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27

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22708	Darglitazone CP-86325	PPAR	DNA Damage/DNA Repair; Metabolism
	Darglitazone (CP-86325) 是一种噻唑烷二酮，是口服有效的PPAR-γ选择性激动剂。Darglitazone 可以有效控制血糖和脂质代谢，在 II 型糖尿病中有研究价值。
T1461	Candesartan CV 11974,坎地沙坦	RAAS	Endocrinology/Hormones
	Candesartan (CV 11974) 是一种血管紧张素II 受体拮抗剂(IC50:0.26 nM)。
TQ0156	GW1929	PPAR	DNA Damage/DNA Repair; Metabolism
	GW1929是PPAR-γ有效激动剂，对人PPAR-γ的pKi 为8.84。对人和鼠的pEC50分别为8.56 和 8.27。
T15575	Indeglitazar PPM 204	PPAR	DNA Damage/DNA Repair; Metabolism
	Indeglitazar (PPM 204) 是 PPAR 的泛激动剂，包括亚型 alpha (α)、delta (δ) 和 gamma (γ)。
T27303	Farglitazar GI-262570,GI 262570,GI262570
	Farglitazar is a PPAR-γ agonist. GI262570 stimulates the ENaC and Na,K-ATPase system resulting in the increasing of water and sodium reabsorption in distal nephron.
T21587	Muraglitazar Pargluva,BMS-298585	PPAR	DNA Damage/DNA Repair; Metabolism
	Muraglitazar (BMS-298585) 是一种 PPAR α/γ的双激动剂，用于治疗2型糖尿病及相关血脂异常。Muraglitazar 对人 PPARα (EC50 = 320 nM)和 PPARγ(EC50 = 110 nM)具有较强的体外活性。
T28589	Ro 41-5253 Ro-41-5253,Ro 415253	Apoptosis; Retinoid Receptor	Apoptosis; Metabolism
	Ro 41-5253 是一种具有口服活性的 RARα 拮抗剂，是过氧化物酶体增殖物激活受体（PPAR）-γ 的配体和部分激动剂，具有抗肿瘤活性，抑制 MCF-7 和 ZR-75.1 雌激素受体阳性乳腺癌细胞的增殖并诱导细胞凋亡。
T8780	AMG131 INT-131,AMG-131,CHS 131	PPAR	DNA Damage/DNA Repair; Metabolism
	AMG131 (CHS 131) 是一种新型非噻唑烷二酮(TZD) 选择性过氧化物酶体增殖物激活受体 (PPAR) γ 调节剂，可用于治疗 2 型糖尿病。
T16739	RG-12525 NID 525	Leukotriene Receptor; PPAR	DNA Damage/DNA Repair; GPCR/G Protein; Metabolism
	RG-12525（NID 525）是一种可口服且具有选择性和竞争性的白三烯 D （LTD）拮抗剂，对 LTC4，LTD4 和 LTE4 诱导的豚鼠薄壁带收缩有抑制作用，IC50 值分别为 2.6 nM，2.5 nM 和 7 nM。RG-12525 对 CYP3A4 有抑制作用， Ki 值为 0.5 µM。RG-12525 是一种新型高效的 PPAR-γ 激动剂（IC50 值约为 60 nM），具有物种特异性，可用于研究哮喘。
T7621	6-Thioinosine 6-Mercaptopurine riboside,6-疏基嘌呤核苷,6TI	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	6-Thioinosine (6TI) 是一种嘌呤抗代谢物，是抗脂肪形成剂，能降低PPAR γ和C/EBPα及其目标基因 aP2、CD36、LPL 和 LXRα 的 mRNA 水平。
T16022	Arhalofenate JNJ 39659100,芳卤芬酯,4-氯-ALPHA-[3-(三氟甲基)苯氧基]苯乙酸 2-(乙酰基氨基)乙酯,MBX 102	PPAR	DNA Damage/DNA Repair; Metabolism
	Arhalofenate (JNJ 39659100) 是一种选择性的(PPAR)-γ部分激动剂，用于研究 2 型糖尿病。
T17044	Tesaglitazar	PPAR	DNA Damage/DNA Repair; Metabolism
	Tesaglitazar 是一种有效且具有选择性的过氧化物 PPAR α / γ受体双重激动剂，对 PPARγ的亲和力比 PPARα更有效，对大鼠PPARα和人PPARα的EC50分别为13.4 μM 和3.6 μM,对大鼠PPARγ和人类 PPARγ的EC50都是0.2 μM。Tesaglitazar 诱导大鼠皮下组织间质间充质细胞DNA 合成和纤维肉瘤形成。
