首页工具

登录

搜索结果

Search Results for " penetration "

100

抑制剂 & 化合物

5

天然产物

如果没找到您满意的产品或者您对产品有其他要求，可以联系我们专业顾问为您提供针对性的合理建议。 QQ咨询网站留言咨询

Cat. No.	Product Name	Target	Signaling Pathways
T5447	Anle138b	Beta Amyloid; Others	Neuroscience; Others
	Anle138b 是一种毒性低，口服生物利用度高，血脑屏障通透性好的低聚物聚集抑调节剂，可阻断朊病毒蛋白和 α-突触核蛋白病理性聚集的形成。它在体内强烈抑制低聚物积累、神经元变性和疾病进展。它阻断 Aβ 通道并挽救淀粉样变性小鼠模型的疾病表型。
T5513	RO-3	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	RO3 是一种能透过大脑的P2X3和P2X2/3拮抗剂，口服有活性。它对人同型多聚体 P2X3和异型多聚体 P2X2/3受体的 pIC50分别为 5.9 和 7.0。
T2354	UNC 0631 UNC0631	Histone Methyltransferase	Chromatin/Epigenetic
	UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂，IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平，IC50为 25 nM。
TQ0232	UNC0646 UNC 0646	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0646 是一种有效的、选择性的同源蛋白赖氨酸甲基转移酶 G9a 和 GLP 抑制剂，IC50分别为 6 和 15 nM，对 G9a/GLP 的选择性比 SETD7、SUV39H2、SETD8 和 PRMT3 高。它降低 MDA-MB-231 细胞中H3K9me2的水平，IC50为 26 nM。
T11799	L-745870 hydrochloride	Dopamine Receptor	GPCR/G Protein; Neuroscience
	L-745870 hydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺 D4受体拮抗剂，Ki=0.43 nM。它对 D2(Ki 为 960 nM) 和 D3(Ki 为 2300 nM) 受体的亲和力相对较弱，对 5-HT2受体，sigma 位点和 α-肾上腺素受体表现出中等亲和力。
T60003	AC1-IN-1	Adenylyl cyclase	Neuroscience
	AC1-IN-1 是 1 型腺苷酸环化酶的选择性抑制剂（AC1，IC50 = 0.54 µM）。
T6039	TAK-285 TAK285,TAK 285	EGFR; MEK; HER; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors
	TAK-285 是一种新型 HER2 和 EGFR(HER1) 双重抑制剂，IC50 分别为 17 和 23 nM。它可穿过血脑屏障，有抗肿瘤活性，对 HER1/2 的选择性是 HER4 的 10 倍以上。
T6920	ON123300	FGFR; c-RET; JAK; CDK; PDGFR; Src; AMPK	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	ON123300 是一种可透过血脑屏障的多激酶抑制剂，作用于 CDK4、CDK6、Ark5、PDGFRβ、FGFR1、RET 和 Fyn，IC50值为3.9、9.82、5、26、26、9.2和11 nM。它在脑肿瘤中抑制 Akt 磷酸化及激活 Erk。
T0682	Lamivudine GR109714X,BCH-189,拉米夫定	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Lamivudine (BCH-189) 是一种核苷逆转录酶抑制剂，可抑制HIV 逆转录酶1和2 以及乙型肝炎病毒的逆转录酶。
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。
T0688	Ganciclovir BW 759,更昔洛韦,RS-21592,2'-Nor-2'-deoxyguanosine	Nucleoside Antimetabolite/Analog; Others; Antibiotic; Antifection; HSV	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
	Ganciclovir (2'-Nor-2'-deoxyguanosine) 是核苷类似物和口服抗病毒药物，对CMV 具有抗病毒活性。它用于治疗与艾滋病相关的巨细胞病毒感染的并发症。
T22337	Ganciclovir sodium RS-21592 sodium,Cytovene IV sodium,2'-Nor-2'-deoxyguanosine sodium,BW 759 sodium,更昔洛韦钠	Nucleoside Antimetabolite/Analog; Others; Antifection; HSV	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
	Ganciclovir sodium (Cytovene IV sodium) 是核苷类似物和口服抗病毒药物，具有抗病毒活性，尤其是针对巨细胞病毒和单纯疱疹病毒 1 型。
T2344	LY 344864 LY344864	5-HT Receptor	GPCR/G Protein; Neuroscience
	LY 344864 是一种特异性受体激动剂，有对克隆 5-HT1F 受体的亲和力，Ki 为6 nM。
T61148	Flutrimazole	Antifungal	Microbiology/Virology
	Flutrimazole is a dual-action imidazole antifungal compound, exhibiting both anti-inflammatory and antifungal properties. Notably, flutrimazole demonstrates limited transdermal penetration, making it particularly advantageous for topical applications in the treatment of fungal infections, especially those accompanied by inflammation.
