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Search Results for " brain-permeable "

56

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。
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。
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。
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)。
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).
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。
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。
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。
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。
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。
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。
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。
T72420	MTK458 EP-0035985	PTEN	PI3K/Akt/mTOR signaling
	MTK458 (EP-0035985) 是一种具有脑渗透性和口服活性的 PINK1 激活剂。MTK458 通过刺激 PINK1/TOM 复合物的二聚化和稳定来选择性地激活 PINK1MTK458 驱动α-突触核蛋白病理学的清除，可用于研究帕金森病。
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。
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).
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].
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.
T41159	NCT 501 hydrochloride
	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
	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
	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].
T40046	UGT8-IN-1 UGT8-IN-1
	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.
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.
T69608	TG11-77 HCl
	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.
T62142	COX-2-IN-17
	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
	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.
T35563	PF-5274857 hydrochloride
	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。
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。
T61611	α-Synuclein inhibitor 4
	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
	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。
T37577	Glycogen Phosphorylase Inhibitor
	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.
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。
T62674	LSD1-IN-21
	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
	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。
T74781	UT-11
	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。
T69632	VRT-043198
	VRT-043198 是 VX-765 (Belnacasan) 的活性代谢物，是有效的、选择性的、能透过血脑屏障的caspase-1的抑制剂。VRT-043198 对caspase-1和 caspase-4 的 Ki 值分别为 0.8 nM 和 0.6 nM。
T83469	10m/ZS44
	10m/ZS44是一种能够穿透血脑屏障的Glioblastoma (GBM) 抑制剂，在小鼠异种移植模型中有效抑制了GBM肿瘤生长，并通过激活SIRT1/p53介导的细胞凋亡途径来抑制U251细胞增殖。
T62062	MAO-B-IN-7
	MAO-B-IN-7 是有效的、具有血脑屏障渗透性的MAO-B 和AChE 抑制剂。MAO-B-IN-7抑制人 AChE、电鳗 AChE 和 MAO-B 的IC50分别为 41 nM、87 nM 和 0.3 μM。MAO-B-IN-7 可以有效缓解氧化应激和神经炎症损伤。
T62578	BuChE-IN-1
	BuChE-IN-1 (Compound 23) 是一种丁酰胆碱酯酶 (BuChE) 的有效抑制剂。其中丁酰胆碱酯酶 (BuChE) 被认为是进展性阿尔茨海默病 (AD) 的生物标志物。BuChE-IN-1 具有低细胞毒性和高血脑屏障 (BBB) 渗透性。BuChE-IN-1 是一种具有潜力能够用于研究 AD 的 BuChE 抑制剂。
T78603	Sotuletinib dihydrochloride BLZ945 dihydrochloride	c-Fms	Tyrosine Kinase/Adaptors
	Sotuletinib (BLZ945) dihydrochloride 是一种CSF1-R特异性抑制剂，具有口服活性和血脑屏障透过性 (IC50=1 nM)。它能诱导肿瘤细胞凋亡，并在小鼠模型中有效抑制肿瘤生长，适用于癌症和肌萎缩侧索硬化症 (ALS) 研究。
T62664	Glucosylceramide synthase-IN-2
	Glucosylceramide synthase-IN-2 (compound T-690) 是一种有效的、具有血脑屏障通透性的、口服具有活力的 glucosylceramide synthase (GCS) 抑制剂，作用于人 GCS (IC50: 15 nM) 和小鼠 GCS (IC50: 190 nM)。Glucosylceramide synthase-IN-2 能够非竞争性抑制 C8 神经酰胺和 UDP 葡萄糖。Glucosylceramide synthase-IN-2 能够用于研究戈谢病。

化合物

nAChR agonist 1

Cat.No: T12165

Synonym: DUN71755

Target: AChR

Cat.No: T14389

Target: GluR

Cat.No: T9956

Target: Mitochondrial Metabolism, Lipid

Cat.No: T1741

Target: GSK-3

Cat.No: T22972

Target: Others

Cat.No: T6679

Synonym: SRT2104,sirtuin modulator,GSK2245840

Target: Sirtuin

Cat.No: TQ0075

Target: Neurotensin Receptor

Cat.No: T5490

Target: Sirtuin

Cat.No: TQ0026

Synonym: DWK-1339

Target: Beta Amyloid, Gamma-secretase

Cat.No: TQ0238

Synonym: LY3314814,AZD3293

Target: BACE

Cat.No: T10355

Target: COX

Cat.No: T5468

Target: Others, Epigenetic Reader Domain, Histone Acetyltransferase

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

Cat.No: T72420

Synonym: EP-0035985

Target: PTEN

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: 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

Cat.No: T14334

Target: GlyT

Casopitant mesylate

Cat.No: T10688

Synonym: GW679769B

Target: P450, Neurokinin receptor

NCT 501 hydrochloride

Cat.No: T41159

Lanabecestat HCl

Cat.No: T70807

α-Synuclein inhibitor 6

Cat.No: T61644

Cat.No: T40046

Synonym: UGT8-IN-1

Cat.No: T11185

Target: Histone Methyltransferase

Cat.No: T69608

Cat.No: T62142

TG11-77 free base

Cat.No: T69609

PF-5274857 hydrochloride

Cat.No: T35563

Cat.No: T79253

Target: Parasite

α-Synuclein inhibitor 4

Cat.No: T61611

Cat.No: T78969

Target: HDAC

mGluR2 modulator 1

Cat.No: T62202

Glycogen Phosphorylase Inhibitor

Cat.No: T37577

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: T62674

Glucosylceramide synthase-IN-1

Cat.No: T62898

Cat.No: T74781

Cat.No: T69632

Cat.No: T83469

Cat.No: T62062

Cat.No: T62578

Sotuletinib dihydrochloride

Cat.No: T78603

Synonym: BLZ945 dihydrochloride

Target: c-Fms

Glucosylceramide synthase-IN-2

Cat.No: T62664

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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