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抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9193	ACH-000143	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	ACH-000143 是一种可口服的褪黑素受体激动剂，对 MT1 和 MT2 的EC50值分别为0.06 和0.32 nM。
T21902	ML351	Lipoxygenase	Metabolism
	ML351 是一种高度特异的15-LOX-1抑制剂，其 IC50=200 nM。它对 T1D 非肥胖糖尿病小鼠模型的血糖异常和β细胞氧化应激有抑制作用。它对相关同工酶 (5-LOX、血小板 12-LOX、15-LOX-2、绵羊 COX-1 和人 COX-2) 表现出良好的选择性(>250倍)。
T8676	FOY 251	Others; Serine/threonin kinase; SARS-CoV	Cell Cycle/Checkpoint; Metabolism; Microbiology/Virology; Others
	FOY 251 是一种蛋白酶抑制剂，是具有抗蛋白水解活性的 Camostate 代谢物，能抑制 SARS-CoV-2 的感染。
T0839	Ketoprofen 酮基布洛芬,RP-19583,酮洛芬	Apoptosis; COX; MRP	Apoptosis; Immunology/Inflammation; Neuroscience
	Ketoprofen (RP-19583) 是一种非甾体抗炎剂，能够有效地抑制COX 的活性，在人血单核细胞中，对 COX-1 和 COX-2 的IC50值分别为 2 nM 和 26 nM。
T24121	GW438014A GW 438014 A,GW-438014-A	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	GW438014A 是一种有效且具有选择性的 NPY-Y5 受体拮抗剂。GW438014A 对食物摄入并减少肥胖啮齿动物的体重增加具有抑制作用。
T26986	Cevoglitazar LBM-642,LBM 642,LBM642	PPAR	DNA Damage/DNA Repair; Metabolism
	Cevoglitazar (LBM-642) 是一种 PPARɑ 激动剂和 PPARγ激动剂。Cevoglitazar 能有效减少肥胖小鼠和猴的食物摄入量和体重。
T15679	L 152804	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	L 152804 是神经肽 Y Y5 受体的特异性拮抗剂，可调节食物摄入和能量消耗，从而导致饮食诱导的肥胖小鼠体重减轻。
TP2047L	CRF (6-33) acetate(120066-38-8 free base)	CRFR	GPCR/G Protein
	CRF (6-33) acetate(120066-38-8 free base) 是促肾上腺皮质激素释放因子结合蛋白 (CRFBP) 抑制肽；从 CRFBP 中替换 CRF。在体内抑制肥胖大鼠的体重增加并增加运动活动。
T38074	Thiodigalactoside	Galectin	Immunology/Inflammation
	Thiodigalactoside 是一种具有口服活性的，有效的半乳凝素 (GAL) 抑制剂，对于 GAL-1 和 GAL-3 的 Kd 值分别为 24 μM，49 μM。Thiodigalactoside 是一种不可代谢的二糖，具有抗炎和抗癌活性。Thiodigalactoside 可显着降低饮食诱发的肥胖大鼠的体重增加。
TP1913L1	BA 1 acetate(183241-31-8 free base)	Bombesin Receptor	GPCR/G Protein
	BA 1 acetate(183241-31-8 free base) 是一种有效的铃蟾肽受体激动剂（BB1、BB2 和 BB3 的 IC50 值分别为 0.26、1.55 和 2.52 nM）。它增强肥胖和糖尿病原发性肌细胞中的葡萄糖转运，还可在体外刺激 NCI-H1299 肺癌细胞增殖。
T4681	T863 DGAT-3,DGAT-1 inhibitor	Acyltransferase; Transferase	Metabolism
	T863 (DGAT-3) 是口服有效的二酰基甘油酰基转移酶1 选择性抑制剂。T863结合DGAT1的酰基辅酶A 结合位点，抑制三酰甘油在细胞内的合成。
T3685	SR9009 Stenabolic,REV-ERB Agonist II	Autophagy	Autophagy
	SR9009 (Stenabolic) 是一种REV-ERBα/β激动剂，可增加由 REV-ERBα/ERBβ 调节的基因的组成性抑制，IC50分别为 670 nM 和 800 nM。
TP1930L1	Spexin acetate(1370290-58-6 free base)	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	Spexin acetate(1370290-58-6 free base) 是一种有效的甘丙肽受体 2/3 (GAL2/GAL3) 激动剂（EC50 值分别为 45.7 和 112.2 nM）。对甘丙肽受体 1 没有显着的活性。抑制脂肪细胞对长链脂肪酸的摄取并减少饮食诱导的肥胖小鼠和大鼠的食物消耗。减少金鱼的 LH 分泌。在体内表现出抗焦虑作用。
T10613	BRL 37344 sodium BRL 37344A	Others	Others
	BRL 37344 sodium is a specific agonist of the β3-adrenergic receptor. The treatment of BRL 37344 sodium significantly lowers the bodyweight of obese mice.
TP2047	CRF(6-33)(human) CRF (6-33)
	CRF(6-33)(human) is a Corticotropin-releasing factor binding protein (CRFBP) inhibitor peptide; displaces CRF from CRFBP. Suppresses body weight gain and increases motor activity in obese rats in vivo.
TP1679	BDC2.5 mimotope 1040-51
	BDC2.5 mimotope 1040-51 is a mimotope peptide for diabetogenic T cell clone BDC2.5. isolated from non-obese diabetic mice.This is a effectively agonistic peptide (mimotope) for diabetogenic T cell clone BDC2.5. from non-obese diabetic (NOD) mice. T cells
T35265	YM-440 YM440,YM 440
	YM-440 is a novel hypoglycemic agent, an insulin sensitizer, that may be used for the treatment of type 2 diabetes mellitus by reducing glucose 6-phosphatase activity in obese Zucker rats and inhibiting liver glucose output through gluconeogenesis.
T21811	LH 21
