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30

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T38514	PMEDAP	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	PMEDAP 是有效的人类免疫缺陷病毒 (HIV) 复制抑制剂。它具有抗小鼠巨细胞病毒活性。它有效抑制莫罗尼鼠肉瘤病毒诱导的肿瘤形成和相关死亡率。
T1643	Penciclovir 喷昔洛韦,BRL 39123,VSA 671	HCV Protease; Antifection; HSV	Microbiology/Virology; Proteases/Proteasome
	Penciclovir (BRL 39123) 是一种疱疹病毒核苷类似物 DNA 聚合酶抑制剂。它作用于HSV1 和 2，IC50分别为 0.04-1.8 μg/mL 和 0.06-4.4 μg/mL。
T22821	GSK J5 GSK-J5,GSKJ5	Histone Demethylase	Chromatin/Epigenetic
	GSK J5 对血吸虫和蠕虫具有抑制作用，常被当作一种吸血虫杀虫剂。GSK J5 以剂量和时间依赖的方式促进血吸虫死亡。GSK J5 可提高血吸虫死亡率、减低成虫活力。
T2264	AM281 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺	Cannabinoid Receptor	GPCR/G Protein
	AM281 是选择性CB1受体拮抗剂，IC50=9.91 nM。它抑制 CB2 受体，IC50=13000 nM。
T76251L	Ac-FEID-CMK TFA	Pyroptosis	Apoptosis; Immunology/Inflammation
	Ac-FEID-CMK TFA 是一种选择性斑马鱼 GSDMEb 衍生肽抑制剂，可减少感染性休克的死亡率和肾损伤。Ac-FEID-CMK TFA 在体内可抑制焦亡，缓解败血性 AKI (急性肾损伤)，抑制 caspy2 介导的非典型炎症小体通路发挥作用。
T0782	Benzthiazide Aquatag,苄噻嗪,Lemazide,Dihydrex	Carbonic Anhydrase	Metabolism
	Benzthiazide (Lemazide) 是长效利尿剂及抗高血压剂。它也是碳酸酐酶 9 的抑制剂，他对 CA9，CA2 和 CA1 的 Ki 分别为 8.0，8.8 和 10 nM。它对肿瘤细胞增殖具有抑制作用。
T9543	Syk Inhibitor II hydrochloride	Others	Others
	Syk Inhibitor II hydrochloride 信号传导的影响在狼疮中可能很突出。
T68025	Zoliprofen	Others	Others
	Zoliprofen 是一种一种高效的且可口服的非甾体抗炎剂，具有抗炎、解热和镇痛活性，对角叉菜素、制霉菌素、刀豆球蛋白A 诱导的大鼠爪水肿，以及抗大鼠兔血清诱导的骨折或背皮水肿具有抑制作用。Zoliprofen 在大鼠和兔子中对胶原蛋白或花生四烯酸引起的血小板聚集方面比布洛芬和非诺洛芬有效20倍。Zoliprofen 对小鼠内毒素诱导的腹泻和花生四烯酸诱导的兔急性死亡抑制作用显著。
T71865	DSM43
	DSM43 is a dihydroorotate dehydrogenase (DHODH) inhibitor. Malaria puts at risk nearly half the world's population and causes high mortality in sub-Saharan Africa, while drug resistance threatens current therapies. The pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) is a validated target for malaria treatmen
T82355	GABA-IN-2
	GABA-IN-2 (Compound 5) 为GABA抑制剂，展现出杀幼虫效果和显著的杀虫能力，在浓度50 mg/L下的死亡率达到87%。
T81886	Maculatin 1.1 TFA
	Maculatin 1.1 TFA 是具有抗金黄色葡萄球菌活性的抗菌肽，其 MIC 值为 7 μM。该肽通过在细菌的菌膜上形成孔道，导致细菌死亡。
T61067	MurB-IN-1
	MurB-IN-1 (compound 44) is a potent inhibitor of MurB, an essential enzyme involved in the synthesis of bacterial cell wall. With a binding affinity of K d 3.57 μM, MurB-IN-1 effectively hinders the activity of MurB, presenting a promising therapeutic option against P. aeruginosa, a highly virulent and opportunistic pathogen associated with severe infections and mortality [1].
T82356	GABA-IN-1
	GABA-IN-1 (Compound 6)为GABA抑制剂，具备显著的杀幼虫效能与杀虫功能，在浓度为50 mg/L时，致死率达93%。
T37692	Piericidin B
	Piericidin B is a bacterial metabolite that has been found inS. mobaraensisand has insecticidal and antimicrobial activities.1,2,3It inhibits NADH oxidase activity in isolated bovine heart mitochondria and inhibits respiration in isolated rat liver mitochondria and isolated cockroach (P. americana) muscle mitochondria.2,3Topical application of piericidin B (4 μg/insect) induces mortality in 87.5% of houseflies (M. domestica).1It induces 93.3, 100, and 100% mortality in rice stem borer (C. simple...
T38861	Tat-beclin 1
	Tat-beclin 1, a peptide derived from the autophagy protein beclin 1, is a powerful inducer of autophagy. It interacts with GAPR-1 (GLIPR2), a negative regulator of autophagy. Tat-beclin 1 effectively reduces the buildup of polyglutamine expansion protein aggregates and inhibits the replication of various pathogens, such as HIV-1, in laboratory experiments. In addition, it has demonstrated the ability to decrease mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
T63314	Antifungal agent 31
	Antifungal agent 31 是口服具有活力的、拥有吡咯三嗪酮支架的三唑类抗真菌剂，对念珠菌和丝状真菌表现出一定的抗真菌作用。Antifungal agent 31 能够明显减少两种致死性全身感染小鼠模型的死亡率和肾脏真菌负担。
T36183	Neospiramycin I
