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35

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3990	AA26-9	Phospholipase; Serine Protease	Metabolism; Proteases/Proteasome
	AA26-9 是广谱丝氨酸水解酶的高效抑制剂。它的靶点包括丝氨酸肽酶、酰胺酶、脂肪酶、酯酶和硫酯酶。在永生化 T 细胞系，检测到它对 40+ 丝氨酸水解酶中的 1/3 有抑制作用。
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。
T3359	Aprotinin 抑酶肽,抑肽酶,Bovine Pancreatic Trypsin Inhibitor,Traskolan,Antilysin	Others; Serine Protease; Influenza Virus; Proteasome	Microbiology/Virology; Others; Proteases/Proteasome; Ubiquitination
	Aprotinin (Traskolan) 是分离自牛肺的一种广谱丝氨酸蛋白酶抑制剂，可抑制多种不同酯酶和蛋白酶的活性。
T14048	5-CFDA 5-羧基荧光素二乙酸酯,5-Carboxyfluorescein diacetate	Others	Others
	5-CFDA (5-Carboxyfluorescein diacetate) 是可透过细胞屏障并被水解为5-carboxyfluorescein，可标记人椎间盘细胞，以便体外荧光显微镜观察。
T15378L	Gemcitabine elaidate hydrochloride CO-101 hydrochloride,Gemcitabine elaidate hydrochloride(210829-30-4(free base)),Gemcitabine 5'-elaidate hydrochloride,CP-4126 hydrochloride	Others	Others
	Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 可以口服给药，具有抗肿瘤活性。
T14319	Aripiprazole Lauroxil	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Aripiprazole lauroxil 是一种长效注射剂 (LAI) 的抗精神病药物，是阿立哌唑的 N-酰氧基甲基前药形式。它能够被体内酯酶裂解为 N-羟甲基阿立哌唑(月桂酸)，再裂解为阿立哌唑，无毒性。
T15082	DDAO	Others	Others
	DDAO 是有潜在用途的近红外红色荧光探针，其激发波长 (600-650 nm) 和长发射波长 (λem = 656 nm)可以调节。它可用于不同酶活性的检测，如 β-半乳糖苷酶，羧酸酯酶 2，硫酸酯酶，蛋白质磷酸酶 2A，人白蛋白和酯酶。
T3934	Isavuconazonium sulfate	Antifungal	Microbiology/Virology
	Isavuconazonium sulfate 是一种口服活性抗真菌药，是活性三唑类抗真菌药物 Isavuconazole 的前药，可用于侵袭性曲霉菌病和毛霉菌病。
T68889	Esterastin
	Esterastin is an Inhibitor of esterases.
T25755	Lorajmine Lorajmina
	Lorajmine, a monochloroacetyl derivative of ajmaline, is a class Ia antiarrhythmic agent that is rapidly hydrolyzed to ajmaline by plasma and tissue esterases.
T20518	Fosinoprilat SQ-27,519,Fosinopril diacid,SQ 27,519,SQ27,519
	Fosinoprilat, an active phosphinic acid metabolite of prodrug fosenopril, is activated by esterases in vivo. Fosinoprilat binds zinc with phosphinic acid group.
T4574L	Sacubitril sodium AHU377,AHU-377,LCZ696,AHU 377
	Sacubitril is an angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases.
T26611	AM7499 AM 7499,AM-7499
	AM7499 is a non-selective cannabinoid receptor agonist with remarkably high in vitro and in vivo potency. It is readily hydrolysed by plasma esterases and to be less prone to deposition in bodily fat than existing classical cannabinoid agonists.
T35612	CytoCalcein™ Violet 500
	CytoCalcein Violet 500 is a fluorogenic dye used to assess cell viability. It is a cell-permeable dye that, upon entering cells, is cleaved by intracellular esterases. CytoCalcein Violet 500 is retained by living cells and displays excitation/emission maxima of 405/500 nm, respectively.
T37918	Prostaglandin E2 isopropyl ester Prostaglandin E2 isopropyl ester
	Prostaglandin E2 (PGE2) isopropyl ester is a more lipophilic form of the free acid, PGE2. PG esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid by endogenous esterases upon in vivo administration, making the esters useful prodrugs. In general, the C-1 esters of PGs show greatly diminished receptor activity in vitro compared to the parent free acids.
T35939	Dabigatran Acyl-β-D-Glucuronide
	Dabigatran acyl-β-D-glucuronide is a major active metabolite of the thrombin inhibitor dabigatran . The prodrug of dabigatran, dabigatran etexilate , is hydrolyzed by plasma esterases to form dabigatran, which is metabolized primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT2B15 to form dabigatran acyl-β-D-glucuronide. Dabigatran acyl-β-D-glucuronide increases activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma equipotently to dabigatran.
T35611	CytoCalcein™ Violet 450
