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32

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8450	TCN 213 TCN213	NMDAR	Neuroscience
	TCN 213 是一种可克服的(surmountable)、甘氨酸依赖的 GluN1/GluN2A NMDAR 选择性拮抗剂，当甘氨酸的含量为75、 750、7500 nM 时，IC50s 值分别为 0.55、3.5、40 μM。它可用于在药理学上监测 NMDAR 表达在发育中的皮层神经元中的转换。
T5104	BTSA1	Apoptosis; BCL	Apoptosis
	BTSA1 是一种有口服活性的 BAX 激活剂，IC50为 250 nM，EC50为 144 nM。它以高亲和力和特异性与 N 末端激活位点结合，并诱导 BAX 发生构象变化，从而导致BAX 介导的细胞凋亡。
T2131	Articaine hydrochloride Ultracaine,盐酸阿替卡因,阿替卡因,Articaine HCl,Hoe-045	Sodium Channel	Membrane transporter/Ion channel
	Articaine hydrochloride (Hoe-045) 一种牙科局部麻醉剂。
T12145L	N-Desethylsunitinib hydrochloride	VEGFR; PDGFR; c-Kit	Angiogenesis; Tyrosine Kinase/Adaptors
	N-Desethylsunitinib hydrochloride 是舒尼替尼的主要且具有药理活性的代谢物，是有效的 ATP 竞争性 VEGFR、PDGFRβ 和 KIT 抑制剂。
T0150	Hydroxyhexamide 乙酸己脲,(±)-Hydroxyhexamid	Potassium Channel; Drug Metabolite	Membrane transporter/Ion channel; Metabolism
	Hydroxyhexamide ((±)-Hydroxyhexamid) 是Acetohexamide 的活性代谢物, 可用作降血糖药。
T7806	Licarbazepine 10,11-hydroxy-10,11 Dihydrocarbamezer,10,11-二氢-10-羟基卡马西平	Others	Others
	Licarbazepine (10,11-hydroxy-10,11 Dihydrocarbamezer) 是一种有效的电压门控钠通道阻滞剂，具有抗惊厥和稳定情绪的功效。
T22431	SU5204 3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one	EGFR; VEGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	SU5204 (3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one) 是酪氨酸激酶抑制剂，是 SU5025 的类似物，对 FLK-1 (VEGFR-2) 和 HER2 的IC50分别为 4 和 51.5 μM。
TP1277	Bradykinin 缓激肽	Endogenous Metabolite; Bradykinin Receptor	GPCR/G Protein; Metabolism
	Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。它是炎症调节因子和神经调节因子，对几种血管和肾功能也有调节作用。
T0182L2	(±) Clopidogrel hydrogen sulfate 硫酸氢氯吡格雷,Plavix,Clopidogrel hydrogen sulfate,Iscover	P2Y Receptor	GPCR/G Protein; Neuroscience
	(±) Clopidogrel hydrogen sulfate (Iscover) 是一种在药理学和结构上类似于ticlopidine 的抗血小板药物，用于抑制脑血管疾病、外周血管疾病和冠状动脉疾病等各种疾病中的血栓。
T0785	Dexchlorpheniramine Maleate S-(+)-Chlorpheniramine maleate salt,右泛醇,马来酸右氯苯那敏	Dopamine Receptor; 5-HT Receptor; Norepinephrine; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Dexchlorpheniramine Maleate (S-(+)-Chlorpheniramine maleate salt) 是一种具有抗胆碱能特性的抗组胺药，用于治疗花粉热或荨麻疹等过敏性疾病。
T1447	Fenclonine Fenchlonine,PCPA,CP-10188,芬克洛宁,4-Chloro-DL-phenylalanine,DL-4-Chlorophenylalanine	Hydroxylase	Metabolism
	Fenclonine (CP-10188) 是一种有效的色氨酸羟化酶(Trp)的不可逆抑制剂。其中色氨酸羟化酶是 5-羟色胺生物合成的限速酶。
T13177	Taquidil
	Tocainide hydrochloride 是一种sodium channel 阻滞剂，它阻断神经膜中产生疼痛的病灶中的钠通道。Tocainide hydrochloride 是利多卡因 (lignocaine) 的一种伯胺类似物，可有效抑制各种情况下的室性心律失常。
T4284	Levamlodipine besylate 左旋氨氯地平,(S)-Amlodipine Besylate (103129-82-4(free base))	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Levamlodipine besylate ((S)-Amlodipine Besylate(103129-82-4(free base))) 是一种二氢吡啶钙通道阻滞剂，具有舒张血管的作用，可用于高血压和心绞痛的研究。
T20714	Levolansoprazole 左旋兰索拉唑,(S)-Lansoprazole,(-)-Lansoprazole	Proton pump	Membrane transporter/Ion channel
	Levolansoprazole ((S)-Lansoprazole) 是一种质子泵抑制剂，不可逆地抑制壁细胞中 H+/K+ 刺激的 ATPase 泵 (IC50: 5.2 µM)。它还抑制分离的犬壁细胞中的酸形成(IC50：82 µM)。 (R)-和 (S)-兰索拉唑均具有药理活性，具有相似的效力。
T1545	Levamlodipine 左旋氨氯地平,(S)-Amlodipine,S-amlodipine	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Levamlodipine (S-amlodipine) 是一种二氢吡啶钙通道阻滞剂，具有舒张血管的作用，可用于高血压和心绞痛的研究。
T28422	Pirlindole free base Pirlindole,Pyrazidol
	Pirlindole is a reversible inhibitor of monoamine oxidase A (RIMA). It is structurally and pharmacologically related to metralindole.
T21155	Metoprolol acid Atenolol acid,H117-04,H 117/04,SL 77-010
	Metoprolol acid is a urinary metoprolol metabolite and doesn't work pharmacologically.
T23959	Dactylyne
