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46

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4188	SDZ285428 SDZ285-428	P450; Parasite; Antifungal	Metabolism; Microbiology/Virology
	SDZ285428 是一种CYP51抑制剂。
T0849	Pyrimethamine Pirimecidan,RP 4753,Pirimetamin,乙胺嘧啶	DHFR; Antifolate; Parasite	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
	Pyrimethamine (Pirimecidan) 是一种二氢叶酸还原酶的竞争性抑制剂，用作抗疟药。
T2279	Tizoxanide 替唑尼特,Desacetyl-nitazoxanide,TIZ	Antiviral; HIV Protease; Antibacterial; Autophagy	Autophagy; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Tizoxanide (Desacetyl-nitazoxanide) 是 Nitazoxanide 活性代谢物，有抗HIV-1的活性。Nitazoxanide 可抗细菌和多种病毒复制。
T15173	DSM265 PfSPZ	Dehydrogenase; Parasite	Metabolism; Microbiology/Virology
	DSM265 (PfSPZ) 是一种具有抗疟活性的二氢乳清酸脱氢酶抑制剂（IC50：8.9 nM）。DSM265 抑制 Pf3D7 寄生虫的生长可用于治疗和预防疟疾感染。
T1061	Toltrazuril BAY-i 9142,Toltrazurilo,妥曲珠利,Baycox,Toltrazurilum,托曲珠利	Antibiotic; Parasite	Microbiology/Virology
	Toltrazuril (Toltrazurilo) 是一种抗原虫剂，对球虫亚纲有效。
T37072	Nitroxynil 4-Hydroxy-3-iodo-5-nitrobenzonitrile,Trodax,Dovenix	Parasite	Microbiology/Virology
	Nitroxynil (4-Hydroxy-3-iodo-5-nitrobenzonitrile) is an anthelmintic compound that effectively targets parasites in both adult and immature stages. It is extensively employed in investigations pertaining to Fasciola hepatica infection.
T0390	Aklomide 阿克洛胺,Alkomide,2-Chloro-4-nitrobenzamide	Antibiotic; Parasite	Microbiology/Virology
	Aklomide (2-Chloro-4-nitrobenzamide) 用于家禽治疗寄生虫。
T5052	Toltrazuril (sulfone) Toltrazuril sulfone,妥曲珠利砜,Ponazuril	Parasite	Microbiology/Virology
	Toltrazuril sulfone (Ponazuril) 是 Toltrazuril 的代谢物，是一种抗原生动物剂。它是一种三嗪类抗球虫剂，用于预防家禽球虫病。
T7744	Piperaquine tetraphosphate tetrahydrate 4,4'-(1,3-丙烷双-4,1-哌嗪基)双(7-氯喹啉)磷酸盐水合物,四磷酸哌喹四水合物	Parasite	Microbiology/Virology
	Piperaquine tetraphosphate tetrahydrate 是一种双喹啉抗寄生虫剂，可与青蒿素联用研究抗疟。
T20812	Azamethiphos 甲基吡啶磷,唑啶磷	AChE	Neuroscience
	Azamethiphos 是有机磷杀虫剂和神经毒性物质，能够抑制乙酰胆碱酯酶的活性。
T3361	Cambendazole 坎苯达唑,Bonlam,MK-905,Novazole	Others	Others
	Cambendazole (Novazole) 是治疗人类圆线虫病最有效的一种药物。
T0951	Hydroxychloroquine sulfate Acidum iopanoicum,硫酸羟基氯喹,硫酸羟氯喹,HCQ sulfate	DNA; SARS-CoV; TLR; Parasite; Autophagy	Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology
	Hydroxychloroquine sulfate (Acidum iopanoicum) 抑制疟原虫血红素聚合酶。它还可抑制 Toll 样受体 7/9 信号传导和 SARS-CoV-2 感染。
T6607	Nitenpyram 烯啶虫胺,Niterndipoine,烯啶蟲胺,Bestguard,Capstar	AChR	Neuroscience
	Nitenpyram (Capstar) 是一种烟碱型乙酰胆碱受体 (AchR) 激动剂，IC50为 14 nM，用作治疗牲畜和宠物寄生虫的兽药。
T28824	SNX0723 SNX 0723,SNX- 0723	HSP	Cytoskeletal Signaling; Metabolism
	SNX0723 是一种 Hsp90 抑制剂，具有抗疟原虫活性。SNX0723 对 HsHsp90 和 PfHsp90 具有高结合亲和力，Ki 分别为 4.4 和 47 nM。SNX0723 抑制肝期伯氏疟原虫 ANKA 寄生虫，EC50 为 3.3 μM。
T9549	Chiniofon Loretin,Ferron,8-hydroxy-7-iodo-5-quinolinesulfonate,quiniophen,喹碘方	Others	Others
	Chiniofon (Ferron) 是一种卤代 8-羟基喹啉，用作抗阿米巴药物。该类抗阿米巴药物通过抑制肠道共生菌发挥抗阿米巴作用，影响阿米巴痢疾，但对肠外阿米巴寄生虫无作用。
T14780	BRD9185	Dehydrogenase	Metabolism
	BRD9185 is an inhibitor of Dihydroorotate dehydrogenase (DHODH) with an EC50 of 16 nM against multidrug-resistant blood-stage parasites in vitro.
T38729	Melarsonyl dipotassium 美拉胂钾,Melarsonic acid dipotassium
	Melarsonyl dipotassium, also known as melarsonic acid dipotassium, is a potent anthelmintic agent with the ability to effectively inhibit parasites.