T12679	(Rac)-VU 6008667	Others; AChR	Neuroscience; Others
	(Rac)-VU 6008667 是一种选择性的毒蕈碱乙酰胆碱受体亚型 5（M5 NAM）负异位调节剂，IC50 为 1.8 μM，pIC50 为 5.75，具有较高的中枢神经系统渗透性。
T10905	CXCR2-IN-1	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	CXCR2-IN-1是可渗透中枢神经系统的 CXCR2拮抗剂，pIC50值为9.3。
T35914	Epitinib succinate HMPL-813 succinate	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Epitinib succinate (HMPL-813 succinate) 是一种具有口服活性和脑渗透性的 EGFR 酪氨酸激酶抑制剂，可用于癌症研究。
T69757	PDDC inhibitor
	PDDC is the first nSMase2 inhibitor that possesses both favorable pharmacodynamics and pharmacokinetic (PK) parameters, including substantial oral bioavailability, brain penetration, and significant inhibition of exosome release from the brain in vivo.
T14345	Atropine methyl bromide 甲溴阿托品,Methylatropine bromide	AChR	Neuroscience
	Atropine methyl bromide (Methylatropine bromide) is a quaternary ammonium salt of atropine, characterized as a muscarinic receptor (mAChR) antagonist. It functions as a mydriatic to dilate the pupil during ophthalmic examination. Compared to atropine, it demonstrates reduced penetration into the central nervous system[1][2]. Its high polarity makes it particularly effective in relieving pyloric spasm in infants.
TP2501	Difelikefalin acetate Difelikefalin acetate(1024828-77-0 free base),CR 845 acetate,Difelikefalin醋酸盐,FE 202845 acetate	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Difelikefalin acetate (CR 845 acetate) 是一种外周受限的 kappa 阿片受体激动剂。CR845 表现出低 P450 CYP 抑制和对大脑的低渗透性。
T33604	Z-Glycine Carbobenzoxyglycine,N-苄氧羰基-甘氨酸,N-Carbobenzoxyglycine	Others	Others
	Z-Glycine (Carbobenzoxyglycine) 是一种药物-脂质结合物，旨在促进脑渗透，基于其亲脂性和与生物膜中脂质的相似性。
T61383	Diaziquone NSC 182986
	Diaziquone (NSC-182986)是一种水溶性的合成的氮杂环苯醌，可增强对血脑屏障的渗透，具有抗肿瘤活性，可用于治疗极性肾功能衰竭。
T10335	Antihistamine-1	P450	Metabolism
	Antihistamine-1 是能够渗透血脑屏障的 H1-抗组胺药 (Ki=6.9 nM), 它也是 CYP2D6 和 hERG 通道的抑制剂，其 IC50 值分别为 5.4 和 0.8 μM。
T20870	IR-820 IR 820,IR820,New Indocyanine Green
	IR-820 (New Indocyanine Green) 是一种近红外染料，具有很好的稳定性、良好的显色性和出色的荧光穿透性。IR-820 是一种红外血池造影剂，用于检测和量化活体动物的病变组织。IR-820 的最大 Ex 和 Em 分别为 710 纳米和 820 纳米。
T10630	BuChE-IN-TM-10 TM-10	AChR	Neuroscience
	BuChE-IN-TM-10 (TM-10) 是一种有效的丁基胆碱酯酶 (BuChE) 抑制剂，其IC50 值为8.9 nM。BuChE inhibitor 1能够抑制和分解自诱导的Aβ聚合, 表现出强大的抗氧化活性和良好的血脑屏障 (BBB) 渗透性。可用于阿尔兹海默症的研究。
T1101	Minocycline hydrochloride Minocycline HCl,盐酸米诺环素,美满霉素	HIF/HIF Prolyl-Hydroxylase; Antibacterial; Antibiotic	Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Minocycline hydrochloride (Minocycline HCl) 是四环素抗生素，具有出色的吸收和组织渗透性，可用于多种细菌感染以及痤疮的治疗。米诺环素可导致在开始治疗后 1 至 3 个月内发生的急性肝炎样综合征或通常在长期治疗后具有自身免疫特征的更隐匿的慢性肝炎。
T73447	NP10679
	NP10679 是一种选择性、pH 依赖性的GluN2B 亚基特异的 N-methyl-D-aspartate (NMDA) 受体抑制剂，具有较高的口服生物利用度和良好的脑穿透性。NP10679 在 pH 6.9 和 7.6 下，抑制 GluN2B 的IC50分别为 23 和 142 nM。NP10679 是histamine H1的拮抗剂和hERG 通道抑制剂，IC50分别为 73 和 620 nM。NP10679 是一种可逆的人肝脏CYP 酶抑制剂。
TP2505L	LAH4 acetate KKALLALALHHLAHLALHLALALKKA acetate,LAH4 acetate(184776-51-0 Free base)	Antibacterial	Microbiology/Virology
	LAH4 acetate 是所设计的两性肽抗生素的α -螺旋结构，能够与DNA 络合，与细胞表面膜结合后被包裹在核内体中，随着pH 值的下降破坏核内体膜。具有强大的抗菌、核酸转染和细胞渗透活性。LAH4 acetate 具有较高的质粒DNA 传递能力。LAH4 acetate 对细菌膜外膜中的阴离子脂具有很强的亲和力。
