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Search Results for " brain-permeable "

Targets Recommended: AChR

63

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12165	nAChR agonist 1 DUN71755	AChR	Neuroscience
	nAChR agonist 1 (DUN71755) 是一种脑渗透性和口服有效的正变构 α7 烟碱乙酰胆碱受体 (α7 nAChR) 调节剂。它在 Ca2+中，对内源性表达 α7 nAChR 的人 IMR-32 神经母细胞瘤细胞的EC50为 0.32 μM。它可用于阿尔茨海默病的研究。
T9956	VK-28	Mitochondrial Metabolism; Lipid	Metabolism
	VK-28 是一种具有神经保护作用的脑渗透性铁螯合剂。 VK-28 抑制基础以及铁诱导的线粒体脂质过氧化。
T14389	AZD 9272	GluR	Neuroscience
	AZD 9272 是一种脑渗透性的mGluR5 拮抗剂，可用于研究胃食管反流。
T27678	JNJ-39220675 JNJ 39220675,JNJ39220675	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	JNJ-39220675 (JNJ 39220675) 是一种具有选择性和脑渗透性的组胺 H3 受体拮抗剂。
T1741	AZD1080	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	AZD1080 是一种选择性GSK3抑制剂。它抑制重组人GSK3α和GSK3β，pKi(IC50) 分别为 8.2 (6.9 nM) 和 7.5 (31 nM)。
T6679	SRT 2104 SRT2104,sirtuin modulator,GSK2245840	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SRT 2104 (GSK2245840) 是一种高度选择性、可通过血脑屏障的 Sirt1激活剂，依赖于 NAD+，增加 Sirt1 蛋白水平，用于糖尿病和亨廷顿氏症的研究。
T22972	Methoxy-X04	Others	Others
	Methoxy-X04, a derivative of Congo red and Chrysamine-G, is a brain-permeable fluorescent probe for amyloid-β (Aβ).
TQ0075	ML314	Neurotensin Receptor	GPCR/G Protein
	ML314 是一种具有脑渗透性非肽 β-抑制素偏向神经降压素 NTR1 受体激动剂（EC50：1.9 μM），是一种用于甲基苯丙胺滥用的偏向神经降压素受体配体，抑制 NTR2 和 GPR35。
T5490	AK-7	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	AK-7 是一种大脑可渗透的 SIRT2 抑制剂，可在神经元模型中表征其降低胆固醇的特性，IC50 为 15.5 μM。
TQ0238	Lanabecestat LY3314814,AZD3293	BACE	Neuroscience
	Lanabecestat (AZD3293) 是一种具有高效性和高渗透性、口服活性且可穿过血脑屏障的 BACE1 抑制剂（Ki：0.4 nM），Lanabecestat 可用于研究像阿尔茨海默症类的神经系统疾病。
TQ0026	MDR-1339 DWK-1339	Beta Amyloid; Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	MDR-1339 是口服有效Aβ聚集抑制剂，可透过血脑屏障的。MDR-1339可用于阿尔兹海默症的研究。
T84285	MM0299	Others	Others
	MM0299 具有脑渗透性，具有抗胶质母细胞瘤活性，抑制羊毛甾醇合酶（LSS），诱导原位GBM肿瘤中EPC的产生。
T40051	Acid Ceramidase-IN-1	Others	Others
	Acid Ceramidase-IN-1 是一种可口服且具有良好的脑渗透性的酸性神经酰胺酶 (AC, ASAH-1) 抑制剂。Acid Ceramidase-IN-1 可用于研究神经系统疾病。
T38789	BMS-984923 BMS984923,BMS 984923	Beta Amyloid; GluR	Neuroscience
	BMS-984923 是可口服且具有血脑屏障透过性的 mGluR5 沉默异构调节剂，抑制β-淀粉样蛋白寡聚体诱导的异常突触信号传导，可用于研究阿尔茨海默症。
T10355	Apyramide	COX	Immunology/Inflammation; Neuroscience
	Apyramide 是一种抗炎试剂 (NSAID)，是吲哚美辛的前药。Indomethacin 是一种强效的、血脑通透的、非选择性的 COX1 和 COX2 抑制剂。
T41143	pCPA methyl ester hydrochloride 4-氯-DL-苯基丙氨酸甲酯盐酸盐,4-Chloro-DL-phenylalanine methyl ester hydrochloride	5-HT Receptor; Hydroxylase	GPCR/G Protein; Metabolism; Neuroscience
	pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) 是色氨酸羟化酶抑制剂和5-HT 合成的抑制剂。 pCPA methyl ester hydrochloride 可穿过血脑屏障并降低 5-HT 中枢可用性。
T5468	YF-2	Others; Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic; Others
	YF-2 是一种高选择性，可透过血脑屏障的组蛋白乙酰转移酶激动剂，能够在海马区乙酰化 H3，对 CBP、PCAF 和 GCN5 的EC50值分别为 2.75、29.04 和 49.31 μM，具有抗肿瘤和抗阿尔滋海默症的活性。
T37577	Glycogen Phosphorylase Inhibitor	Others	Others
	Glycogen phosphorylase in the liver, muscle, and brain initiate glycogenolysis by releasing glucose-1-phosphate from glycogen. Glycogen phosphorylase inhibitor is a cell-permeable acyl urea first identified as an inhibitor of human liver glycogen phosphorylase (IC50 = 53 nM). It blocks glucagon-induced hepatic glycogenolysis in vivo. Glycogen phosphorylase inhibitor has been used to study glycogen utilization in human liver HepG2 cells, retinal explants, and human T lymphocyte Kit 225 cells.
T14338	Atabecestat RSC-385896,JNJ-54861911	BACE	Neuroscience
	Atabecestat (JNJ-54861911) 是一种具有口服活性和脑渗透性的 β-位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂，减缓临床前阿尔茨海默病参与者的认知能力下降。Atabecestat 可用于研究阿尔茨海默氏病。
T13298	Verubulin hydrochloride MPC-6827 hydrochloride,N-(4-甲氧基苯基)-N,2-二甲基-4-喹唑啉胺盐酸盐	Microtubule Associated	Cytoskeletal Signaling
	Verubulin hydrochloride (MPC-6827 hydrochloride) 是一种血脑屏障渗透性微管破坏剂，具有强效和广谱的细胞毒活性，在人 MX-1 乳腺癌和其他小鼠异种移植癌模型中具有有效的抗癌活性。
T33514	MSC 2032964A MSC-2032964A,MSC2032964A	ASK	Apoptosis
	MSC 2032964A 是一种有效的选择性 ASK1 抑制剂 (IC50 = 93 nM)，具有口服生物利用度和脑渗透性。它在小鼠 EAE 模型中抑制神经炎症，并在培养的小鼠星形胶质细胞中阻断 LPS 诱导的 ASK1 和 p38 磷酸化。
T73177	hCAII-IN-9	Carbonic Anhydrase	Metabolism
	hCAII-IN-9 是一种强效的碳酸酐酶抑制剂，对hCA II、hCA IX 和hCA XII 有抑制作用，IC50 分别为 1.18 μM 和 0.17 μM , and 2.99 μM 。hCAII-IN-9 没有血脑屏障透过性。
T8702	SKF-83566	Dopamine Receptor; 5-HT Receptor; AChR	GPCR/G Protein; Neuroscience
	SKF-83566 是一种具有血脑渗透性和口服活性的 D1 样多巴胺受体拮抗剂和一种较弱的竞争性 5-HT2 受体拮抗剂，Ki 为 11 nM。它是竞争性多巴胺转运蛋白抑制剂，可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。
T4494	CLOZAPINE N-OXIDE 氯氮平N-氧化,氯氮平N-氧化物	Dopamine Receptor; 5-HT Receptor; AChR; Drug Metabolite	GPCR/G Protein; Metabolism; Neuroscience
	Clozapine N-oxide 是 Clozapine 的主要代谢产物，具有血脑屏障渗透性。Clozapine N-oxide 是一种 DREADDs 激动剂，可激活 DREADD 受体 hM3Dq 和 hM4Di。Clozapine N-oxide 也是一种多巴胺拮抗剂和选择性毒蕈碱 M4 受体激动剂。
T72420	MTK458 Mitophagy activator 1,EP-0035985	PTEN	PI3K/Akt/mTOR signaling
	MTK458 (EP-0035985) 是一种具有口服活性和脑渗透性的 PINK1 激活剂，在PFF 接种模型中促进 α-突触核蛋白病理学的清除并降低 pUb。MTK458 通过刺激 PINK1/TOM 复合物的二聚化和稳定来诱导病理学的α-突触核蛋白清除。MTK458 可用于帕金森病的研究。
