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7

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16279	Nebicapone BIA 3-202	Others	Others
	Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor and is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of CO
T35431	(±)-Clopidogrel (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 metabolite via CYP2C19 in the liver enables its anti-aggregating activity. Marketed under the name Plavix , clopidogrel in combination with aspirin has been shown to be beneficial in the prevention of vascu...
T76114	Diaphorase
	Diaphorase 能从厌氧污泥生物中获得。Diaphorase 通过脱硝作用，催化六氢-1,3,5-三硝基-1,3,5-三嗪 (RDX) 的生物转化。
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...
T83786	8-Chloroadenosine-5'-triphosphate sodium 8-chloro ATP
	8-Chloroadenosine-5’-triphosphate（8-chloro ATP）是抗癌剂8-chloro cAMP的活性代谢物，也是核苷酸腺苷5’-三磷酸（ATP）的衍生物。它通过8-chloro cAMP、8-chloroadenosine以及一磷酸和二磷酸中间体形成。应用8-chloro cAMP或8-chloroadenosine后，8-chloro ATP可累积长达12小时，与细胞生长抑制、内源性ATP水平下降以及患者源多发性骨髓瘤细胞中RNA合成减少（但DNA合成不受影响）相关。在1.5至8 mM浓度范围内，它抑制topoisomerase II-α依赖的超螺旋pUC19 DNA放松，同时在1 mM时减少了K562人髓性白血病细胞中topoisomerase II-α催化的ATP水解50%。
T13421	(-)-Cevimeline hydrochloride hemihydrate (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate	ALK	Angiogenesis; Tyrosine Kinase/Adaptors
	(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂，是一种治疗干燥综合征口干症的候选治疗药物。
T35635	rac-trans-4-hydroxy Glyburide
	rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes ...

化合物

Cat.No: T16279

Synonym: BIA 3-202

Target: Others

(±)-Clopidogrel (hydrochloride)

Cat.No: T35431

Cat.No: T76114

Clopidogrel Carboxylic Acid (hydrochloride)

Cat.No: T36112

8-Chloroadenosine-5'-triphosphate sodium

Cat.No: T83786

Synonym: 8-chloro ATP

(-)-Cevimeline hydrochloride hemihydrate

Cat.No: T13421

Synonym: (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate

Target: ALK

rac-trans-4-hydroxy Glyburide

Cat.No: T35635

Cat. No.	Product Name	Target	Signaling Pathways
T41044	Naringinase	Glucosidase	Metabolism
	Naringinase 是一种在自然界中广泛存在的水解酶复合物，具有 α-L-鼠李糖苷酶和 β-D-葡萄糖苷酶的活性，主要用于糖苷的水解。
Fr13756	Isonicotinic acid	Endogenous Metabolite; Drug Metabolite	Metabolism
	Isonicotinic acid 是 Isoniazid 的代谢产物。Isoniazid 通过肼解转化为 Isonicotinic acid。 Isoniazid 向 Isonicotinic acid 的生物转化可以通过细胞色素 P450 酶催化。
T3881	Vaccarin	Integrin; Akt; PERK; AMPK	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Vaccarin 是从王不留行中提取的一种黄酮糖苷，可显著促进伤口愈合以及伤口部位的内皮和成纤维细胞增殖。它通过激活 AMPK 信号通路改善胰岛素抵抗和脂肪变性。
T6S1559	Aurantio-obtusin	Others	Others
	Aurantio-obtusin 是从决明子中分离出的蒽醌类化合物，具有抗炎、抗凝血、抗氧化、抗高血压的活性。它能抑制 IgE 介导的肥大细胞和过敏模型中的过敏反应，具有研究过敏相关疾病的潜力。在大鼠中，它通过内皮细胞 PI3K/AKT/ eNOS 依赖信号通路放松全身动脉，是潜在的新型血管扩张剂。
T83584	(±)-Lavandulol
	(±)-Lavandulol为一不对称的单萜醇，能由米根霉(Rhizopus oryzae)真菌转化为其对应氧化代谢产物。
T83241	7-Hydroxy-TSU-68
	7-Hydroxy-TSU-68为TSU-68的衍生物，该化合物为TSU-68在人类肝微粒体内经生物转化途径形成的代谢产物，其含量标识了TSU-68自身诱导的羟基化程度。
T83320	4'-Demethylpodophyllotoxone
	4'-Demethylpodophyllotoxone为链格孢（Alternaria alternata）S-f6的生物转化中间产物，经4-(2,3,5,6-tetramethylpyrazine-1) (4-TMP)修饰后形成的新化合物，可有效抑制人胃癌细胞系（BGC-823）的生长。

天然产物

Cat.No: T41044

Target: Glucosidase

Isonicotinic acid

Cat.No: Fr13756

Target: Endogenous Metabolite, Drug Metabolite

Cat.No: T3881

Target: Integrin, Akt, PERK, AMPK

Aurantio-obtusin

Cat.No: T6S1559

Target: Others

(±)-Lavandulol

Cat.No: T83584

7-Hydroxy-TSU-68

Cat.No: T83241

4'-Demethylpodophyllotoxone

Cat.No: T83320

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