T10506	PPAR agonist 1	PPAR	DNA Damage/DNA Repair; Metabolism
	PPAR agonist 1 is an agonist of PPAR α/γ, used for reducing blood glucose, lipid levels, reducing body weight, and lowering cholesterol.
T27513	GW7845 GW 7845,GW-7845
	GW7845, an L-tyrosine derivative, is a PPAR-γ agonist.
T28542	Rivoglitazone HCl CI-1037,CI1037,CS011,CS-011,CI 1037
	Rivoglitazone, also known as CI-1037; CS-011; DE-101; R-119702; Rivo, is a peroxisome proliferator-activated receptor γ agonist (PARPγ agonist) potentially for the treatment of type 2 diabetes. Rivoglitazone has been shown, through small clinical studies,
T10596	BR102375	Others	Others
	BR102375 is a non-TZD PPAR γ full agonist (EC50: 0.28 μM) for the treatment of type 2 diabetes.
T78582	15-keto-Prostaglandin E2 15-keto-PGE2	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	15-keto-Prostaglandin E2为内源性代谢产物，通过与STAT3Cys259残基结合，抑制STAT3激活作用。该化合物能够结合并稳定EP2与EP4受体，进而抑制乳腺癌细胞生长与进展，并通过激活PPAR-γ促进真菌生长。
T33415	MK 0767 MK0767,MK-0767
	MK 0767 is a dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist that has been investigated as a potential treatment for type 2 diabetes and dyslipidemia.
T62576	Darglitazone Sodium
	Darglitazone Sodium 是一种噻唑烷二酮，是一种选择性的、口服具有活力的 PPAR-γ (过氧化物酶体增殖物激活受体)激动剂。Darglitazone Sodium 可以有效控制血糖和脂质代谢，能够用于研究 II 型糖尿病。
T81121	SP4e	PPAR	DNA Damage/DNA Repair; Metabolism
	SP4e是一种PPAR-γ激活剂，其在HK-2细胞中展现出的EC50为739 nM。在瑞士白化病小鼠模型中，SP4e能有效降低血糖和脂质过氧化水平，并提升谷胱甘肽含量及过氧化氢酶的活性。
T79231	DSO-5a	PPAR	DNA Damage/DNA Repair; Metabolism
	DSO-5a为具口服活性的BB3激动剂，兼具效力与选择性。此化合物为DMAKO-00系列衍生物，能够通过BB3提升ppar-γ功能并促进ERK1/2的磷酸化。DSO-5a主要应用于糖尿病领域的研究。
T37579	GW 1929 hydrochloride
	Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 \|Nugent et al (2001) Pote...
T81120	SP4f	PPAR	DNA Damage/DNA Repair; Metabolism
	SP4f为PPAR-γ激活剂，其在HK-2细胞中EC50值为826 nM。在瑞士白化病小鼠中，SP4f能够降低血糖和脂质过氧化水平，同时提升谷胱甘肽含量和过氧化氢酶活性。
T37829	CAY10573
	The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively. CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound ros...
T69671	SR1903 TFA
	SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-190...
T61976	DS-6930
	DS-6930 是一种有效的和选择性的 PPARγ激动剂（EC50= 41 nM）。DS-6930 可有效降低血浆葡萄糖 (PG)水平，此外，与 Rosiglitazone 相比，具有更少的 PPARγ 相关不良反应。DS-6930 在糖尿病中具有研究价值。
T35813	CAY10592
	Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) ...