	Neospiramycin I is a macrolide antibiotic and derivative of spiramycin I.1It is active against the macrolide-sensitive KB210, but not the macrolide-resistant KB224, strain ofS. aureus(MICs = 3.12 and >100 μg/ml, respectively), as well asB. cereus,B. subtilis,M. luteus,E. coli, andK. pneumoniae(MICs = 1.56, 3.12, 3.12, 0.2, 50, and 12.5 μg/ml, respectively). Neospiramycin I binds toE. coliribosomes with an IC50value of 1.2 μM. It protects against mortality in a mouse model ofS. pneumoniaetype III...
T76251	Ac-FEID-CMK
	Ac-FEID-CMK 是一种有效的斑马鱼特异性GSDMEb 衍生肽抑制剂。Ac-FEID-CMK 可减轻感染性休克的死亡率和肾损伤。Ac-FEID-CMK 在体内可抑制焦亡，减轻败血性 AKI (急性肾损伤)。Ac-FEID-CMK 可抑制 caspy2 介导的非典型炎症小体通路。
T28884	SUN-C5174 SUNC-5174
	SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma
T37754	Avilamycin A
	Avilamycin A is an antibiotic.1 It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).1,2 Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.3 Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock. \|1. Watkins, K.L., Shryock, T.R., Dearth, R.N., et al. In-vitro antimicrobial susceptibility of Cl...
T83068	Antifungal agent 77
	Antifungalagent 77 (Compound 13h) 作为一种化合物，展现出对粘虫、棉铃虫、玉米螟及草地贪夜蛾的杀虫效力，其浓度为500 μg/mL时，相应的死亡率为30%、25%、40% 和 25%。同时，该化合物对斑马鱼胚胎具有毒性，其半致死浓度（LC50）为2.43 μg/mL。
T83872	Oleoyl-L-carnitine chloride L-Carnitine oleoyl ester,L-Octadecanoylcarnitine,C18:1 Carnitine,CAR 18:1
	Oleoyl-L-carnitine是一种长链酰基肉碱，也是一种糖苷转运体2（GlyT2；IC50 = 340 nM）的抑制剂，对GlyT2比对GlyT1（IC50 = >10,000 nM）具有选择性。慢性肾脏病或接受初始血液透析的终末期肾脏病患者的血浆中Oleoyl-L-carnitine水平增高，这与心血管死亡率相关。
T38118	Zanamivir-13C,15N2 Zanamivir-13C,15N2
	Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intra...
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...
T38156	N-Acetyl-DL-penicillamine
	N-Acetyl-DL-penicillamine is a chelating agent.1,2,3It inhibits the binding of methyl mercury to isolated human erythrocytes by 50% and removes 50% of methyl mercury ions from methyl mercury-loaded blood cells when used at a concentration of 1 mM.1,2N-Acetyl-DL-penicillamine (3 mmol/kg per day, p.o.) reduces the biological half-life of mercury and decreases liver, kidney, brain, and blood mercury levels, as well as increases urinary excretion of mercury in a concentration-dependent manner, in mi...
T76058	Tat-beclin 1 TFA
	Tat-beclin 1 TFA是一种来源于自噬蛋白区域(beclin 1)的肽，有效诱导自噬(autophagy)并与GAPR-1 (GLIPR2)发生相互作用，具有显著的自噬负调控作用。该化合物能有效减少体外聚谷氨酰胺扩增蛋白聚集体的积累，并抑制HIV-1等多种病原体的复制。同时，Tat-beclin 1 TFA能显著降低感染基孔肯雅病(CHIKV)或西尼罗河病毒(WNV)小鼠的死亡率。
T37052	Tetranactin
	Tetranactin is a macrotetrolide and a monovalent cation ionophore that has been found in S. aureus and has antibacterial, insecticidal, and mitogenic activities. It exhibits an equilibrium permeability ratio 1,000-fold greater for lithium than sodium or cesium ions accross bilayer membranes at low voltages. Tetranactin inhibits the growth of Gram-positive bacteria and C. miyabeanus and R. solani fungi when used at concentrations less than 0.9 μg/ml. Tetranactin (0.5-1.5 μg per insect) dose-depen...
T38297	Ribavirin-13C5 Ribavirin-13C5
	Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coro...
T36618	Rupatadine
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...
T65396	Piperazine 2HCl
	Piperazine (2HCl) is gamma-aminobutyric acid (GABA) agonists and its major effects appear to be on the central nervous system. Piperazine was the anthelmintic with the greatest number of reports of toxicoses and suspected toxicoses in cats. Piperazine neurotoxicity in cats and dogs usually was manifested by muscle tremors, ataxia, and/or behavioral disturbances within 24 hours after estimated daily dose(s) between 20 and 110 mg/kg[1]. For di-substituted derivatives, ciprofloxacin was selected an...

