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Search Results for " mptp "

24

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4081	MPTP hydrochloride MPTP-hydrochloride	Apoptosis; Dopamine Receptor	Apoptosis; GPCR/G Protein; Neuroscience
	MPTP hydrochloride 是 MPP+ 的前体，是一种多巴胺神经毒素，具有血脑屏障渗透性。MPTP hydrochloride 对多巴胺能神经元有毒，可以导致帕金森症，被广泛应用于帕金森动物模型的构建。
T71195	mPTP-IN-22
	mPTP-IN-22 is a novel mitochondrial permeability transition pore (mptp) inhibitor
T71193	Jak2-IN-7j
	Jak2-IN-7j is a selective Jak2 inhibitor which demonstrates a time-dependent knock-down of pSTAT5, which is a downstream target of Jak2.
T4491	LMPTP INHIBITOR 1 hydrochloride LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base))	Phosphatase	Metabolism
	LMPTP INHIBITOR 1 hydrochloride 是一种高选择性的低分子量蛋白酪氨酸磷酸酶 (LMPTP) 抑制剂。LMPTP INHIBITOR 1 (hydrochloride) 能够抑制 LMPTP-A 的活性，IC50值为 0.8 μM。
T41298	LMPTP INHIBITOR 1 dihydrochloride	Phosphatase	Metabolism
	LMPTP INHIBITOR 1 dihydrochloride 是选择性的低分子量蛋白酪氨酸磷酸酶（LMPTP）抑制剂，抑制 LMPTP-A 活性的IC50为 0.8 μM。
T73120	MptpB-IN-1
	MptpB-IN-1 是一种有效的、具有口服活性的 MptpB 抑制剂。结核分枝杆菌蛋白-酪氨酸-磷酸酶 B (MptpB) 是一种分泌的毒力因子，可破坏宿主的抗菌活性。MptpB-IN-1 可降低耐多药结核分枝杆菌的存活率和感染负担。
T79479	MptpB-IN-2	Antibiotic	Microbiology/Virology
	MptpB-IN-2（化合物20）是一种高选择性的结核分枝杆菌蛋白酪氨酸磷酸酶B（MptpB）抑制剂，其对MptpB、MptpA和PTP1B的IC50值分别为0.64 μM、4.06 μM和4.14 μM。此化合物对Mtb H37Rv表现出较低的抗结核活性，MIC为64.9 μM。
T15241	ER-000444793	Others; Mitochondrial Metabolism	Metabolism; Others
	ER-000444793 是一种线粒体通透性转换孔开放抑制剂。它能够抑制 mPTP，IC50=2.8 μM。
T26686	AV-101 L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine	NMDAR	Neuroscience
	AV-101 (4-Cl-KYN) 是 NMDA 受体甘氨酸位点的前药拮抗剂，具有抗抑郁活性，可减少 MPTP 猴子中左旋多巴诱导的运动障碍。
T10404	ATP synthase inhibitor 1	ATPase	Membrane transporter/Ion channel
	ATP synthase inhibitor 1 是 F1/FO-ATP 合酶复合物 c 亚基的有效抑制剂，抑制线粒体通透性转换孔的开放。
T61268	Vutiglabridin HSG4112	Phosphatase	Metabolism
	Vutiglabridin (HSG4112) 是一种新型且安全的PON2调节剂，是一个外消旋化合物。Vutiglabridin 是Glabridin 的优化结构类似物，比Glabridin 在减重效果和化学稳定性方面更加优越。Vutiglabridin 通过靶向线粒体对氧磷酶-2改善mptp 诱导的帕金森病小鼠的神经变性。Vutiglabridin 是一种治疗肥胖的临床2期药物，在PD 模型中对对线粒体PON2具有治疗作用。Vutiglabridin 渗透到大脑，结合PON2，恢复1-甲基-4-苯基吡啶(MPP)诱导的SH-SY5Y 神经母细胞瘤细胞线粒体功能障碍。Vutiglabridin 在小鼠实验中显著减轻了1-甲基-4苯基-1,2,3,6-四氢吡啶(MPTP*)诱导的PD 模型小鼠的运动障碍和多巴胺能神经元损伤。
T38034	MAO-IN-M30 dihydrochloride M 30 dihydrochloride	Monoamine Oxidase	Neuroscience
	MAO-IN-M30 dihydrochloride (M 30 dihydrochloride) 是一种口服活性，可通过血脑屏障的，脑选择性不可逆 MAO-A (IC50=37 nM) 和 MAO-B (IC50=57 nM) 抑制剂。MAO-IN-M30 dihydrochloride 是有效的铁螯合剂、自由基清除剂。MAO-IN-M30 dihydrochloride 对 Dexamethasone 诱导的脑细胞凋亡具有神经保护作用。MAO-IN-M30 dihydrochloride 在 MPTP 和 lactacystin 帕金森病模型中也显示出神经恢复活性。
T9169	MPP+ iodide	Mitochondrial Metabolism; Autophagy	Autophagy; Metabolism
	MPP+ iodide 是一种 5-羟色胺转运体的高亲和力底物，也是一种神经毒素 MPTP 的有毒代谢物，通过选择性破坏黑质多巴胺能神经元，在动物模型中引起帕金森病症状。它被多巴胺转运体吸收进入多巴胺能神经元，通过影响呼吸链复合体 I 对线粒体发挥神经毒性作用。