化合物

Cat.No: T22708

Synonym: CP-86325

Target: PPAR

Cat.No: T1461

Synonym: CV 11974,坎地沙坦

Target: RAAS

Cat.No: TQ0156

Target: PPAR

Cat.No: T15575

Synonym: PPM 204

Target: PPAR

Cat.No: T27303

Synonym: GI-262570,GI 262570,GI262570

Cat.No: T21587

Synonym: Pargluva,BMS-298585

Target: PPAR

Cat.No: T28589

Synonym: Ro-41-5253,Ro 415253

Target: Apoptosis, Retinoid Receptor

Cat.No: T8780

Synonym: INT-131,AMG-131,CHS 131

Target: PPAR

Cat.No: T16739

Synonym: NID 525

Target: Leukotriene Receptor, PPAR

Cat.No: T7621

Synonym: 6-Mercaptopurine riboside,6-疏基嘌呤核苷,6TI

Target: Nucleoside Antimetabolite/Analog

Cat.No: T16022

Synonym: JNJ 39659100,芳卤芬酯,4-氯-ALPHA-[3-(三氟甲基)苯氧基]苯乙酸 2-(乙酰基氨基)乙酯,MBX 102

Target: PPAR

Cat.No: T17044

Target: PPAR

PPAR agonist 1

Cat.No: T10506

Target: PPAR

Cat.No: T27513

Synonym: GW 7845,GW-7845

Rivoglitazone HCl

Cat.No: T28542

Synonym: CI-1037,CI1037,CS011,CS-011,CI 1037

Cat.No: T10596

Target: Others

15-keto-Prostaglandin E2

Cat.No: T78582

Synonym: 15-keto-PGE2

Target: Prostaglandin Receptor

Cat.No: T33415

Synonym: MK0767,MK-0767

Darglitazone Sodium

Cat.No: T62576

Cat.No: T81121

Target: PPAR

Cat.No: T79231

Target: PPAR

GW 1929 hydrochloride

Cat.No: T37579

Cat.No: T81120

Target: PPAR

Cat.No: T37829

Cat.No: T69671

Cat.No: T61976

Cat.No: T35813

Cat. No.	Product Name	Target	Signaling Pathways
T1633	β-Carotene beta-胡萝卜素,Carotaben,Beta-Carotene,Provitamin A,β-胡萝卜素	Apoptosis; ROS; Endogenous Metabolite	Apoptosis; Immunology/Inflammation; Metabolism
	β-Carotene (Provitamin A) 是一种天然存在的视黄醇（维生素 A）前体。它是一种 ROS 调节剂，具有抗氧化和抗炎活性。它可作为抗氧化剂或者促氧化剂，可诱导乳腺癌细胞凋亡，具有抗癌活性。
TN1693	Glabrone	Influenza Virus; PPAR	DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
	Glabrone 是从甘草根中分离的一种异黄酮，可与 PPAR-γ 配体结合，具有抗流感活性。
T2946	Tanshinone IIA sulfonate sodium 丹参酮IIA磺酸盐,丹参酮IIA-磺酸钠,Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium	CaMK; P450; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) 是从丹参中提取的丹参酮IIA 的水溶性衍生物，是SOCE 抑制剂，用于心血管疾病的研究。
T6S0117	Avicularin Fenicularin,扁蓄苷	ERK	MAPK
	Avicularin (Fenicularin) 具有抗过敏、抗炎、保肝、抗氧化、抗肿瘤等活性。它能通过调节 NF-κB(p65)、COX-2 和 PPAR-γ 的活性来改善人类肝细胞癌。在 LPS 刺激的 RAW 264.7 巨噬细胞中，它通过抑制 ERK 信号通路产生抗炎活性。
T2932	Ginsenoside Rh1 Sanchinoside B2,人参皂苷 Rh1,人参皂苷Rh1,Prosapogenin A2,20(S)-Ginsenoside Rh1,Sanchinoside Rh1	IL Receptor; TNF; Endogenous Metabolite; PPAR; Interleukin	Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism
	Ginsenoside Rh1 (Sanchinoside B2) 是人参的一种主要成分，具有抗炎作用，抑制PPAR-γ，TNF-α，IL-6和IL-1β的表达。
TN1018	Angeloylgomisin H 当归酰戈米辛 H,当归酰戈米辛H	PPAR	DNA Damage/DNA Repair; Metabolism
	Angeloylgomisin H 是从五味子中提取的一种木脂素类天然产物。它通过激活PPAR-γ来改善胰岛素刺激的葡萄糖摄取潜力。
TN2601	12-O-Methylcarnosic acid	Reductase	Endocrinology/Hormones; Metabolism