T4019	Cambinol SIRT1/2 Inhibitor IV,NSC 112546	Apoptosis; Phospholipase; Sirtuin	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism
	Cambinol (SIRT1/2 Inhibitor IV) 是一种SIRT1和SIRT2的抑制剂，IC50值分别为 56 μM 和 59 μM。它是中性鞘磷脂酶的外泌体抑制剂。
T77341	GSK-3 inhibitor 4	GSK-3; CDK	Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
	GSK-3 inhibitor 4 是一种具有口服活性和脑渗透性的 GSK-3，CDK2 和 CDK5 三重抑制剂，对 GSK-3β，GSK-3α，CDK2 和 CDK5 具有抑制作用，IC50 值分别为 0.56 nM ，0.45 nM ，0.47 μM，0.68 μM。GSK-3 inhibitor 4 可有效降低 Tau protein 水平。GSK-3 inhibitor 4 可用于研究阿尔茨海默症。
T77342	GSK-3 inhibitor 3	GSK-3; Microtubule Associated	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells
	GSK-3 inhibitor 3 是一种具有选择性、具有口服活性和脑渗透性的 GSK-3 抑制剂，对 GSK-3α 和 GSK-3β 具有抑制作用， IC50s 分别为 0.35 nM 和 0.25 nM。GSK-3 inhibitor 3 在三重转基因小鼠阿尔茨海默病模型中降低 Tau 蛋白 (tau protein) S396 磷酸化水平，IC50为 10 nM。GSK-3 inhibitor 3 可用于研究神经系统疾病。
T13001	SRT3657	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SRT3657 is a brain-permeable SIRT1 activator, has neuroprotective effect.
T15407	GNE-0723	Others	Others
	GNE 0723 is an NMDAR brain permeable positive allosteric modulator (EC50: 21 nM for GluN2A; 7.4 and 6.2 μM for GluN2C and GluN2D, respectively).
T15408	GNE 5729	Others	Others
	GNE 5729 is an NMDAR of brain permeable positive allosteric modulator (EC50: 37 nM for GluN2A; 4.7 and 9.5 μM for GluN2C and GluN2D, respectively).
T10688	Casopitant mesylate GW679769B	P450; Neurokinin receptor	GPCR/G Protein; Metabolism; Neuroscience
	Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.
T14334	ASP2535	GlyT	Neuroscience
	ASP2535 is a potent, selective, orally bioavailable, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor.ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease[1].
T85023	TG11-77 hydrochloride	Others	Others
	TG11-77 hydrochloride is a potent, selective, and water-soluble EP2 receptor antagonist that is brain-permeable, demonstrating a KB value of 9.7 nM.
T41159	NCT 501 hydrochloride	Others	Others
	NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Blood-brain barrier permeable.
T70807	Lanabecestat HCl	Others	Others
	Lanabecestat, also known as AZD3293 and LY3314814, is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. AZD3293 displayed significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ.
T61644	α-Synuclein inhibitor 6	Others	Others
	α-Synuclein inhibitor 6 (compound 3ge) is a highly effective and blood-brain barrier-permeable inhibitor that targets the aggregation of α-Synuclein (α-Syn). It exhibits a potent inhibitory activity, with an IC50 value of 1.70 μM, leading to a remarkable inhibition ratio of 94.4% at 30 μM [1].