	Dactylyne is a new drug metabolism inhibitor of marine origin. It was isolated from the sea hare Aplysia dactylomela and characterized pharmacologically.
T32886	Lorzafone Lorzafonum,45-0088S
	Lorzafone is used in the detection & analysis of pharmacologically active benzodiazepines.
T13713	GP531	AChR	Neuroscience
	GP531 is a second-generation adenosine regulating agent. It is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.
T16389	Omidenepag	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Omidenepag is a pharmacologically active form of Omidenepag Isopropyl and is a selective, non-prostanoid EP2 receptor agonist (EC50: 1.1 nM). Omidenepag displays binding affinities (IC50: 10 nM for h-EP2).
T25691	Levamlodipine gentisate (S)-Amlodipine gentisate,(S)-(-)-Amlodipine gentisate
	Levamlodipine gentisate is a pharmacologically active enantiomer of amlodipine. Amlodipine is the dihydropyridine calcium channel blocker used as an antihypertensive and antianginal drug.
T16272	Naproxen etemesil LT-NS 001,MX 1094	PDE	Metabolism
	Naproxen is a COX-1 and COX-2 inhibitor (IC50s: 8.72 and 5.15 μM, respectively in cell assay). Naproxen etemesil is a lipophilic and non-acidic prodrug of naproxen. It is hydrolyzed to pharmacologically active Naproxen once absorbed.
T23962	DA-E 5090 DA-E-5090,DA-E5090,DA E 5090
	DA-E 5090 is a pharmacologically active metabolite of E 5090, is an interleukin-1 antagonist. DA-E 5090 is a novel inhibitor of IL-1 generation, in vitro inhibitory effects on the generation of IL-1 by human monocytes.
T1077L	Fluvoxamine
	Fluvoxamine (DU-23000) 作为选择性的5-羟色胺再吸收抑制剂，发挥抗抑郁作用。
T41192	CNV Dopamine
	CNV Dopamine is a carboxynitroveratryl (CNV)-caged dopamine; releases dopamine upon ultraviolet light stimulation (365 nm). Induces dopaminergic currents upon photolysis in brain slices expressing wild-type or GFP-labeled D2receptors. Displays no decrease in current (rundown) with UV light flash duration of up to 100 ms. Pharmacologically inactive prior to photolysis.
T10351	Aprocitentan D4 ACT-132577 D4	Others	Others
	Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA/ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).
T19360	Hydroxy bosentan Ro 48-5033	Others	Others
	Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Hydroxy bosentan assists BOS pharmacologically, retaining 10%-20% activities.
T69983	Ixazomib citrate EtOH
	Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrolyzing to pharmacologically active MLN2238 (ixazomib), is a next-generation proteasome inhibitor with demonstrated preclinical and clinical antimyeloma activity. MLN9708, compared with bortezomib, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinic...
T37391	PSEM 308 hydrochloride
	PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neu...
T69657	GS-441524 HCl
	GS-441524 is a potent inhibitor of feline infectious peritonitis (FIP) virus with an EC50 of 0.78 μM.. GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. GS-441524 is a molecular precursor to a pharmacologically active nucleoside triphosphate molecule. These analogs act as an alternative substrate and RNA-chain terminator of viral RNA dependent RNA polymerase. GS-441524 was non-toxic in feline cells at concentrations ...
T82805	Butaprost free acid
	(R)-Butaprost (free acid) 是PGE2的一个结构类似物，特异性地对EP2受体亚型有选择性。该化合物用于药理学研究，以确定不同人类及动物组织和细胞中EP受体的分布。去除甲酯基团并恢复C-1自然羧酸后，增强了(R)-butaprost与前列腺素受体的结合亲和力，通常情况下，游离酸形式的亲和力是相应酯形式的10到100倍。尽管(R)-butaprost作为C-16的较低活性差向异构体，其药理作用未经充分研究，但在1986年Gardiner的论文中提到的TR 4979即布他前列素，结构中的差向异构体错误表达为16(R)，实际为16(S)，该错误直至1990年代后期才被美国和日本的研究纠正。