	12-O-Methylcarnosic acid 是分离自小叶丹参的丙酮提取物的一种二萜肉桂酸，可抑制 5α-还原酶 (5α-reductase) 活性，IC50为 61.7 μM。它抑制 LNCaP 细胞的增殖。它具有抗微生物活性、抗氧化和抗癌活性。
T4956	Tetrahydroxystilbene-2-O-β-D-glucoside tetrahydroxyl diphenylethylene-2-o-gluco,何首乌苷,EH-201	Others	Others
	Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) 是一种低分子量的促红细胞生成素诱导剂。
T3867	Alpinetin 山姜素,(-)-alpinetin	BCL; PPAR	Apoptosis; DNA Damage/DNA Repair; Metabolism
	Alpinetin ((-)-alpinetin) 是从草豆蔻中分离得到的一种黄酮类天然产物，能够活化PPAR-γ，具有抗炎、抗菌活性。它通过抑制增殖、调节 Bcl-2 家族和 XIAP 表达、释放细胞色素 c 和激活 caspase 具有很强的抗肝癌和胰腺癌细胞作用。
TN4860	Pueroside B	COX; PPAR	DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience
	Pueroside B may can treat coronary heart disease, it can interact with two or more targets[peroxisome proliferator activated receptor γ (PPAR-γ), angiotensin-converting enzyme (ACE), hydroxymethylglutaryl coenzyme A receptor (HMGR), cyclooxygenase-2 (COX2
TN3219	7,8-Didehydrocimigenol	ERK; IκB/IKK; TNF; NF-κB; Akt; PPAR	Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
	7,8-Didehydrocimigenol can be used for the treatment of cardiovascular disorders such as atherosclerosis. It upregulates PPAR-γ in EC inhibits NF-kB activity of TNF-α-activated EC which leads to selective inhibition of VCAM-1 expression.
TN3655	Cimiside E	ERK; TNF; ROS; Akt; PI3K; PKC; PPAR	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Metabolism; PI3K/Akt/mTOR signaling
	Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC are involved in this effect.Cimiside E may be an effective chemopreventive agen

天然产物

Cat.No: T1633

Synonym: beta-胡萝卜素,Carotaben,Beta-Carotene,Provitamin A,β-胡萝卜素

Target: Apoptosis, ROS, Endogenous Metabolite

Cat.No: TN1693

Target: Influenza Virus, PPAR

Tanshinone IIA sulfonate sodium

Cat.No: T2946

Synonym: 丹参酮IIA磺酸盐,丹参酮IIA-磺酸钠,Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium

Target: CaMK, P450, Calcium Channel

Cat.No: T6S0117

Synonym: Fenicularin,扁蓄苷

Target: ERK

Ginsenoside Rh1

Cat.No: T2932

Synonym: Sanchinoside B2,人参皂苷 Rh1,人参皂苷Rh1,Prosapogenin A2,20(S)-Ginsenoside Rh1,Sanchinoside Rh1

Target: IL Receptor, TNF, Endogenous Metabolite, PPAR, Interleukin

Angeloylgomisin H

Cat.No: TN1018

Synonym: 当归酰戈米辛 H,当归酰戈米辛H

Target: PPAR

12-O-Methylcarnosic acid

Cat.No: TN2601

Target: Reductase

Tetrahydroxystilbene-2-O-β-D-glucoside

Cat.No: T4956

Synonym: tetrahydroxyl diphenylethylene-2-o-gluco,何首乌苷,EH-201

Target: Others

Cat.No: T3867

Synonym: 山姜素,(-)-alpinetin

Target: BCL, PPAR

Cat.No: TN4860

Target: COX, PPAR

7,8-Didehydrocimigenol

Cat.No: TN3219

Target: ERK, IκB/IKK, TNF, NF-κB, Akt, PPAR

Cat.No: TN3655

Target: ERK, TNF, ROS, Akt, PI3K, PKC, PPAR

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