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69

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T27719	KD-026 SLx 4090,SLx4090,KD026,SLx-4090	CETP	Metabolism
	KD-026 (SLx 4090) 是具有口服活性的、肠细胞特异性的微粒体甘油三酯转移蛋白 (MTP)抑制剂，IC50为 8.0 nM。KD-026 (SLx 4090) 在糖尿病2型中有研究的价值。
T20625	Prochloraz 咪鲜胺,Sporgon,Prelude	Estrogen Receptor/ERR; AhR; Androgen Receptor; Antifungal	Endocrinology/Hormones; Immunology/Inflammation; Metabolism; Microbiology/Virology
	Prochloraz (Prelude) 是咪唑类抗真菌剂。Prochloraz 抑制羊毛甾醇的细胞色素 P450 依赖性 14α-脱甲基作用，由此抑制麦角固醇的生物合成，从而导致真菌细胞膜破裂和细胞死亡。它也是雌激素受体和雄激素受体的拮抗剂，IC50分别为25 μM 和4 μM，并激活芳烃受体，EC50为1μM。
T23861	CAY10526 CAY-10526,BTH,CAY 10526	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂，可抑制 NF-κB 信号通路。
T12856	SC-26196 ALPHA,ALPHA-二苯基-4-[(3-吡啶亚甲基)氨基]-1-吡嗪戊腈	Others	Others
	SC-26196 是一种 Delta6 去饱和酶 (D6D, FADS2) 抑制剂 (在大鼠肝微粒体中，IC50=0.2 µM)，具有口服活性，具有抗炎作用。
T14523	Beauvericin	Others; Acyltransferase	Metabolism; Others
	Beauvericin 是一种镰刀菌霉菌毒素。Beauvericin 在大鼠肝微粒体酶实验中对酰基-CoA：胆固醇酰基转移酶（ACAT）有抑制作用，其 IC50 值为 3 μM。
T28089	mPGES-1 Inhibitor-1	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	mPGES-1 Inhibitor-1 是一种新型的微粒体前列腺素 E 合酶-1（mPGES-1）选择性抑制剂，具有抗炎镇痛活性，可用于研究急性肝损伤。
T16928	SR144528	Cannabinoid Receptor	GPCR/G Protein
	SR144528 是 CB2 受体的拮抗剂 (Ki = 0.6 nM) 并抑制微粒体 ACAT 活性 (IC50 = 3.6 μM)。
T2545	Lomitapide Mesylate 甲磺酸洛美他派,BMS-201038 mesylate,AEGR-733 mesylate	CETP	Metabolism
	Lomitapide Mesylate (BMS-201038 mesylate) 是一种高效MTP 蛋白抑制剂，其体外IC50值为8 nM。
T16865	SCH28080	ATPase; Proton pump	Membrane transporter/Ion channel
	SCH28080 是一种可逆且具有 K+ 竞争性的胃 H+/K+-ATP 酶 (H+/K+-ATPase) 抑制剂，IC50 值为 20 nM (家兔微粒体膜)。SCH28080 在体内是有效的酸分泌抑制剂，具有抗溃疡活性、抗分泌和细胞保护活性。
T27084	Crisdesalazine AAD2004,AAD 2004,AAD-2004	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Crisdesalazine (AAD 2004) 是微粒体前列腺素 E2 合酶 1 (mPGES-1) 的抑制剂。 Crisdesalazine 可减少自噬体形成、轴索病变和运动神经元变性，改善运动功能并延长寿命。
T30506	BMS-212122 UNII-0Z473OO6GB,BMS212122,BMS 212122	CETP	Metabolism
	BMS-212122 (UNII-0Z473OO6GB) 是一种有效的微粒体甘油三酯转移蛋白(MTP )抑制剂，在动物实验中显示出降血脂作用。BMS-212122 显著减少动脉粥样硬化斑块中的脂质含量和单核细胞衍生(CD68+)细胞。
T21738	PF-9184	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂，IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。
T31992	Granotapide	CETP	Metabolism
	Granotapide 是一种微粒体甘油三酯转移蛋白（MTP）抑制剂，治疗和而预防动脉硬化，冠状动脉疾病，代谢综合征，肥胖，糖尿病，糖尿病前期和高血压。
T37825	CAY10434	P450	Metabolism
	CAY10434是一种有作用的 CYP4A 羟化酶 (CYP4A hydroxylase) 抑制剂，在人肾微粒体测试中的 IC50值为8.8 nM。CAY 10434 在改善血管紧张素 II 的收缩过程中 Emax 为 6764 mg。
T15006	Dirlotapide CP742033,Slentrol	Others; CETP	Metabolism; Others
	Dirlotapide (CP742033) 是一种肠道选择性微粒体甘油三酯转移蛋白(MTP)抑制剂。它可以减轻糖尿病狗的体重。Dirlotapide 以剂量依赖性方式减少食物摄入量，可能是通过增加肽YY 释放到循环中。
T1055	Ifosfamide NSC109724,Isophosphamide,异环磷酰胺	DNA Alkylator/Crosslinker; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ifosfamide (NSC-109724) 是一种烷化剂，具有抗肿瘤活性。它烷基化并形成 DNA 交联，从而防止 DNA 链分离和 DNA 复制。它是一种前药，必须通过肝微粒体酶的羟基化来激活。