T26722	AZD7268 AZD-7268,AZD 7268
	AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration.
T12179	Nav1.1 activator 1	Others	Others
	Nav1.1 activator 1 is a highly potent activator of Nav1.1 with BBB penetration.
T12416	PF-03654746 Tosylate	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	PF-03654746 Tosylate is selective antagonist of histamine H3 receptor with high brain penetration.
T29142	VU6001966 VU 6001966,VU-6001966
	VU6001966 is a potent and selective mGlu2 inhibitor (mGlu2 IC50 = 78 nM) and negative allosteric modulator. VU6001966 exhibits excellent central nervous system (CNS) penetration.
T27474	GSK-345931A GSK-345931A free acid,GSK 345931A free acid,GSK 345931A
	GSK-345931A, an EP(1) receptor antagonist, shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain.
T70133	BAY-846
	BAY-846 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model.
T25124	AZ599 AZ-599,AZ 599
	AZ599 is a full agonist of CB1 with good solubility and low CNS penetration.
T11799L	L-745870	Dopamine Receptor	GPCR/G Protein; Neuroscience
	L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43 nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960 nM) and D3 (Ki: 2300 nM) receptors affinity.
T29359	2-n-Nonyl-1,3-dioxolane AI3-22560,Decanal ethylene acetal,2-Nonyldioxolane
	2-n-Nonyl-1,3-dioxolane is a biochemical. It is used as an absorption and penetration enhanceron transdermal.
T27437	GS-462808 GS462808,GS 462808
	GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.
T11797	L-690488	Others	Others
	L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.
T29016	Trolamine salicylate ester Trolamine salicylate (ester)
	Trolamine salicylate (ester) is a salicylate ester with Trolamine. Trolamine salicylate ester may have better skin penetration.
T16772	Ro 64-6198	Others	Others
	Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors.
T40051	Acid Ceramidase-IN-1
	Acid Ceramidase-IN-1 is a highly effective and orally bioavailable inhibitor of acid ceramidase (AC, ASAH-1), with an inhibitory concentration (IC50) of 0.166 μM. Additionally, Acid Ceramidase-IN-1 exhibits exceptional brain penetration capabilities in mice.
T28067	ML372 ML 372,ML-372
	ML372 is a potent and selective SMN Modulator (EC50 = 12 nM, 325% increase inSMN2) with good potency, pharmacokinetics, tolerance, and CNS penetration.
T71037	BAY-438
	BAY-438 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model.
T70420	PHA 543613 hydrochloride
	PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.
T35081	VU0486321 VU 0486321,VU-0486321
	VU0486321 is a potent mGlu1 PAM with moderate rat PK (CLp = 13.3. mL/min/kg,t1/2 = 54 min), good free fraction (human fu = 0.05, rat fu =0.03) and excellent CNS penetration (Kp = 1.02).
T17241	Auglurant VU0424238	Others	Others
	Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration.
T82175	HR2-18
	HR2-18为具有生物活性的肽类化合物，能够抑制SARS-CoV渗入细胞。
T37822	AR-C 141990 hydrochloride
	Monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.
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].