	CytoCalcein Violet 450 is a fluorogenic dye used to assess cell viability. It is a cell-permeable dye that, upon entering cells, is cleaved by intracellular esterases. CytoCalcein Violet 450 is retained by living cells and displays excitation/emission maxima of 405/450 nm, respectively.
T37290	Resolvin D3 methyl ester
	Resolvin D3 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.
T37169	Resolvin D2 methyl ester
	Resolvin D2 (RvD2) is a lipid mediator biosynthesized by the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase. It evokes diverse anti-inflammatory effects which may mediate the resolution of inflammation. RvD2 methyl ester is a methyl ester version of the free acid which may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.
T36327	Calcein Red™ AM
	Calcein Red AM is a fluorogenic dye that is used to assess cell viability. As the acetoxymethyl ester, Calcein Red AM is non-fluorescent but cell-permeant and is hydrolyzed to the fluorescent probe Calcein Red by intracellular esterases. Calcein Red is retained by living cells and displays excitation/emission maxima of 560/574 nm, respectively. Calcein Red AM is a red-emitting variant of the green fluorophore calcein AM , which has been used to evaluate cell viability and cytotoxicity.
T37168	Resolvin D1 methyl ester Resolvin D1 methyl ester
	Resolvin D1 is produced physiologically from the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase . It reduces human polymorphonuclear leukocyte transendothelial migration, the earliest event in acute inflammation, with an EC50 value of ~30 nM. RvD1 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracell...
T70621	Cefditoren Pivoxil HCl
	Cefditoren Pivoxil is a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity. Cefditoren pivoxil is a prodrug that is rapidly hydrolyzed by intestinal esterases during absorption to the microbiologically active cefditoren, an active aminothiazolyl cephalosporin. Cefditoren inactivates penicillin binding proteins (PBPs) thereby interfering with peptidoglycan synthesis and inhibiting bacterial cell wall synthesis.
T38123	5(6)-Carboxy-2′,7′-dichlorofluorescein diacetate
	5(6)-Carboxy-2’,7’-dichlorofluorescein diacetate is an oxidant-sensitive and cell-permeable fluorescent probe.1Base hydrolysis of the ester bonds by intracellular esterases releases the acetate groups and the resulting compound, 5(6)-carboxy-2’,7’,-dichlorofluorescein, is oxidized by reactive oxygen species (ROS) and nitric oxide (NO) and displays excitation/emission maxima of 504 and 530 nm, respectively, which can be quantified as a measure of oxidant production. 1.Hempel, S.L., Buettner, G.R....
T36325	Calcein Blue AM
	Calcein Blue AM 是一种可以透过细胞膜的活细胞标记染料。进入细胞后，细胞内的酯酶切割乙酰氧基甲基 (AM) 的酯基，产生无法透过细胞膜的 Calcein Blue 荧光染料。
T36388	Rhod-5N AM
	Rhod-5N AM is a cell-permeant acetoxymethyl ester of the fluorescent calcium indicator rhod-5N . As rhod-5N AM enters cells, it is hydrolyzed by intracellular esterases to produce rhod-5N. Rhod-5N displays a low affinity for calcium (Kd = 19 μM). Low affinity calcium indicators are particularly useful for studying compartments with high concentrations of calcium, such as endoplasmic reticulum, where high affinity dyes will be insensitive to luminal fluctuations. Rhod-5N has excitation/emission m...
T36369	3,6-diacetoxy Phthalonitrile
	3,6-diacetoxy Phthalonitrile is a fluorescent probe for monitoring intracellular pH by flow cytometry in living cells. It rapidly crosses cell membranes and is cleaved by cytosolic esterases to form the fluorescent pH indicator 2,3-dicyano-hydroquinone (DCH), which is excited at UV wavelengths. DCH can be excited at 351 nm, with pH-dependent emission in the range of 450-476 nm (pH 5.0-10.0) using a potassium-based buffer.
T38352	Ebelactone A