T6267	Lomitapide AEGR-733,洛美他派,BMS-201038	CETP	Metabolism
	Lomitapide (AEGR-733) 是一种高效的微粒体甘油三酯转移蛋白(MTP)抑制剂，体内试验的IC50值为8 nM。
T9394	CHIKV-IN-2	Dehydrogenase	Metabolism
	CHIKV-IN-2 基孔肯雅病毒的选择性抑制剂，具有强大的细胞抗病毒活性 (EC90=270 nM) 以及能够改善肝微粒体稳定性。它能够抑制细胞靶二氢乳清酸脱氢酶的活性。
T72470	Estrone O-sulfamate Estrone 3-O-sulfamate	Others	Others
	Estrone O-sulfamate (Estrone 3-O-sulfamate) 是一种高效的的类固醇硫酸酯酶 (STS) 抑制剂。Estrone O-sulfamate 是一种胎盘微粒体抑制剂 (P.M.) ，IC50 值分别为 18 nM。Estrone O-sulfamate 在 MCF-7 细胞中对 STS 显示出抑制作用，IC50 值分别为 0.83 nM。Estrone O-sulfamate 可用于研究癌症。
T35610	2,5-dimethyl Celecoxib	Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor	Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
	2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂，mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T6412	CVT-12012	Stearoyl-CoA Desaturase (SCD)	Metabolism
	CVT-12012 是口服具有活性的硬脂酰-CoA 去饱和酶抑制剂，能够抑制大鼠微粒体和人 HEPG2 的活性，它们的IC50值分别为 38 nM，6.1 nM。
T12765	RPR107393 free base	Others	Others
	RPR107393 free base is a selective inhibitor of squalene synthase(rat liver microsomal squalene synthase, with an IC50 of 0.8 nM).
T33110	M 79193 M79193,M-79193
	M 79193 induces total hepatic microsomal cytochrome P-450.
T25440	FR20 FR-20,FR 20
	FR20 is a human microsomal prostaglandin synthase 1 (mPGES 1) inhibitor.
T24223	JTT 130 JTT-130,JTT130
	JTT 130 is an agent of hypolipidemic. It inhibits microsomal triglyceride transfer protein.
T13418	CP-319340(free base)	Others	Others
	CP-319340 free base is a inhibitor of microsomal triglyceride transfer protein (MTP) .
T15570	Implitapide 英普他派,AEGR 427	CETP	Metabolism
	Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).
T10504	Implitapide Racemate	Others	Others
	Implitapide Racemate is the racemate of Implitapide. Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).
T12100	mPGES1-IN-3	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	mPGES1-IN-3 is a potent and selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) .
T23596	A-933548 A933548,A 933548
	A-933548 is a potent Calpain inhibitor. A-933548 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.
T35005	Usistapide R-256918,JNJ-16269110,JNJ16269110,R256918,JNJ 16269110,R 256918
	UsISpide(JNJ-16269110 R256918) is an inhibitor of microsomal triglyceride transfer protein (MTTP) under development for the treatment of obesity and type 2 diabetes.
T68375	KD026-metabolite
	KD026-metabolite, is a metabolite of KD-026. KD026, also known as SLx-4090, is a microsomal triglyceride transfer protein (MTTP) inhibitor potentially for the treatment of type 2 diabetes.
T16158	PF-02575799	Adenosine Receptor	GPCR/G Protein; Neuroscience
	PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).
T23598	A-953227 A 953227,A953227
	A-953227 is a highly effective and selective inhibitor of calpain. A-953227 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.