T27959	LY503430 LY-503430,LY 503430
	LY503430 is a AMPA receptor potentiator with oral activity. LY503430 has both nootropic and neuroprotective effects, reducing brain damage caused by 6-hydroxydopamine or MPTP.
T24645	Piroheptine HCl Piroheptine Hydrochloride,Trimol
	Piroheptine HCl is an agent of anticholinergic that acts by inhibiting dopamine uptake and completely preventing loss of striatal dopamine in MPTP-treated mice.
T33450	ML 23 ML-23,ML23
	ML 23 is a melatonin analogue in the treatment and management of Parkinson's disease. ML-23 is a potential clinical candidate for the treatment of PD, and the present study has been undertaken to determine the efficacy of ML-23 in the 1-methyl-4-phenyl, 1
T38202	PAQ
	PAQ is a neuroprotective agent. It protects dopaminergic neurons from cell death without inhibiting glial cell proliferation in a rat midbrain culture model of Parkinson's disease when used at a concentration of 10 μM. PAQ (25 or 50 mg/kg, twice per day) prevents loss of dopaminergic neurons in the substantia nigra in a mouse model of Parkinson's disease induced by MPTP.
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
TP2019L	[D-Ala2]-GIP (human) acetate(444073-04-5 Free base)
	[D-Ala2]-GIP (human) acetate(444073-04-5 Free base) 是一种高效的 GIP 受体激动剂 (EC50 = 630 ± 119 pM)。在表达野生型 GIP 受体的细胞中，与天然 GIP 相比，[D-Ala2]-GIP (human) acetate 显示出同等的 cAMP 刺激特性，并提高了对酶促降解的抵抗力。 [D-Ala2]-GIP (human) acetate 可改善各种肥胖和糖尿病动物模型的葡萄糖耐量、胰岛素释放和认知功能。 [D-Ala2]-GIP (human) acetate 在 PD 的 MPTP 模型中显示出神经保护作用。
TP2019	[D-Ala2]-GIP (human)
	Highly potent GIP receptor agonist (EC50 = 630 ± 119 pM). Displays equivalent cAMP stimulating properties and improved resistance to enzymatic degradation compared to native GIP in cells expressing wild type GIP receptor. Improves glucose tolerance, insul
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...
T83726	Tat-βsyn-degron TFA
	Tat-βsyn-degron是一种降低α-synuclein表达的肽。其结构包括HIV-1 Tat质膜跨导域、与β-synuclein氨基酸36-45相对应的α-synuclein结合域βsyn，以及蛋白酶体定向域degron。在肽-蛋白结合实验中，Tat-βsyn-degron能够与重组α-synuclein结合，并在大鼠初级皮质神经元培养中降低α-synuclein水平，这一效应可以通过蛋白酶体抑制剂MG132阻止。体内研究显示，Tat-βsyn-degron (40 mg/kg)能够在过表达人类A53T突变体α-synuclein的M38转基因小鼠的大脑中降低α-synuclein水平，并且在黑质和脑桥中降低磷酸化α-synuclein水平，以及在通过α-synuclein预成纤维诱导的扩散性α-synuclein病理模型小鼠中减少神经炎症。此外，Tat-βsyn-degron (6 µmol/kg, i.p.)在MPTP诱导的帕金森病小鼠模型中，保护多巴胺能神经元，缓解运动缺陷。
T83894	4A7C-301-Nurr1 Agonist 4A7C-301-Nuclear Receptor-Related 1
	4A7C-301-Nurr1激动剂是一种核受体相关1（Nurr1）的激动剂。它通过与Nurr1配体结合域（LBD；IC50 = 48.22 nM）结合，增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性（EC50s = 6.53 和 50-70 µM，分别）。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡，并减少运动和嗅觉缺陷，而不诱发类似运动障碍的行为。
T37297	Ru360
	Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce...