	LH-21 是一种有效的体内中性大麻素 CB1受体拮抗剂。LH-21 会导致剂量依赖性进食抑制，减少肥胖 Zucker 大鼠的食物摄入和体重增加。
TP1913	BA 1
	Potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). Enhances glucose transport in obese and diabetic primary myocytes. Also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
T82079	IGRP(206-214)
	IGRP(206-214) 是一种肽，具有生物活性。它对应于非肥胖糖尿病型(NOD)小鼠中胰岛特异性葡萄糖6磷酸酶催化亚基相关蛋白（IGRP）的206-214残基，并能诱导此类小鼠产生糖尿病。此外，该肽对胰岛素原特异性T细胞有着特定的作用。
T81663	NN1177 NNC9204-1177
	NN1177为一种长效GLP-1/胰高血糖素受体共激动剂，其能够在饮食诱导肥胖(DIO)小鼠中引发剂量依赖性的体重下降。NN1177适用于减肥与代谢控制研究领域。
T37640	trans-2-Hexadecenoyl-L-carnitine
	trans-2-Hexadecenoyl-L-carnitine is an endogenous metabolite in urine[1]. [1]. Pengxiang She, et al. Leucine and protein metabolism in obese Zucker rats. PLoS One. 2013;8(3):e59443.
T28511	Reglitazar JTT-501,JTT501,PNU-182716,PNU182716,PNU-716
	Reglitazar is a PPARɑ agonist and PPARγ agonist. Reglitazar rapidly stimulates glucose disposal rates by enhancing insulin signal transduction in skeletal muscle. Reglitazar improves insulin resistance in genetic and non-genetic insulin-resistant models.
T76002	Spexin TFA
	Spexin TFA, a potent agonist for galanin receptor 2/3 (GAL2/GAL3) with EC50 values of 45.7 and 112.2 nM respectively, shows no significant activity towards galanin receptor 1. As an endogenous peptide promoting satiety, it reduces long chain fatty acid uptake by adipocytes and lowers food consumption in diet-induced obese mice and rats. Additionally, it moderates LH secretion in goldfish and demonstrates anxiolytic effects in vivo.
T81214	SAR441255
	SAR441255为高效单分子肽GLP-1/GIP/GCG受体激动剂，能平衡激活三种靶受体，表现出高效力。此外，SAR441255对糖尿病肥胖猴子具有显著的急性血糖调节效果。
T35809	C20 Sphingomyelin (d18:1/20:0)
	C20 Sphingomyelin is a naturally occurring sphingolipid. Levels of C20 sphingomyelin are upregulated in the hippocampus of rats with diabetes induced by streptozotocin and in human plasma where it is positively correlated with insulin resistance in obese humans. C20 sphingomyelin is also upregulated in the liver of a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. The plasma concentration of C20 sphingomyelin is decreased in m...
T15043	D5D-IN-326	Others	Others
	D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in die
T35631	Peptide YY (human) (trifluoroacetate salt) Peptide Tyrosine Tyrosine
	Peptide YY (PYY) is a 36-amino acid peptide and anorectic gut hormone agonist for the neuropeptide Y receptors Y1, Y2, Y5, and Y6 with EC50 values of 0.7, 0.58, 1, and 0.8 nM, respectively, for supression of forskolin-induced cAMP accumulation. PYY is cleaved in vivo to PYY (3-36) . Release of PYY occurs postprandially in proportion to calorie intake from intestinal enteroendocrine L cells, indicating it may be a satiety signal. In humans, PYY inhibits food intake and gastrointestinal transit in...
TP1930	Spexin
	Potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by adipocytes and decreas
T35445	1-Stearoyl-3-Oleoyl-rac-glycerol
	1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fa...
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) ...
T82354	GAD65 (524-543)
	GAD65 (524-543) 是具有生物活性的肽，属于谷氨酸脱羧酶 65 (GAD65) 氨基酸片段 524-543。作为胰岛抗原的关键片段之一，该肽在自发性自身免疫性糖尿病非肥胖糖尿病 (NOD) 小鼠模型中，可诱导增殖性 T 细胞反应。GAD65 (524-543) 对T细胞克隆BDC2.5具有特异性刺激作用，但可能存在亲和力较低的问题。此外，p524-543免疫可增强NOD小鼠对通过BDC2.5 T细胞过继转移诱导的1型糖尿病的敏感性。
T35622	FKGK 18
	FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits gl...
T35547	YW1128
	YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid ac...
T35799	MBX-8025 (sodium salt)
	MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transamin...