T33690	Nitroscanate Lopatol,CGA-23654GS,CGA 23654
	Nitroscanate is an anthelmintic found to be effective in certain strains of parasites in canines.
T70673	NEU617
	NEU617 is an inhibitor of the growth of protozoan parasites, against T. brucei bloodstream proliferation.
T75331	Brilliant green
	Brilliant green, a cationic dye, is utilized for coloring silk and wool. Additionally, it halts the propagation of mold, intestinal parasites, and fungus, proving effective against Gram-positive bacteria [1] [2].
T40087	DSM502
	DSM502, a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor, demonstrates potent nanomolar activity against Plasmodium DHODH and Plasmodium parasites, while not inhibiting mammalian DHODHs.
T71841	MMV085203
	MMV08520 is a novel inhibitor of Plasmodium falciparum, killing both blood- and sexual-stage P. falciparum parasites.
T37639	Toltrazuril sulfoxide
	Toltrazuril sulfoxide, a transient intermediary metabolite of Toltrazuril, undergoes in vivo metabolism to yield the reactive toltrazuril sulfone (TZR-SO2). Toltrazuril functions as an antiprotozoal agent targeting Coccidia parasites[1].
T10328	Anti-parasitic agent 3	Others	Others
	Anti-parasitic agent 3 是一种抗寄生虫剂，对耐药寄生虫具有活性。
T27400	Ganaplacide KAF 156,KAF-156,GNF-156,GNF 156,GNF156,KAF156
	Ganaplacide is an antimalarials with activity against asexual and sexual blood stages and the preerythrocytic liver stages of malarial parasites. KAF156 showed antimalarial activity without evident safety concerns in a small number of adults with uncompli
T39256	MMV674850 MMV674850
	MMV674850 exhibits potency against asexual stage parasites, with IC50 values of 2.7 and 4.5 nM. Furthermore, it demonstrates a preferential affinity for early-stage gametocytes, displaying an IC50 value of 4.5 ± 3.6 nM, compared to late-stage gametocytes with an IC50 value of 28.7 ± 0.2 nM.
T70507	KAI-407
	KAI407 is a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi early dormant liver stage parasites in vitro. KAI407 showed an activity profile similar to that of primaquine (PQ), efficiently killing the earliest stages of the parasites that become either primary hepatic schizonts or hypnozoites (50% inhibitory concentration [IC50] for hypnozoites, KAI407, 0.69 μM, and PQ, 0.84 μM; for developing liver stages, KAI407, 0.64 μM, and PQ, 0.37 μM). KAI407 may represent a new compou...
T28937	Tebuquine WR-228,258,WR 228,258,CI 897,CI897,CI-897
	Tebuquine is an antimalarial agent. Tebuquine is active against P. falciparum in vitro. Tebuquine in vitro shows a chloroquine-like effect, but not in vivo, suggesting that its mode of action in vivo is different from that of chloroquine. Tebuquine has no
T40291	DSM705 DSM705
	DSM705 is a pyrrole-based inhibitor of Dihydroorotate Dehydrogenase (DHODH). It demonstrates high potency in the nanomolar range against Plasmodium DHODH and Plasmodium parasites, while not interfering with mammalian DHODHs. DSM705 shows significant efficacy as an antimalarial compound.
T62362	GNF6702
	GNF6702 是一种选择性的动质体蛋白酶体 (kinetoplastid proteasome) 抑制剂。GNF6702 对利什曼病、南美锥虫病和人类非洲锥虫病小鼠模型中的寄生虫具有清除作用。
T74934	Trypanothione synthetase-IN-3