T16504	PF-4693627	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
T39000	Zaloglanstat GRC-27864,ISC-27864
	Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases.
T38666	CP-346086 dihydrate
	CP-346086 dihydrate is a potent and orally active inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM for both human and rodent MTP. This compound effectively lowers plasma cholesterol and triglyceride levels in vivo.
T14564	BI-4924	Others	Others
	BI-4924 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH) (IC50=3 nM). It has excellent Microsomal and hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis at 72 h ( IC50: 2200 nM).
T38143	Elaidamide
	Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-150...
T37840	20-hydroxy Prostaglandin F2α 20-hydroxy Prostaglandin F2α
	20-hydroxy Prostaglandin F2α (20-hydroxy PGF2α) is the ω-oxidation product of PGF2α. Cultured type II alveolar cells from pregnant rabbits metabolize exogenous PGF2α via microsomal cytochrome P450 ω-oxidation, producing 20-hydroxy PGF2α and its 15-hydroxy PGDH metabolites. Cells from male rabbits exhibit only the 15-hydroxy PGDH pathway.
T39303	CP-346086
	CP-346086 is a highly potent and orally bioavailable inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM against both human and rodent MTP. This compound effectively reduces plasma levels of cholesterol and triglycerides when administered in vivo.
T62850	IRAK4-IN-13
	IRAK4-IN-13 (compound 21) 是一种选择性的、有效的 IRAK4 抑制剂 (IC50: 0.6 nM)。IRAK4-IN-13 具有高代谢清除率，人肝微粒体 (HLM) 固有清除率为 96 μL/min/mg。
T74520	TD-802
	TD-802 (Compound 33c) 是一种雄激素受体 (androgen receptor)PROTAC 降解剂。TD-802 具有良好的体内抗肿瘤效果，能被用于转移性去势抵抗性前列腺癌的研究。
T60346	PDE4-IN-10
	PDE4-IN-10 (compound 7a) 是一种有效的PDE4抑制剂，其对PDE4B 的IC50值为 7.01 μM。PDE4-IN-10 表现出选择性，微粒体稳定性，对TNF-α有抑制作用，并且在体外无明显毒性。
T61690	mEH-IN-1
	mEH-IN-1 (Compound 62) is a potent inhibitor of microsomal epoxide hydrolase (mEH), with an IC50 value of 2.2 nM. mEH is an α/β-fold hydrolase enzyme that is widely expressed in various mammalian tissues, responsible for the hydrolysis of a diverse range of epoxide-containing molecules. This enzyme is primarily localized in the endoplasmic reticulum (ER) of eukaryotic cells. Research involving mEH-IN-1 can contribute to the understanding of preeclampsia, hypercholanemia, and cancer [1].
T61504	PKM2 activator 3
	PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.)
T79440	DprE1-IN-5
	DprE1-IN-5（Compound 10）为一种DprE1抑制剂，对Mtb H37Rv菌株表现出抗结核活性（MIC: 4 μM），并对耐药菌株具有抗分枝杆菌效果，同时展现出较高的微粒体稳定性。
T75067	Antimalarial agent 19	Parasite	Microbiology/Virology
	Antimalarial agent 19（compound 6e）是一种活性抗疟疾化合物，对K1型恶性疟原虫和伯氏疟原虫展现出较强的抑制效果，其EC50值分别为0.3 µM和15.3 µM。相较于γ-肝硫平，该化合物具有更好的水溶性、肠道渗透性以及微粒体稳定性。
T79533	PDE5-IN-10
	PDE5-IN-10 (compound 4b)，一有效PDE5抑制剂，IC50值为20 nM。该化合物体外微粒体稳定性增强（t1/2= 44.6 分钟），在长期增强恢复方面效果显著，适用于阿尔茨海默病（AD）研究。