化合物

Cat.No: T9193

Target: Melatonin Receptor, MT Receptor

Cat.No: T21902

Target: Lipoxygenase

Cat.No: T8676

Target: Others, Serine/threonin kinase, SARS-CoV

Cat.No: T0839

Synonym: 酮基布洛芬,RP-19583,酮洛芬

Target: Apoptosis, COX, MRP

Cat.No: T24121

Synonym: GW 438014 A,GW-438014-A

Target: Neuropeptide Y Receptor

Cat.No: T26986

Synonym: LBM-642,LBM 642,LBM642

Target: PPAR

Cat.No: T15679

Target: Neuropeptide Y Receptor

CRF (6-33) acetate(120066-38-8 free base)

Cat.No: TP2047L

Target: CRFR

Thiodigalactoside

Cat.No: T38074

Target: Galectin

BA 1 acetate(183241-31-8 free base)

Cat.No: TP1913L1

Target: Bombesin Receptor

Cat.No: T4681

Synonym: DGAT-3,DGAT-1 inhibitor

Target: Acyltransferase, Transferase

Cat.No: T3685

Synonym: Stenabolic,REV-ERB Agonist II

Target: Autophagy

Spexin acetate(1370290-58-6 free base)

Cat.No: TP1930L1

Target: Neuropeptide Y Receptor

BRL 37344 sodium

Cat.No: T10613

Synonym: BRL 37344A

Target: Others

CRF(6-33)(human)

Cat.No: TP2047

Synonym: CRF (6-33)

BDC2.5 mimotope 1040-51

Cat.No: TP1679

Cat.No: T35265

Synonym: YM440,YM 440

Cat.No: T21811

Cat.No: TP1913

Cat.No: T82079

Cat.No: T81663

Synonym: NNC9204-1177

trans-2-Hexadecenoyl-L-carnitine

Cat.No: T37640

Cat.No: T28511

Synonym: JTT-501,JTT501,PNU-182716,PNU182716,PNU-716

Cat.No: T76002

Cat.No: T81214

C20 Sphingomyelin (d18:1/20:0)

Cat.No: T35809

Cat.No: T15043

Target: Others

Peptide YY (human) (trifluoroacetate salt)

Cat.No: T35631

Synonym: Peptide Tyrosine Tyrosine

Cat.No: TP1930

1-Stearoyl-3-Oleoyl-rac-glycerol

Cat.No: T35445

Cat.No: T35813

GAD65 (524-543)

Cat.No: T82354

Cat.No: T35622

Cat.No: T35547

MBX-8025 (sodium salt)

Cat.No: T35799

Cat. No.	Product Name	Target	Signaling Pathways
T17303	α-Cyclodextrin Alfadex,NSC269470,α-环糊精,NSC 269470,NSC-269470	Others	Others
	α-Cyclodextrin (Alfadex) 是一种多功能可溶性膳食纤维，可作为纤维原料销售。
T4785	Oxfenicine 4-羟基-L-苯甘氨酸,4-Hydroxy-L-phenylglycine	Others	Others
	Oxfenicine (4-Hydroxy-L-phenylglycine) 是具有口服活性的肉碱棕榈酰转移酶-1 抑制剂。它在缺血期间保护心脏免受坏死组织的损害。它可抑制心脏中脂肪酸的氧化。
T2S2173	(E)-Naringenin chalcone Isosalipurpol,柚皮苷查尔酮,Chalconaringenin,trans-2'4'6'4-tetrahydroxychalcone,柚皮素查耳酮	Others	Others
	Naringenin chalcone (Isosalipurpol) 是一种黄酮醇生物合成的中间体，在查耳酮异构酶的作用下，自发代谢成柚皮素。它具有抗炎和抗过敏活性。
T10044	13-Oxo-9E,11E-octadecadienoic acid	PPAR	DNA Damage/DNA Repair; Metabolism
	13-Oxo-9E,11E-octadecadienoic acid, a potent PPARα activator derived from tomato juice and an isomer of 9-oxo-ODA, exhibits the ability to decrease plasma and hepatic triglyceride levels in obese diabetic mice[1].

天然产物

α-Cyclodextrin

Cat.No: T17303

Synonym: Alfadex,NSC269470,α-环糊精,NSC 269470,NSC-269470

Target: Others

Cat.No: T4785

Synonym: 4-羟基-L-苯甘氨酸,4-Hydroxy-L-phenylglycine

Target: Others

(E)-Naringenin chalcone

Cat.No: T2S2173

Synonym: Isosalipurpol,柚皮苷查尔酮,Chalconaringenin,trans-2'4'6'4-tetrahydroxychalcone,柚皮素查耳酮

Target: Others

13-Oxo-9E,11E-octadecadienoic acid

Cat.No: T10044

Target: PPAR

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