T69608	TG11-77 HCl	Others	Others
	TG11-77 HCl is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 HCl has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 HCl are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.
T11185	EML741	Histone Methyltransferase	Chromatin/Epigenetic
	EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.
T40046	UGT8-IN-1 UGT8-IN-1	Others	Others
	UGT8-IN-1 is a brain-permeable and orally-active inhibitor that specifically targets the ceramide galactosyltransferase enzyme (UGT8). By inhibiting UGT8, this compound has the potential to be employed in research pertaining to lysosomal storage disorders.
T62142	COX-2-IN-17	Others	Others
	COX-2-IN-17 是一种有效的、具有血脑屏障通透性的 COX-2(环氧化酶 -2) 抑制剂 (IC50: 0.02 μM)，具有抗炎和镇痛活性。
T69609	TG11-77 free base	Others	Others
	TG11-77 free base is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 free base has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 free base are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.
T79253	HAT-IN-8	Parasite	Microbiology/Virology
	HAT-IN-8（Compound 38）是一款能穿透血脑屏障的T. brucei抑制剂（EC50：0.18 μM），适用于研究人类非洲锥虫病。
T35563	PF-5274857 hydrochloride	Others	Others
	PF-5274857 hydrochloride 是有效的、具有口服活性的、选择性的、可透过血脑屏障的 Smo 拮抗剂，其 IC50=5.8 nM，Ki=4.6 nM。它有用于包括激活的 Hh 途径驱动的脑肿瘤和脑转移在内的多种肿瘤的研究潜力。
T61611	α-Synuclein inhibitor 4	Others	Others
	α-Synuclein inhibitor 4 (compound 3gh) is a highly effective and blood-brain barrier-permeable inhibitor of α-Synuclein aggregation. It displays potent activity, with an IC50 value of 0.98 μM, and exhibits a remarkable inhibition ratio of 91.2% at a concentration of 30 μM [1].
T78969	PB131	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PB131为选择性HDAC6抑制剂，能穿透血脑屏障且显示出高结合亲和性（IC50: 1.8 nM）。该化合物展现出显著的抗炎活性，适用于炎症特别是神经炎症的研究领域。
T62202	mGluR2 modulator 1	Others	Others
	mGluR2 modulator 1 (compound 95) 是一种有效的、具有血脑屏障通透性的 mGluR2 (代谢型谷氨酸受体-2)正向变构调节剂 (EC50: 0.03 μM)。mGluR2 modulator 1 能够用于研究精神病。
T74781	UT-11	Others	Others
	UT-11是一种有效且具有脑渗透性的mPGES-1抑制剂，能够降低人类(SK-N-AS)和小鼠(BV2)细胞内PGE2的生成，其IC50s分别是0.10 μM和2.00 μM。
T62674	LSD1-IN-21	Others	Others
	LSD1-IN-21 是一种有效的、具有血脑屏障通透性的 LSD1 (赖氨酸特异性去甲基化酶-1) 抑制剂 (IC50: 0.956 μM)。LSD1-IN-21 能够明显减少促炎细胞因子 TNF-α，表现出良好的抗癌和抗炎效果。
T62898	Glucosylceramide synthase-IN-1	Others	Others
	Glucosylceramide synthase-IN-1 (T-036) 是一种有效的、口服具有活力的、具有血脑屏障通透性的 glucosylceramide synthase (GCS) 抑制剂，作用于人 GCS (IC50: 31 nM) 和小鼠 GCS (IC50: 51 nM)。Glucosylceramide synthase-IN-1 能够用于研究戈谢病。