化合物

Cat.No: T27719

Synonym: SLx 4090,SLx4090,KD026,SLx-4090

Target: CETP

Cat.No: T20625

Synonym: 咪鲜胺,Sporgon,Prelude

Target: Estrogen Receptor/ERR, AhR, Androgen Receptor, Antifungal

Cat.No: T23861

Synonym: CAY-10526,BTH,CAY 10526

Target: Prostaglandin Receptor

Cat.No: T12856

Synonym: ALPHA,ALPHA-二苯基-4-[(3-吡啶亚甲基)氨基]-1-吡嗪戊腈

Target: Others

Cat.No: T14523

Target: Others, Acyltransferase

mPGES-1 Inhibitor-1

Cat.No: T28089

Target: Prostaglandin Receptor

Cat.No: T16928

Target: Cannabinoid Receptor

Lomitapide Mesylate

Cat.No: T2545

Synonym: 甲磺酸洛美他派,BMS-201038 mesylate,AEGR-733 mesylate

Target: CETP

Cat.No: T16865

Target: ATPase, Proton pump

Cat.No: T27084

Synonym: AAD2004,AAD 2004,AAD-2004

Target: Prostaglandin Receptor

Cat.No: T30506

Synonym: UNII-0Z473OO6GB,BMS212122,BMS 212122

Target: CETP

Cat.No: T21738

Target: Prostaglandin Receptor

Cat.No: T31992

Target: CETP

Cat.No: T37825

Target: P450

Cat.No: T15006

Synonym: CP742033,Slentrol

Target: Others, CETP

Cat.No: T1055

Synonym: NSC109724,Isophosphamide,异环磷酰胺

Target: DNA Alkylator/Crosslinker, DNA/RNA Synthesis

Cat.No: T6267

Synonym: AEGR-733,洛美他派,BMS-201038

Target: CETP

Cat.No: T9394

Target: Dehydrogenase

Estrone O-sulfamate

Cat.No: T72470

Synonym: Estrone 3-O-sulfamate

Target: Others

2,5-dimethyl Celecoxib

Cat.No: T35610

Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor

Cat.No: T36696

Cat.No: T6412

Target: Stearoyl-CoA Desaturase (SCD)

RPR107393 free base

Cat.No: T12765

Target: Others

Cat.No: T33110

Synonym: M79193,M-79193

Cat.No: T25440

Synonym: FR-20,FR 20

Cat.No: T24223

Synonym: JTT-130,JTT130

CP-319340(free base)