化合物

Cat.No: T38514

Target: Others, HIV Protease

Cat.No: T1643

Synonym: 喷昔洛韦,BRL 39123,VSA 671

Target: HCV Protease, Antifection, HSV

Cat.No: T22821

Synonym: GSK-J5,GSKJ5

Target: Histone Demethylase

Cat.No: T2264

Synonym: 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺

Target: Cannabinoid Receptor

Ac-FEID-CMK TFA

Cat.No: T76251L

Target: Pyroptosis

Cat.No: T0782

Synonym: Aquatag,苄噻嗪,Lemazide,Dihydrex

Target: Carbonic Anhydrase

Syk Inhibitor II hydrochloride

Cat.No: T9543

Target: Others

Cat.No: T68025

Target: Others

Cat.No: T71865

Cat.No: T82355

Maculatin 1.1 TFA

Cat.No: T81886

Cat.No: T61067

Cat.No: T82356

Cat.No: T37692

Cat.No: T38861

Antifungal agent 31

Cat.No: T63314

Neospiramycin I

Cat.No: T36183

Cat.No: T76251

Cat.No: T28884

Synonym: SUNC-5174

Cat.No: T37754

Antifungal agent 77

Cat.No: T83068

Oleoyl-L-carnitine chloride

Cat.No: T83872

Synonym: L-Carnitine oleoyl ester,L-Octadecanoylcarnitine,C18:1 Carnitine,CAR 18:1

