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14

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2112	Fexinidazole 非昔硝唑,HOE 239	Others; Parasite	Microbiology/Virology; Others
	Fexinidazole (HOE 239) 是具有口服活性的硝基咪唑抗锥虫药物。它显示出对布鲁氏杆菌亚种和菌株的杀锥虫活性，IC50值为 0.7-3.3 μM (0.2-0.9 μg/ml)。它具有用于因感染布鲁氏菌引起的人类昏睡病的潜力。
T1110	Meclizine dihydrochloride Meclozine dihydrochloride,NSC28728,Meclizine 2HCl,盐酸美克洛嗪	Apoptosis; Histamine Receptor	Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Meclizine dihydrochloride (NSC28728) 是一种组胺 H1 拮抗剂，用于治疗妊娠期间的晕动病、眩晕和恶心以及放射病。它是小鼠组成型雄甾烷受体激动剂，是人 CAR 的反向激动剂。它可透过血脑屏障，可用于多聚谷氨酰胺毒性障碍方面的研究。
T3282	Alimemazine hemitartrate Alimemazine Tartrate,Methylpromazine Tartrate,酒石酸异丁嗪,Trimeprazine tartrate,Trimeprazine hemitartrate	Others	Others
	Alimemazine hemitartrate (Trimeprazine hemitartrate) 是血凝素 (HA)-受体的拮抗剂，也是一种吩噻嗪衍生物，常用作止痒剂。
T21281	Zolamide CL 5343,Tio-urasin,5-Amino-TDSNH2,乙酰唑胺杂质D	Others	Others
	Zolamide (CL 5343) 可用于预防高原反应和减轻症状。
T60351	Acetazolamide sodium OT-302 sodium	Carbonic Anhydrase	Metabolism
	Acetazolamide sodium (OT-302 sodium) 是一种高效的碳酸酐酶 (CA)IX抑制剂，具有利尿、抗淋球菌和降压活性，可用于癫痫、青光眼、水肿和高原反应等适应症。
T40652	Meclizine Meclozine	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Meclizine (Meclozine) (Meclozine)具有抗组胺作用，可可逆地抑制组胺与H1受体的相互作用。Meclizine 是哌嗪类H1拮抗剂的一个成员。Meclizine 是一种有效的抗运动病剂。Meclizine 可通过血脑屏障。Meclizine 是小鼠组成型雄烷受体(CAR)的激动剂配体，也是人CAR 的反向激动剂。Meclizine 可用于polyQ 毒性疾病的研究，如亨廷顿病。
T33278	Melarsoprol Melarsoprolum,RP 3854,RP3854,RP-3854
	Melarsoprol, an organoarsenic compound, can be used to treat trypanosomiasis (human African sleeping sickness).
T28011	Megazol CL 64855,CL-64855,CL64855
	Megazol is a nitroimidazole based drug that cures some protozoan infections. A study of nitroimidazoles found the drug extremely effective against T. cruzi and T. brucei which cause Chagas disease and African sleeping sickness, respectively.
T71685	NEU-1953
	NEU-1953 is a potential candidate for sleeping sickness.
T69012	Cinnarizine clofibrate
	Cinnarizine clofibrate is a calcium channel protein inhibitor as well as an antihistamine channel blocker. The compound is a drug derivative of piperazine. Cinnarizine is used for the control of vomiting due to motion sickness. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus
T61832	hCAI/II-IN-3
	hCAI/II-IN-3 (compound 5b) is a highly effective dual inhibitor of hCA I/II enzymes. It exhibits Ki values of 51.25, 13.15, and 42.18 nM for hCA I, hCA II, and hCA Ⅸ, respectively. hCAI/II-IN-3 demonstrates anti-hypoxic properties against acute mountain sickness (AMS) and exhibits low cellular activity [1].
T61635	hCAI/II-IN-4
	hCAI/II-IN-4 (compound 6d) is a powerful inhibitor of both hCA I and hCA II enzymes, with Ki values of 16.95 nM and 15.22 nM, respectively. It demonstrates inhibitory activity against hCA IX with a Ki value of 27.04 nM. Additionally, hCAI/II-IN-4 exhibits anti-hypoxia properties while maintaining low toxicity. This compound is suitable for investigating acute mountain sickness (AMS) in research studies [1].
T61282	hCAI/II-IN-2
	hCAI/II-IN-2 (compound 2b) is a highly effective dual inhibitor of human carbonic anhydrase I and II (hCA I/II), with Ki values of 40.97 nM, 15.15 nM, and 61.88 nM for hCA I, hCA II, and hCA IX, respectively. With its anti-hypoxic properties, hCAI/II-IN-2 demonstrates activity against acute mountain sickness (AMS). Furthermore, this compound exhibits low cellular activity [1].
T35904	O-11
	O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killingTrypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50of less than 1 μM in a cell culture assay.1,2The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface gl...

化合物

Cat.No: T2112

Synonym: 非昔硝唑,HOE 239

Target: Others, Parasite

Meclizine dihydrochloride

Cat.No: T1110

Synonym: Meclozine dihydrochloride,NSC28728,Meclizine 2HCl,盐酸美克洛嗪

Target: Apoptosis, Histamine Receptor

Alimemazine hemitartrate

Cat.No: T3282

Synonym: Alimemazine Tartrate,Methylpromazine Tartrate,酒石酸异丁嗪,Trimeprazine tartrate,Trimeprazine hemitartrate

Target: Others

Cat.No: T21281

Synonym: CL 5343,Tio-urasin,5-Amino-TDSNH2,乙酰唑胺杂质D

Target: Others

Acetazolamide sodium

Cat.No: T60351

Synonym: OT-302 sodium

Target: Carbonic Anhydrase

Cat.No: T40652

Synonym: Meclozine

Target: Histamine Receptor

Cat.No: T33278

Synonym: Melarsoprolum,RP 3854,RP3854,RP-3854

Cat.No: T28011

Synonym: CL 64855,CL-64855,CL64855

Cat.No: T71685

Cinnarizine clofibrate

Cat.No: T69012

Cat.No: T61832

Cat.No: T61635

Cat.No: T61282

Cat.No: T35904

Cat. No.	Product Name	Target	Signaling Pathways
TN3497	Benzylamine hydrochloride	Others	Others
	Benzylamine hydrochloride 由卞胺和盐酸制的，可用于治疗晕动病和蛔虫病，具有止吐特性。
T7641	5-Hydroxytryptophol 5-羟基色醇	Endogenous Metabolite	Metabolism
	5-Hydroxytryptophol 是哺乳动物 5-羟色胺的代谢物，它被用作饮酒的生物标志物并可以导致昏睡病。
T3O2784	Vitamin B6 维生素B6	Others	Others
	Vitamin B6 是人体某些辅酶的成分，参与多种代谢反应，特别是与氨基酸代谢有关。维生素B6在防治妊娠和放射病呕吐中的临床应用。

天然产物

Benzylamine hydrochloride

Cat.No: TN3497

Target: Others

5-Hydroxytryptophol

Cat.No: T7641

Synonym: 5-羟基色醇

Target: Endogenous Metabolite

Cat.No: T3O2784

Synonym: 维生素B6

Target: Others

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