	Ebelactone A is a β-lactone enzyme inhibitor that was first isolated from a cultured strain of soil actinomycetes. It can inhibit esterases, lipases, and N-formylmethionine aminopeptidases (IC50s = 0.056, 0.003, and 0.08 μg/ml, respectively) found on cell surfaces, which has been shown to stimulate host defense in immune cells. Ebelactone A is also reported to inhibit cutinases produced by fungal pathogens, thus demonstrating a plant-protective function.
T36871	5-Octyl-α-ketoglutarate
	In addition to its role in the Krebs cycle, α-ketoglutarate (2-oxoglutarate) has roles as a substrate or modulator of enzymes. 5-Octyl-α-ketoglutarate, also known as α-ketoglutarate octyl ester, is a stable, cell-permeable molecule that generates free α-ketoglutarate upon hydrolysis of the ester bond by cytoplasmic esterases. It is used in experiments to increase levels of intracellular α-ketoglutarate. 5-Octyl-α-ketoglutarate has been shown to modulate a variety of enzymes and signaling pathway...
T15378	Gemcitabine elaidate Gemcitabine 5'-elaidate,反油酸吉西他滨,吉西他滨反油酸酯,Gemcitabine (elaidate),CO-101,CP-4126	Apoptosis; Nucleoside Antimetabolite/Analog; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Gemcitabine elaidate (CP-4126) 是 Gemcitabine 的亲脂性前药。它通过酯酶转化为 Gemcitabine 以被磷酸化。它具有抗肿瘤活性。
T36112	Clopidogrel Carboxylic Acid (hydrochloride)
	Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active thiol metabolite via CYP2C19 in the liver enables its anti-aggregating activity. An estimated 15% of administered clopidogrel is metabolized by CYP2C19 to the thiol metabolite. Clopidogrel carboxylic acid i...
T37188	BTC AM
	BTC AM is a cell-permeable acetoxy-methyl ester of BTC . As BTC AM enters cells, it is hydrolyzed by intracellular esterases to produce BTC. BTC is a low affinity calcium indicator (Kd = 7-26 μM) that displays excitation/emission spectra of 401/529 nm, respectively. It exhibits a shift in the excitation maximum from approximately 480 to 401 nm upon calcium binding, enabling determination of ratiometric calcium measurements. BTC is suitable for detecting elevated calcium levels associated with ac...
T37320	Rhod-FF AM
	Rhod-FF AM is a cell-permeant acetoxymethyl ester of the fluorescent calcium indicator rhod-FF . As rhod-FF AM enters cells, it is hydrolyzed by intracellular esterases to produce rhod-FF. Rhod-FF is a difluorinated analog of the cell-impermeant calcium indicator rhod-2. It has a very low affinity for calcium (Kd = 320 μM). Low affinity calcium indicators are particularly useful for studying compartments with high concentrations of calcium, such as endoplasmic reticulum, where high affinity dyes...
T83293	5-CFDA-AM
	5-CFDA-AM作为一种细胞渗透性的酯酶底物，用于测定酶活性和细胞膜完整性，该化合物为电子中性，其渗透细胞的能力超过CFDA且所需浓度更低。在细胞内部，5-CFDA-AM经酯酶水解生成羧基荧光素，后者带有额外负电荷，因此能更有效地在细胞内保留。
T71305	Clofibric Acid-d4
	Clofibric acid-d4 is intended for use as an internal standard for the quantification of clofibric acid by GC- or LC-MS. Clofibric acid is a peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 50 µM in a transactivation assay) and the active metabolite of clofibrate. It is formed from clofibrate by tissue and serum esterases. Dietary administration of clofibric acid (0.067-0.22%) reduces serum cholesterol, phospholipid, and triglyceride levels in rats. It decreases glutamate oxal...
T37762	Fura-FF AM
	Fura-FF AM is a cell-permeable acetoxymethyl ester of the fluorescence calcium indicator fura-FF (potassium salt) . As fura-FF AM enters cells, it is hydrolyzed by intracellular esterases to produce fura-FF. Fura-FF is a difluorinated derivative of the calcium indicator fura-2 . Unlike, fura-2, fura-FF has negligible magnesium sensitivity, thus reducing interference from this cation. Fura-FF also has a higher calcium dissociation constant than fura-2 (Kd(calcium) = 6 and 0.14 μM, respectively). ...