	Trypanothione synthetase-IN-3是一种针对Trypanothione synthetase (TryS)的非竞争性混合双曲线抑制剂，其Ki值为0.8 μM。该化合物主要用于研究寄生虫，例如L. infantum。
T62550	DSM705 hydrochloride
	DSM705 hydrochloride 是一种有效的抗疟化合物，是一种基于吡咯的二氢乳清酸脱氢酶 (DHODH) 抑制剂。DSM705 hydrochloride 对 PlasmodiumDHODH 和 Plasmodium 寄生虫显示出纳摩尔级作用，不抑制哺乳动物 DHODH。
T79471	Antileishmanial agent-20	Parasite	Microbiology/Virology
	Antileishmanial agent-20 显示对利什曼原虫的选择性抑制作用，其针对L. infantum和L. braziliensis的IC50值分别为2.8 μM 和0.2 μM，适用于寄生虫研究领域。
T35740	FR900098 (sodium salt)
	FR900098 is a derivative of fosmidomycin that has antimalarial activity (IC50s = 170, 170, and 90 nM for HB3, A2, and Dd2 P. falciparum strains, respectively). FR900098 inhibits DOXP reductoisomerase, a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis, in vitro in a dose-dependent manner. FR900098 (>10 mg/kg, i.p.) eradicated P. vinckei parasites within four days in mice.
T61917	TCMDC-125457
	TCMDC-125457 可以有效诱导钙再分布，但抑制血红素结晶的作用较小。TCMDC-125457与青蒿琥酯联合使用时，可以有效治疗紧密同步的青蒿素耐药环期寄生虫。
T35732	Diacetylcercosporin
	Diacetylcercosporin is a perylenequinone produced by Cercospora and Septoria that has diverse biological activities. It inhibits the growth of P. falciparum strains that are sensitive and resistant to chloroquine and L. donovani parasites (IC50 = 3.1 μM) in vitro. Diacetylcercosporin exhibits cytotoxicity against SK-MEL, KB, BT549, and SK-OV-3 human cancer cell lines (IC50s = 4.8-8.7 μM). It is also a phytotoxin that inhibits the growth of lettuce and bentgrass at a concentration of 1.62 mM
T72547	Plm IV inhibitor-2
	Plm IV inhibitor-2 是一种有效的Plm IV 抑制剂，对Plm IV、II 和 I 的IC50分别为24 nM、70 nM 和 0.3 μM。适用于研究Plasmodium 寄生虫引起的疟疾。
T62677	Ganaplacide hydrochloride
	Ganaplacide (KAF156) hydrochloride 是一种首创的、口服具有活力的咪唑哌嗪类抗疟药 (antimalarial)。Ganaplacide hydrochloride 对多种疟原虫（包括耐药寄生虫）有作用。Ganaplacide hydrochloride 对无性和有性血液阶段以及肝脏阶段均具有杀虫效果。
T75536	Koshidacin B
	Koshidacin B为针对疟原虫的环四肽类化合物，其针对抗疟原虫(P. falciparum) FCR3和K1系的IC50值分别为0.89 μM与0.83 μM。此化合物在体内能有效抑制疟原虫，适用于疟疾感染的科学研究。
T79277	Cysteine protease inhibitor-3	Parasite	Microbiology/Virology
	Cysteine protease Inhibitor-3 (Compound 15) 是抗疟作用的半胱氨酸蛋白酶抑制剂，能够有效地抑制 Pf3D7、PfW2、PfFP2 和 PfFP3，其 IC50 分别为 0.74 μM、1.05 μM、3.5 μM 和 4.9 μM。该化合物对药物敏感性和耐药性寄生虫均有效。
T38269	Purfalcamine
	Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...
T12250	NPD-1335	Others	Others
	NPD-1335 (Benzyl alkynamide 37) 一种有效的布氏锥虫磷酸二酯酶 B1 (TbrPDEB1) 抑制剂，具有针对布氏锥虫寄生虫的亚微摩尔活性。 NPD-1335 (Benzyl alkynamide 37) 显示出改善的细胞毒性谱。 NPD-1335 (Benzyl alkynamide 37) 会增加细胞内 cAMP 水平，导致细胞周期和细胞死亡的改变。
T9763	MMV666810
	MMV666810 是一种类似于 MMV390048 的2-氨基吡嗪，5.94 nM 的 MMV666810 对无性寄生虫有效。与早期相比，MMV666810 对晚期配子体细胞的选择性是早期的3.3倍（早期配子体:IC50603 ± 88 nM; 晚期配子体:IC50179 ± 8 nM）。
T75338	Acridine Orange base
	Acridine Orange base是细胞通透性荧光染料，可使生物体（例如细菌、寄生虫、病毒等）呈现亮橙色，而在特定条件下（pH=3.5，Ex=460 nm）则能使人类细胞显现绿色，便于用荧光显微镜检测。此外，Acridine Orange base与dsDNA结合产生绿色荧光（Ex=488, Em=520-524），与ssDNA（Ex=457, Em= 630-644）或ssRNA结合时则显红色荧光（Ex=457, Em=630-644），适用于细胞周期的测定。
T74247	TPE-MI
	TPE-MI（Tetraphenylethene maleimide）在与马来酰亚胺与硫醇反应前不具荧光性。在与游离的半胱氨酸硫醇标记时，其荧光被激活，后者多在球形蛋白质的核心，仅在展开时显露。TPE-MI适用于测量细胞中未折叠蛋白质的负荷，并能在亨廷顿病诱导的多能干细胞模型中监测蛋白质平衡失衡，以及在形成可见聚合体之前，监测转染突变亨廷顿外显子1的细胞的状况。此外，TPE-MI用于检测双氢青蒿素处理后疟疾寄生虫的蛋白质损伤。应暗处储存。
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: T4188