化合物

Cat.No: T8450

Synonym: TCN213

Target: NMDAR

Cat.No: T5104

Target: Apoptosis, BCL

Articaine hydrochloride

Cat.No: T2131

Synonym: Ultracaine,盐酸阿替卡因,阿替卡因,Articaine HCl,Hoe-045

Target: Sodium Channel

N-Desethylsunitinib hydrochloride

Cat.No: T12145L

Target: VEGFR, PDGFR, c-Kit

Hydroxyhexamide

Cat.No: T0150

Synonym: 乙酸己脲,(±)-Hydroxyhexamid

Target: Potassium Channel, Drug Metabolite

Cat.No: T7806

Synonym: 10,11-hydroxy-10,11 Dihydrocarbamezer,10,11-二氢-10-羟基卡马西平

Target: Others

Cat.No: T22431

Synonym: 3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one

Target: EGFR, VEGFR, HER

Cat.No: TP1277

Synonym: 缓激肽

Target: Endogenous Metabolite, Bradykinin Receptor

(±) Clopidogrel hydrogen sulfate

Cat.No: T0182L2

Synonym: 硫酸氢氯吡格雷,Plavix,Clopidogrel hydrogen sulfate,Iscover

Target: P2Y Receptor

Dexchlorpheniramine Maleate

Cat.No: T0785

Synonym: S-(+)-Chlorpheniramine maleate salt,右泛醇,马来酸右氯苯那敏

Target: Dopamine Receptor, 5-HT Receptor, Norepinephrine, Histamine Receptor

Cat.No: T1447

Synonym: Fenchlonine,PCPA,CP-10188,芬克洛宁,4-Chloro-DL-phenylalanine,DL-4-Chlorophenylalanine

Target: Hydroxylase

Cat.No: T13177

Levamlodipine besylate

Cat.No: T4284

Synonym: 左旋氨氯地平,(S)-Amlodipine Besylate (103129-82-4(free base))

Target: Calcium Channel

Levolansoprazole

Cat.No: T20714

Synonym: 左旋兰索拉唑,(S)-Lansoprazole,(-)-Lansoprazole

Target: Proton pump

Cat.No: T1545

Synonym: 左旋氨氯地平,(S)-Amlodipine,S-amlodipine

Target: Calcium Channel

Pirlindole free base

Cat.No: T28422

Synonym: Pirlindole,Pyrazidol

Metoprolol acid

Cat.No: T21155

Synonym: Atenolol acid,H117-04,H 117/04,SL 77-010

Cat.No: T23959

Cat.No: T32886

Synonym: Lorzafonum,45-0088S

Cat.No: T13713

Target: AChR

Cat.No: T16389

Target: Prostaglandin Receptor

Levamlodipine gentisate

Cat.No: T25691

Synonym: (S)-Amlodipine gentisate,(S)-(-)-Amlodipine gentisate

Naproxen etemesil

Cat.No: T16272

Synonym: LT-NS 001,MX 1094

Target: PDE

Cat.No: T23962

Synonym: DA-E-5090,DA-E5090,DA E 5090

Cat.No: T1077L

Cat.No: T41192

Aprocitentan D4

Cat.No: T10351

Synonym: ACT-132577 D4

Target: Others

Hydroxy bosentan

Cat.No: T19360

Synonym: Ro 48-5033

Target: Others

Ixazomib citrate EtOH

Cat.No: T69983

PSEM 308 hydrochloride

Cat.No: T37391

Cat.No: T69657

Butaprost free acid

Cat.No: T82805

Cat. No.	Product Name	Target	Signaling Pathways
TN2080	Pinoresinol 松脂酚，松脂素,(+)-Pinoresinol	Apoptosis; NF-κB; CDK; p53	Apoptosis; Cell Cycle/Checkpoint; NF-κB
	Pinoresinol ((+)-Pinoresinol) 是一种植物来源的木质素，具有抗炎、保肝和杀真菌活性。它导致 CDK 抑制剂 p21(WAF1/Cip1) 在 mRNA 和蛋白质水平上调，抑制 NF-kappaB 和激活蛋白 1 。
T32704	Levoleucovorin levo-Folinic,LFP-754,Levofolinic acid,Levofolene,LFP 754
	Levoleucovorin, as a folate analog, consists of the pharmacologically active isomer of leucovorin.

天然产物

Cat.No: TN2080

Synonym: 松脂酚，松脂素,(+)-Pinoresinol

Target: Apoptosis, NF-κB, CDK, p53

Cat.No: T32704

Synonym: levo-Folinic,LFP-754,Levofolinic acid,Levofolene,LFP 754

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