化合物

Cat.No: T3990

Target: Phospholipase, Serine Protease

Etilevodopa hydrochloride

Cat.No: T24047

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

Target: Others, Dopamine Receptor, Drug Metabolite

Cat.No: T3359

Synonym: 抑酶肽,抑肽酶,Bovine Pancreatic Trypsin Inhibitor,Traskolan,Antilysin

Target: Others, Serine Protease, Influenza Virus, Proteasome

Cat.No: T14048

Synonym: 5-羧基荧光素二乙酸酯,5-Carboxyfluorescein diacetate

Target: Others

Gemcitabine elaidate hydrochloride

Cat.No: T15378L

Synonym: CO-101 hydrochloride,Gemcitabine elaidate hydrochloride(210829-30-4(free base)),Gemcitabine 5'-elaidate hydrochloride,CP-4126 hydrochloride

Target: Others

Aripiprazole Lauroxil

Cat.No: T14319

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T15082

Target: Others

Isavuconazonium sulfate

Cat.No: T3934

Target: Antifungal

Cat.No: T68889

Cat.No: T25755

Synonym: Lorajmina

Cat.No: T20518

Synonym: SQ-27,519,Fosinopril diacid,SQ 27,519,SQ27,519

Sacubitril sodium

Cat.No: T4574L

Synonym: AHU377,AHU-377,LCZ696,AHU 377

Cat.No: T26611

Synonym: AM 7499,AM-7499

CytoCalcein™ Violet 500

Cat.No: T35612

Prostaglandin E2 isopropyl ester

Cat.No: T37918

Synonym: Prostaglandin E2 isopropyl ester

Dabigatran Acyl-β-D-Glucuronide

Cat.No: T35939

CytoCalcein™ Violet 450

Cat.No: T35611

Resolvin D3 methyl ester

Cat.No: T37290

Resolvin D2 methyl ester

Cat.No: T37169

Calcein Red™ AM

Cat.No: T36327

Resolvin D1 methyl ester

Cat.No: T37168

Synonym: Resolvin D1 methyl ester

Cefditoren Pivoxil HCl

Cat.No: T70621

5(6)-Carboxy-2′,7′-dichlorofluorescein diacetate

Cat.No: T38123

Calcein Blue AM

Cat.No: T36325

Cat.No: T36388

3,6-diacetoxy Phthalonitrile

Cat.No: T36369

Cat.No: T38352

5-Octyl-α-ketoglutarate

Cat.No: T36871

Gemcitabine elaidate

Cat.No: T15378

Synonym: Gemcitabine 5'-elaidate,反油酸吉西他滨,吉西他滨反油酸酯,Gemcitabine (elaidate),CO-101,CP-4126

Target: Apoptosis, Nucleoside Antimetabolite/Analog, Autophagy

Clopidogrel Carboxylic Acid (hydrochloride)

Cat.No: T36112

Cat.No: T37188

Cat.No: T37320

Cat.No: T83293

Clofibric Acid-d4

Cat.No: T71305

Cat.No: T37762

Cat. No.	Product Name	Target	Signaling Pathways
T15255	Etilevodopa Levodopa ethyl ester,L-DOPA ethyl ester	Others	Others
	Etilevodopa is an ethyl-ester prodrug of Levodopa which is used for the treatment of Parkinson's disease (PD). It is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Levodopa is the direct precursor of dop

天然产物

Cat.No: T15255

Synonym: Levodopa ethyl ester,L-DOPA ethyl ester

Target: Others

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