Synonym: SDZ285-428

Target: P450, Parasite, Antifungal

Cat.No: T0849

Synonym: Pirimecidan,RP 4753,Pirimetamin,乙胺嘧啶

Target: DHFR, Antifolate, Parasite

Cat.No: T2279

Synonym: 替唑尼特,Desacetyl-nitazoxanide,TIZ

Target: Antiviral, HIV Protease, Antibacterial, Autophagy

Cat.No: T15173

Synonym: PfSPZ

Target: Dehydrogenase, Parasite

Cat.No: T1061

Synonym: BAY-i 9142,Toltrazurilo,妥曲珠利,Baycox,Toltrazurilum,托曲珠利

Target: Antibiotic, Parasite

Cat.No: T37072

Synonym: 4-Hydroxy-3-iodo-5-nitrobenzonitrile,Trodax,Dovenix

Target: Parasite

Cat.No: T0390

Synonym: 阿克洛胺,Alkomide,2-Chloro-4-nitrobenzamide

Target: Antibiotic, Parasite

Toltrazuril (sulfone)

Cat.No: T5052

Synonym: Toltrazuril sulfone,妥曲珠利砜,Ponazuril

Target: Parasite

Piperaquine tetraphosphate tetrahydrate

Cat.No: T7744

Synonym: 4,4'-(1,3-丙烷双-4,1-哌嗪基)双(7-氯喹啉)磷酸盐水合物,四磷酸哌喹四水合物

Target: Parasite

Cat.No: T20812

Synonym: 甲基吡啶磷,唑啶磷

Target: AChE

Cat.No: T3361

Synonym: 坎苯达唑,Bonlam,MK-905,Novazole

Target: Others

Hydroxychloroquine sulfate

Cat.No: T0951

Synonym: Acidum iopanoicum,硫酸羟基氯喹,硫酸羟氯喹,HCQ sulfate

Target: DNA, SARS-CoV, TLR, Parasite, Autophagy

Cat.No: T6607

Synonym: 烯啶虫胺,Niterndipoine,烯啶蟲胺,Bestguard,Capstar

Target: AChR

Cat.No: T28824

Synonym: SNX 0723,SNX- 0723

Target: HSP

Cat.No: T9549

Synonym: Loretin,Ferron,8-hydroxy-7-iodo-5-quinolinesulfonate,quiniophen,喹碘方

Target: Others

Cat.No: T14780

Target: Dehydrogenase

Melarsonyl dipotassium

Cat.No: T38729

Synonym: 美拉胂钾,Melarsonic acid dipotassium

Cat.No: T33690

Synonym: Lopatol,CGA-23654GS,CGA 23654

Cat.No: T70673

Brilliant green

Cat.No: T75331

Cat.No: T40087

Cat.No: T71841

Toltrazuril sulfoxide

Cat.No: T37639

Anti-parasitic agent 3

Cat.No: T10328

Target: Others

Cat.No: T27400

Synonym: KAF 156,KAF-156,GNF-156,GNF 156,GNF156,KAF156

Cat.No: T39256

Synonym: MMV674850

Cat.No: T70507

Cat.No: T28937

Synonym: WR-228,258,WR 228,258,CI 897,CI897,CI-897

Cat.No: T40291

Synonym: DSM705

Cat.No: T62362

Trypanothione synthetase-IN-3

Cat.No: T74934

DSM705 hydrochloride

Cat.No: T62550

Antileishmanial agent-20

Cat.No: T79471

Target: Parasite

FR900098 (sodium salt)