Cat.No: T13418

Target: Others

Cat.No: T15570

Synonym: 英普他派,AEGR 427

Target: CETP

Implitapide Racemate

Cat.No: T10504

Target: Others

Cat.No: T12100

Target: Prostaglandin Receptor

Cat.No: T23596

Synonym: A933548,A 933548

Cat.No: T35005

Synonym: R-256918,JNJ-16269110,JNJ16269110,R256918,JNJ 16269110,R 256918

KD026-metabolite

Cat.No: T68375

Cat.No: T16158

Target: Adenosine Receptor

Cat.No: T23598

Synonym: A 953227,A953227

Cat.No: T16504

Target: Prostaglandin Receptor

Cat.No: T39000

Synonym: GRC-27864,ISC-27864

CP-346086 dihydrate

Cat.No: T38666

Cat.No: T14564

Target: Others

Cat.No: T38143

20-hydroxy Prostaglandin F2α

Cat.No: T37840

Synonym: 20-hydroxy Prostaglandin F2α

Cat.No: T39303

Cat.No: T62850

Cat.No: T74520

Cat.No: T60346

Cat.No: T61690

PKM2 activator 3

Cat.No: T61504

Cat.No: T79440

Antimalarial agent 19

Cat.No: T75067

Target: Parasite

Cat.No: T79533

Cat. No.	Product Name	Target	Signaling Pathways
T5261	(E)-Oct-2-enoic acid trans-2-Octenoic acid,2-Octenoate,2-辛烯酸,2-Octenoic acid	Others; Endogenous Metabolite	Metabolism; Others
	(E)-Oct-2-enoic acid (2-Octenoate) 是内源性代谢产物的一种。
TN1818	Kaempferol 3-O-β-D-glucuronide Kaempferol-3-O-glucuronide,Kaempferol-3-beta-O-glucuronide,山奈酚葡萄糖醛酸苷,Kaempferol-3-glucuronide	IL Receptor	Immunology/Inflammation
	Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-beta-O-glucuronide) 具有抗氧化活性。类黄酮葡糖苷酸可以被来自各种人体细胞的微粒体 α2-葡糖苷酸酶解偶联。
TN1674	Garcinone D 伽升沃 D	Reactive Oxygen Species; Nrf2; STAT	Immunology/Inflammation; JAK/STAT signaling; Metabolism; NF-κB; Stem Cells
	Garcinone D 是来自山竹的一种呫吨酮，可促进 C17.2 神经干细胞的增殖。它以浓度和时间依赖的方式增加磷酸化信号转导和转录激活因子 3 (p-STAT3)、Cyclin D1 和核因子红细胞 2 相关因子 (Nrf2)、以及血红素加氧酶-1 (HO-1) 的蛋白质水平。
TN3069	4beta-Carboxy-19-nortotarol	NADPH-oxidase	Immunology/Inflammation
	4 beta-Carboxy-19-nortotarol can inhibit microsomal lipid peroxidation induced by Fe(III)-ADP/NADPH and mitochondrial lipid peroxidation induced by Fe(III)-ADP/ NADH, it inhibits linoleic acid autoxidation but not generation of superoxide anion.
T37972	12-OxoETE
	12-OxoETE is synthesized by human platelets and Aplysia nervous tissue after incubation with arachidonic acid. Microsomal fractions of various tissues will reduce 12-oxoETE to 12(S)-HETE or a mixture of 12(S)- and 12(R)-HETE. 12-OxoETE induces a rapid, dose dependent increase of cytoplasmic free calcium via a leukotriene B4 receptor or a common activation sequence.

天然产物

(E)-Oct-2-enoic acid

Cat.No: T5261

Synonym: trans-2-Octenoic acid,2-Octenoate,2-辛烯酸,2-Octenoic acid

Target: Others, Endogenous Metabolite

Kaempferol 3-O-β-D-glucuronide

Cat.No: TN1818

Synonym: Kaempferol-3-O-glucuronide,Kaempferol-3-beta-O-glucuronide,山奈酚葡萄糖醛酸苷,Kaempferol-3-glucuronide

Target: IL Receptor

Cat.No: TN1674

Synonym: 伽升沃 D

Target: Reactive Oxygen Species, Nrf2, STAT

4beta-Carboxy-19-nortotarol

Cat.No: TN3069

Target: NADPH-oxidase

Cat.No: T37972

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