Zanamivir-13C,15N2

Cat.No: T38118

Synonym: Zanamivir-13C,15N2

Cat.No: T70063

N-Acetyl-DL-penicillamine

Cat.No: T38156

Tat-beclin 1 TFA

Cat.No: T76058

Cat.No: T37052

Cat.No: T38297

Synonym: Ribavirin-13C5

Cat.No: T36618

Piperazine 2HCl

Cat.No: T65396

Cat. No.	Product Name	Target	Signaling Pathways
T15277	Fervenulin	Parasite	Microbiology/Virology
	Fervenulin 具有杀灭线虫活性，抑制线虫M. incognita 卵孵化和 J2 的校正死亡率，MIC 分别为 30 μg/mL 和 120 μg/mL。
TN1742	Homovanillyl alcohol 高香草醇,4-羟基-3-甲氧基苯乙醇	TNF; Drug Metabolite	Apoptosis; Metabolism
	Homovanillyl alcohol 是羟基酪醇的生物代谢物。Hydroxytyrosol 是存在于原始橄榄油和葡萄酒中的酚类化合物。它能够保护红细胞免受氧化损伤，并对心血管具有保护作用。
T4S0878	Prunetin 樱黄素,Prunusetin	ERK; Dehydrogenase; NF-κB	MAPK; Metabolism; NF-κB
	Prunetin (Prunusetin) 是一种O-甲基化异黄酮，具有抗炎的作用。它是人醛脱氢酶的有效抑制剂。
T13753	(±)-Licarin A (±)-trans-Dehydrodiisoeugenol	Others	Others
	(±)-Licarin A ((±)-trans-Dehydrodiisoeugenol) is a dihydrobenzofuran neolignan, the resultant of an oxidative coupling reaction of isoeugenol and horseradish peroxidase (HRP) enzyme. (±)-Licarin A shows 100% parasites mortality at 200 μM.
TN4694	Odoratone	Others	Others
	Odoratone shows insecticidal activities, it shows mortality on fourth instar larvae of mosquitoes (Anopheles stephensi) with LC(50) values of 154 ppm. Odoratone exhibits strong antifeedant activity against Pieris brassicae.
TN3549	Burchellin	Antifection	Microbiology/Virology
	Burchellin has larvicidal activity, it can interfer with the development cycle of the mosquito, where its strongest toxic effect is 100% mortality in larvae (L3) at concentrations ¥ 30 ppm. Burchellin and licarin A have activity against Trypanosoma cruzi
T36992	Monocerin
	Monocerin is a fungal metabolite that has been found inF. larvarumand has diverse biological activities.1,2,3It is active against the bacteriaE. coliandB. megaterium, the phytopathogenic fungusM. violaceum, and the algaC. fuscain an agar diffusion assay when used at a concentration of 50 μg/disc.1Monocerin (17.5 μg/ml) induces mortality in adultC. erythrocephala.2It reduces root elongation in pre-germinatedS. halepenseseeds when used at a concentration of 33 ppm.3 1.Zhang, W., Krohn, K., Draeger...
T37690	Phenylpyropene A
	Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 \|1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of ...
T37810	6',7'-Epoxybergamottin
	6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transpo...

天然产物

Cat.No: T15277

Target: Parasite

Homovanillyl alcohol

Cat.No: TN1742

Synonym: 高香草醇,4-羟基-3-甲氧基苯乙醇

Target: TNF, Drug Metabolite

Cat.No: T4S0878

Synonym: 樱黄素,Prunusetin

Target: ERK, Dehydrogenase, NF-κB

Cat.No: T13753

Synonym: (±)-trans-Dehydrodiisoeugenol

Target: Others

Cat.No: TN4694

Target: Others

Cat.No: TN3549

Target: Antifection

Cat.No: T36992

Phenylpyropene A

Cat.No: T37690

6',7'-Epoxybergamottin

Cat.No: T37810

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