Cat.No: T35740

Cat.No: T61917

Diacetylcercosporin

Cat.No: T35732

Plm IV inhibitor-2

Cat.No: T72547

Ganaplacide hydrochloride

Cat.No: T62677

Cat.No: T75536

Cysteine protease inhibitor-3

Cat.No: T79277

Target: Parasite

Cat.No: T38269

Cat.No: T12250

Target: Others

Cat.No: T9763

Acridine Orange base

Cat.No: T75338

Cat.No: T74247

Piperazine 2HCl

Cat.No: T65396

Cat. No.	Product Name	Target	Signaling Pathways
TN6730	Epoxyazadiradione	NF-κB	NF-κB
	Epoxyazadiradione 是从印楝果实中得到的柠檬苦素。它能够可逆的、非竞争性的抑制人类、约氏疟原虫、疟原虫的互变异构酶活性。它具有抗疟原虫和人类 MIF 诱导的促炎反应的潜力。
T13539	Allopurinol riboside	Others; Endogenous Metabolite; Parasite; Drug Metabolite	Metabolism; Microbiology/Virology; Others
	Allopurinol riboside 是别嘌醇的代谢产物，具有抗寄生虫作用。 Allopurinol riboside 竞争性抑制嘌呤核苷磷酸化酶对肌苷的作用，Ki 为 277 μM。
TN4883	Quinine sulfate dihydrate 奎宁树	Others	Others
	Quinine sulfate dihydrate 在钾通道阻滞剂中起主要作用。它也被用作抗疟疾、抗胆碱能、抗高血压和降糖药。它抑制线粒体atp 调节的钾通道。它也被用来研究生物结晶血红素，血红素，在疟疾寄生虫的代谢和研究血红素(FP)复合物的毒性。
T75617	Salviandulin E
	Salviandulin E 是一种二萜类化合物，可从墨西哥鼠尾草中分离。Salviandulin E 显示出对 T. b. bruceiGUTat 3.1寄生虫 (parasites) 的抗锥虫体活性，IC50值为 0.72 µg/mL。
TN1442	Betulinic acid methyl ester	Antifection	Microbiology/Virology
	Betulinic acid methyl ester showed antiplasmodial activity against chloroquine-resistant Plasmodium falciparum parasites in vitro.It also inhibited B16 2F2 cell proliferation by induction of apoptosis.
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.
T16381	Okadaic acid	Others	Others
	Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A, and PP3 inhibitor (IC50s: 10-15 nM, 0.5 nM, and 4 nM, respectively). Okadaic acid is extracted from black sponges of the genus Halic

天然产物

Epoxyazadiradione

Cat.No: TN6730

Target: NF-κB

Allopurinol riboside

Cat.No: T13539

Target: Others, Endogenous Metabolite, Parasite, Drug Metabolite

Quinine sulfate dihydrate

Cat.No: TN4883

Synonym: 奎宁树

Target: Others

Cat.No: T75617

Betulinic acid methyl ester

Cat.No: TN1442

Target: Antifection

Cat.No: T13753

Synonym: (±)-trans-Dehydrodiisoeugenol

Target: Others

Cat.No: T16381

Target: Others

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