化合物

MPTP hydrochloride

Cat.No: T4081

Synonym: MPTP-hydrochloride

Target: Apoptosis, Dopamine Receptor

Cat.No: T71195

Cat.No: T71193

LMPTP INHIBITOR 1 hydrochloride

Cat.No: T4491

Synonym: LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base))

Target: Phosphatase

LMPTP INHIBITOR 1 dihydrochloride

Cat.No: T41298

Target: Phosphatase

Cat.No: T73120

Cat.No: T79479

Target: Antibiotic

Cat.No: T15241

Target: Others, Mitochondrial Metabolism

Cat.No: T26686

Synonym: L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine

Target: NMDAR

ATP synthase inhibitor 1

Cat.No: T10404

Target: ATPase

Cat.No: T61268

Synonym: HSG4112

Target: Phosphatase

MAO-IN-M30 dihydrochloride

Cat.No: T38034

Synonym: M 30 dihydrochloride

Target: Monoamine Oxidase

Cat.No: T9169

Target: Mitochondrial Metabolism, Autophagy

Cat.No: T27959

Synonym: LY-503430,LY 503430

Piroheptine HCl

Cat.No: T24645

Synonym: Piroheptine Hydrochloride,Trimol

Cat.No: T33450

Synonym: ML-23,ML23

Cat.No: T38202

AMK (hydrochloride)

Cat.No: T36176

[D-Ala2]-GIP (human) acetate(444073-04-5 Free base)

Cat.No: TP2019L

[D-Ala2]-GIP (human)

Cat.No: TP2019

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Tat-βsyn-degron TFA

Cat.No: T83726

4A7C-301-Nurr1 Agonist

Cat.No: T83894

Synonym: 4A7C-301-Nuclear Receptor-Related 1

Cat.No: T37297

Cat. No.	Product Name	Target	Signaling Pathways
T4S2126	Ginkgetin 银杏双黄酮,银杏素	Apoptosis; Wnt/beta-catenin; COX; STAT; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; Stem Cells
	Ginkgetin 是从银杏叶中分离得到的一种双黄酮，具有抗肿瘤、抗炎、神经保护、抗真菌的作用。它也是 Wnt 信号抑制剂，IC50值为 5.92 μM。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。
T4954L	Smilagenin PYM50028,Cogane,AI3-44895,PYM 50028
	Smilagenin is an orally active inducer of nonpeptide neurotrophic factor. It also prevents and reverses neuronal damage induced by MPP+ in mesencephalic neurons, and by MPTP in a mouse model of Parkinson's disease.
TN2945	3-Hydroxybakuchiol	ATPase; Caspase	Apoptosis; Membrane transporter/Ion channel; Proteases/Proteasome
	3-Hydroxybakuchiol exerts cytotoxic and anti-proliferative effects on the TA3/Ha mouse mammary adenocarcinoma cell line and induces a decrease in the mitochondrial transmembrane potential, the activation of caspase-3, the opening of the mitochondrial perm

天然产物

Cat.No: T4S2126

Synonym: 银杏双黄酮,银杏素

Target: Apoptosis, Wnt/beta-catenin, COX, STAT, Autophagy

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

Cat.No: T4954L

Synonym: PYM50028,Cogane,AI3-44895,PYM 50028

3-Hydroxybakuchiol

Cat.No: TN2945

Target: ATPase, Caspase

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