化合物

nAChR agonist 1

Cat.No: T12165

Synonym: DUN71755

Target: AChR

Cat.No: T9956

Target: Mitochondrial Metabolism, Lipid

Cat.No: T14389

Target: GluR

Cat.No: T27678

Synonym: JNJ 39220675,JNJ39220675

Target: Histamine Receptor

Cat.No: T1741

Target: GSK-3

Cat.No: T6679

Synonym: SRT2104,sirtuin modulator,GSK2245840

Target: Sirtuin

Cat.No: T22972

Target: Others

Cat.No: TQ0075

Target: Neurotensin Receptor

Cat.No: T5490

Target: Sirtuin

Cat.No: TQ0238

Synonym: LY3314814,AZD3293

Target: BACE

Cat.No: TQ0026

Synonym: DWK-1339

Target: Beta Amyloid, Gamma-secretase

Cat.No: T84285

Target: Others

Acid Ceramidase-IN-1

Cat.No: T40051

Target: Others

Cat.No: T38789

Synonym: BMS984923,BMS 984923

Target: Beta Amyloid, GluR

Cat.No: T10355

Target: COX

pCPA methyl ester hydrochloride

Cat.No: T41143

Synonym: 4-氯-DL-苯基丙氨酸甲酯盐酸盐,4-Chloro-DL-phenylalanine methyl ester hydrochloride

Target: 5-HT Receptor, Hydroxylase

Cat.No: T5468

Target: Others, Epigenetic Reader Domain, Histone Acetyltransferase

Glycogen Phosphorylase Inhibitor

Cat.No: T37577

Target: Others

Cat.No: T14338

Synonym: RSC-385896,JNJ-54861911

Target: BACE

Verubulin hydrochloride

Cat.No: T13298

Synonym: MPC-6827 hydrochloride,N-(4-甲氧基苯基)-N,2-二甲基-4-喹唑啉胺盐酸盐

Target: Microtubule Associated

Cat.No: T33514

Synonym: MSC-2032964A,MSC2032964A

Target: ASK

Cat.No: T73177

Target: Carbonic Anhydrase

Cat.No: T8702

Target: Dopamine Receptor, 5-HT Receptor, AChR

CLOZAPINE N-OXIDE

Cat.No: T4494

Synonym: 氯氮平N-氧化,氯氮平N-氧化物

Target: Dopamine Receptor, 5-HT Receptor, AChR, Drug Metabolite

Cat.No: T72420

Synonym: Mitophagy activator 1,EP-0035985

Target: PTEN

Cat.No: T4019

Synonym: SIRT1/2 Inhibitor IV,NSC 112546

Target: Apoptosis, Phospholipase, Sirtuin

GSK-3 inhibitor 4

Cat.No: T77341

Target: GSK-3, CDK

GSK-3 inhibitor 3

Cat.No: T77342

Target: GSK-3, Microtubule Associated

Cat.No: T13001

Target: Sirtuin

Cat.No: T15407

Target: Others

Cat.No: T15408

Target: Others

Casopitant mesylate

Cat.No: T10688

Synonym: GW679769B

Target: P450, Neurokinin receptor

Cat.No: T14334

Target: GlyT

TG11-77 hydrochloride

Cat.No: T85023

Target: Others

NCT 501 hydrochloride

Cat.No: T41159

Target: Others

Lanabecestat HCl

Cat.No: T70807

Target: Others

α-Synuclein inhibitor 6

Cat.No: T61644

Target: Others

Cat.No: T69608

Target: Others

Cat.No: T11185

Target: Histone Methyltransferase

Cat.No: T40046

Synonym: UGT8-IN-1

Target: Others

Cat.No: T62142

Target: Others

TG11-77 free base

Cat.No: T69609

Target: Others

Cat.No: T79253

Target: Parasite

PF-5274857 hydrochloride

Cat.No: T35563

Target: Others

α-Synuclein inhibitor 4

Cat.No: T61611

Target: Others

Cat.No: T78969

Target: HDAC

mGluR2 modulator 1

Cat.No: T62202

Target: Others

Cat.No: T74781

Target: Others

Cat.No: T62674

Target: Others

Glucosylceramide synthase-IN-1

Cat.No: T62898

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T16012	Marizomib NPI-0052,Salinosporamide A,ML858	Proteasome	Proteases/Proteasome; Ubiquitination
	Marizomib (ML858) 是一种新型不可逆的脑渗透性泛蛋白酶体 (proteasome) 抑制剂，对 20S 蛋白酶体的 CT-L (β5)、CT-T-laspase 样 (C-L, β1) 和胰蛋白酶样 (T-L, β2) 具有抑制作用， IC50 分别为 3.5, 28, 430 nM。
T13493	3-Acetyldeoxynivalenol	Others	Others
	3-Acetyldeoxynivalenol is a trichothecene mycotoxin deoxynivalenol acetylated derivative and a blood-brain barrier (BBB) permeable mycotoxin.

天然产物

Cat.No: T16012

Synonym: NPI-0052,Salinosporamide A,ML858

Target: Proteasome

3-Acetyldeoxynivalenol

Cat.No: T13493

Target: Others

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