化合物

Cat.No: T5447

Target: Beta Amyloid, Others

Cat.No: T5513

Target: P2X Receptor

Cat.No: T2354

Synonym: UNC0631

Target: Histone Methyltransferase

Cat.No: TQ0232

Synonym: UNC 0646

Target: Histone Methyltransferase

L-745870 hydrochloride

Cat.No: T11799

Target: Dopamine Receptor

Cat.No: T60003

Target: Adenylyl cyclase

Cat.No: T6039

Synonym: TAK285,TAK 285

Target: EGFR, MEK, HER, Aurora Kinase

Cat.No: T6920

Target: FGFR, c-RET, JAK, CDK, PDGFR, Src, AMPK

Cat.No: T0682

Synonym: GR109714X,BCH-189,拉米夫定

Target: HIV Protease, Reverse Transcriptase

Etilevodopa hydrochloride

Cat.No: T24047

Synonym: Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester

Target: Others, Dopamine Receptor, Drug Metabolite

Cat.No: T0688

Synonym: BW 759,更昔洛韦,RS-21592,2'-Nor-2'-deoxyguanosine

Target: Nucleoside Antimetabolite/Analog, Others, Antibiotic, Antifection, HSV

Ganciclovir sodium

Cat.No: T22337

Synonym: RS-21592 sodium,Cytovene IV sodium,2'-Nor-2'-deoxyguanosine sodium,BW 759 sodium,更昔洛韦钠

Target: Nucleoside Antimetabolite/Analog, Others, Antifection, HSV

Cat.No: T2344

Synonym: LY344864

Target: 5-HT Receptor

Cat.No: T61148

Target: Antifungal

(Rac)-VU 6008667

Cat.No: T12679

Target: Others, AChR

Cat.No: T10905

Target: CXCR

Epitinib succinate

Cat.No: T35914

Synonym: HMPL-813 succinate

Target: EGFR

Cat.No: T69757

Atropine methyl bromide

Cat.No: T14345

Synonym: 甲溴阿托品,Methylatropine bromide

Target: AChR

Difelikefalin acetate

Cat.No: TP2501

Synonym: Difelikefalin acetate(1024828-77-0 free base),CR 845 acetate,Difelikefalin醋酸盐,FE 202845 acetate

Target: Opioid Receptor

Cat.No: T33604

Synonym: Carbobenzoxyglycine,N-苄氧羰基-甘氨酸,N-Carbobenzoxyglycine

Target: Others

Cat.No: T61383

Synonym: NSC 182986

Antihistamine-1

Cat.No: T10335

Target: P450

Cat.No: T20870

Synonym: IR 820,IR820,New Indocyanine Green

Cat.No: T10630

Synonym: TM-10

Target: AChR

Minocycline hydrochloride

Cat.No: T1101

Synonym: Minocycline HCl,盐酸米诺环素,美满霉素

Target: HIF/HIF Prolyl-Hydroxylase, Antibacterial, Antibiotic

Cat.No: T73447

Cat.No: TP2505L

Synonym: KKALLALALHHLAHLALHLALALKKA acetate,LAH4 acetate(184776-51-0 Free base)

