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16

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4118	SB 271046 hydrochloride SB 271046A	5-HT Receptor	GPCR/G Protein; Neuroscience
	SB 271046 hydrochloride (SB 271046A) 是高效、选择性和具有口服活性的5-HT6受体拮抗剂，对大鼠、猪和人的pKi 分别为 9.02、8.55 和 8.81。它增加额叶皮层中的细胞外天冬氨酸和谷氨酸并表现出抗惊厥活性，EC50为 0.16 μM。它对 5-HT6 受体、结合位点和离子通道的选择性超过 200 倍。
T1579	Mestranol Devocin,Norquen,美雌醇,Menophase	Estrogen Receptor/ERR; Estrogen/progestogen Receptor	Endocrinology/Hormones
	Mestranol (Devocin) 是一种雌激素受体激动剂，是一种非活性的前药，在转化为炔雌醇时具有生物活性。动物实验中，它可以与黄体酮联合使用，它可用于更年期激素或月经紊乱的研究。
T12678	(Rac)-Telmesteine 替美司坦,3-(Ethoxycarbonyl)thiazolidine-4-carboxylic acid,3-ethoxycarbonyl-1,3-thiazolidine-4-carboxylic acid,3,4-Thiazolidinedicarboxylic Acid 3-Ethyl Ester	Protease	Proteases/Proteasome
	(Rac)-Telmesteine (3,4-Thiazolidinedicarboxylic Acid 3-Ethyl Ester) 是蛋白酶抑制剂，可用作含蛋白酶的洗涤剂和清洗剂中的酶稳定剂。
T71708	Minamestane	Aromatase	Endocrinology/Hormones
	Minamestane 是一种新型不可逆芳香化酶抑制剂。Minamestane 引起人胎盘芳香化酶的时间依赖性抑制，半衰期为4分钟，K 为59nM。Minamestane 具有抗肿瘤活性。
T1536	Promestriene 3-propyl ethyl,舒经劳,17B-methyl estradiol,Promestriano	Estrogen/progestogen Receptor	Endocrinology/Hormones
	Promestriene (3-propyl ethyl) 是局部有效的雌激素，是合成的雌二醇二乙醚。它对阴道萎缩有作用，但吸收量小。
T1587	Exemestane EXE,依西美坦,FCE 24304,PNU155971	Aromatase	Endocrinology/Hormones
	Exemestane (EXE) 是一种选择性的、具有口服活性的、不可逆的甾体芳香酶抑制剂，能够作用于人胎盘芳香酶 (IC50:30 nM) 和大鼠卵巢芳香酶 (IC50:40 nM)，可用于研究激素依赖性乳腺癌。
T29886	Almestrone BA-38372,BA 38372,Ciba-38372,BA38372,Ciba 38372
	Almestrone (developmental code names Ba 38372, Ciba 38372), also known as 7α-methylestrone, is a synthetic, steroidal estrogen which was synthesized in 1967 but was never marketed. It is used as a precursor in the synthesis of several highly active steroi
T24012	Domesticine, (-)- L-Domesticine
	Domesticine, (-)- is an antagonist of alpha-1D-adrenoceptor.
T20956	Telmesteine
	Telmesteine is a mucolitic drug.
T28942	Telomestatin SOT 095,GM95,(R)-Telomestatin,GM 95,GM-95
	Telomestatin is an inhibitor of the telomerase, it induces the formation of basket-type G-quadruplex (G4) structures from hybrid-type G-quadruplexes in the telomeric region.
T33032	Lynestrenol mixture with mestranol
	Lynestrenol mixture with mestranol is a bioactive chemical.
T35676	17β-hydroxy Exemestane
	17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = ...
T35772	Emestrin
	Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.1,2,3,4,5 It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg/ml, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestr...
T68720	Plomestane
	Plomestane is a selective inhibitor of aromatization in human breast tissue and may provide a mechanism for controlling estrogen responsive processes.
T31485	Dimestrol
	Dimestrol can induce DNA damage.
T68775	Etamestrol
	Etamestrol is a synthetic, steroidal estrogen described as an ovulation inhibitor or hormonal contraceptive

化合物

SB 271046 hydrochloride

Cat.No: T4118

Synonym: SB 271046A

Target: 5-HT Receptor

Cat.No: T1579

Synonym: Devocin,Norquen,美雌醇,Menophase

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

(Rac)-Telmesteine

Cat.No: T12678

Synonym: 替美司坦,3-(Ethoxycarbonyl)thiazolidine-4-carboxylic acid,3-ethoxycarbonyl-1,3-thiazolidine-4-carboxylic acid,3,4-Thiazolidinedicarboxylic Acid 3-Ethyl Ester

Target: Protease

Cat.No: T71708

Target: Aromatase

Cat.No: T1536

Synonym: 3-propyl ethyl,舒经劳,17B-methyl estradiol,Promestriano

Target: Estrogen/progestogen Receptor

Cat.No: T1587

Synonym: EXE,依西美坦,FCE 24304,PNU155971

Target: Aromatase

Cat.No: T29886

Synonym: BA-38372,BA 38372,Ciba-38372,BA38372,Ciba 38372

Domesticine, (-)-

Cat.No: T24012

Synonym: L-Domesticine

Cat.No: T20956

Cat.No: T28942

Synonym: SOT 095,GM95,(R)-Telomestatin,GM 95,GM-95

Lynestrenol mixture with mestranol

Cat.No: T33032

17β-hydroxy Exemestane

Cat.No: T35676

Cat.No: T35772

Cat.No: T68720

Cat.No: T31485

Cat.No: T68775

Cat. No.	Product Name	Target	Signaling Pathways
T12564	Prudomestin 3,5,7-Trihydroxy-4',8-dimethoxyflavone,3,5,7-三羟基-8,4'-二甲氧基黄酮	Xanthine Oxidase	Metabolism
	Prudomestin (3,5,7-Trihydroxy-4',8-dimethoxyflavone) 是一种分离自 Prunus domestica 心材中，具有很强的黄嘌呤氧化酶(XO)抑制活性(IC50≈6 µM)。
TQ0295	Coumestrol 拟雌内酯,考迈斯托醇	Estrogen Receptor/ERR	Endocrinology/Hormones
	Coumestrol 是一种大豆产品中存在的植物雌激素。它抑制ES2细胞增殖的IC50值为50 μM。它可用于癌症，神经障碍和自身免疫疾病的研究。
TN5883	4'-O-Methylcoumestrol 4'-O-甲基香豆雌酚,9-O-Methylcoumestrol
	4'-O-Methylcoumestrol is a natural product from Glycyrrhiza pallidiflora Maxim.
T82220	Hedysarimcoumestan B
	Hedysarimcoumestan B为从Hedysarum multijugum根部提取的天然化合物。

天然产物

Cat.No: T12564

Synonym: 3,5,7-Trihydroxy-4',8-dimethoxyflavone,3,5,7-三羟基-8,4'-二甲氧基黄酮

Target: Xanthine Oxidase

Cat.No: TQ0295

Synonym: 拟雌内酯,考迈斯托醇

Target: Estrogen Receptor/ERR

4'-O-Methylcoumestrol

Cat.No: TN5883

Synonym: 4'-O-甲基香豆雌酚,9-O-Methylcoumestrol

Hedysarimcoumestan B

Cat.No: T82220

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