生的环状肽,在敏感植物中,当其浓度在纳摩尔到微摩尔之间时,会使 F1马达失活,而更高的浓度会超过该酶的天然活性 | |||
T75576 | Solidagonic acid | ||
Solidagonic acid 通过促进异常单极纺锤体向双极纺锤体的转变来抑制 HSET 运动活动。Solidagonic acid 抑制裂殖酵母细胞死亡,并使有丝分裂纺锤体从单极形态逆转为双极形态。Solidagonic acid 对 Lactuca sativaL. 和 Lolium multiflorumLam 的幼苗具有生长抑制活性。 |