Target: Antibacterial

Cat.No: T26722

Synonym: AZD-7268,AZD 7268

Nav1.1 activator 1

Cat.No: T12179

Target: Others

PF-03654746 Tosylate

Cat.No: T12416

Target: Histamine Receptor

Cat.No: T29142

Synonym: VU 6001966,VU-6001966

Cat.No: T27474

Synonym: GSK-345931A free acid,GSK 345931A free acid,GSK 345931A

Cat.No: T70133

Cat.No: T25124

Synonym: AZ-599,AZ 599

Cat.No: T11799L

Target: Dopamine Receptor

2-n-Nonyl-1,3-dioxolane

Cat.No: T29359

Synonym: AI3-22560,Decanal ethylene acetal,2-Nonyldioxolane

Cat.No: T27437

Synonym: GS462808,GS 462808

Cat.No: T11797

Target: Others

Trolamine salicylate ester

Cat.No: T29016

Synonym: Trolamine salicylate (ester)

Cat.No: T16772

Target: Others

Acid Ceramidase-IN-1

Cat.No: T40051

Cat.No: T28067

Synonym: ML 372,ML-372

Cat.No: T71037

PHA 543613 hydrochloride

Cat.No: T70420

Cat.No: T35081

Synonym: VU 0486321,VU-0486321

Cat.No: T17241

Synonym: VU0424238

Target: Others

Cat.No: T82175

AR-C 141990 hydrochloride

Cat.No: T37822

Cat.No: T36644

Cat. No.	Product Name	Target	Signaling Pathways
T4763	trans-Cyclohexane-1,2-diol trans-1,2-Cyclohexanediol,反式-1,2-环己二醇	Others; Endogenous Metabolite	Metabolism; Others
	trans-Cyclohexane-1,2-diol (trans-1,2-Cyclohexanediol) 是内源性代谢产物的一种。
TN1979	Neocnidilide 新蛇床内酯,新蛇床内酯,新川芎内酯	Antifungal	Microbiology/Virology
	Neocnidilide 是一种从川芎中提取的烷基邻苯二甲酸酯，具有抑制产生真菌毒素的真菌生长和杀虫。Neocnidilide 对 D. melanogaster 幼虫的LC50 值为 9.9 μmol/mL。它可以增强苯甲酸的皮肤渗透性。
T4820	Maleimide 马来酰亚胺,2,5-Pyrroledione	Others	Others
	Maleimide (2,5-Pyrroledione) 可用于制备荧光探针，主要用于硫醇分析物的特异性检测。它也可用于制备用于癌症研究的抗体-药物偶联物 (ADC)。
T4943	Monoolein 1-Oleoyl-rac-glycerol,甘油单油酸酯	Others; Endogenous Metabolite	Metabolism; Others
	Monoolein (1-Oleoyl-rac-glycerol) 是内源性代谢产物的一种。
T3229	Cytochalasin D	ATPase; p38 MAPK; Calcium Channel; Akt; PI3K	Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
	Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

天然产物

trans-Cyclohexane-1,2-diol

Cat.No: T4763

Synonym: trans-1,2-Cyclohexanediol,反式-1,2-环己二醇

Target: Others, Endogenous Metabolite

Cat.No: TN1979

Synonym: 新蛇床内酯,新蛇床内酯,新川芎内酯

Target: Antifungal

Cat.No: T4820

Synonym: 马来酰亚胺,2,5-Pyrroledione

Target: Others

Cat.No: T4943

Synonym: 1-Oleoyl-rac-glycerol,甘油单油酸酯

Target: Others, Endogenous Metabolite

Cat.No: T3229

Target: ATPase, p38 MAPK, Calcium Channel, Akt, PI3K

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Copyright © 2015-2024 TargetMol Chemicals Inc. All rights reserved. 沪ICP备20019793号-4

沪公网安备 31010602006700号

沪公网安备 31010602006700号

TargetMol Loading

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