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APD668

Catalog No. A14342
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GPR119 激动剂

APD668是有效的GPR119激动剂，hGPR119和ratGPR119的EC50分别为2.7 nM和33 nM。了解更多

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Isoprenaline HCl

Catalog No. A10484
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β adrenoceptor 激动剂

Isoprenaline HCl或isoproterenol是非选择性β肾上腺素能激动剂，在结构上类似于肾上腺素。了解更多

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Bromocriptin mesylate

Catalog No. A13705
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dopamine D2 receptor 激动剂

Bromocriptin mesylate是一种有效的多巴胺受体激动剂，它以最高的亲和力（Ki = 2.5 nM）与D2受体结合。了解更多

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Mosapride citrate

Catalog No. A10607
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5-HT4-receptor 激动剂

Mosapride citrate起5-HT4受体激动剂和5-HT3受体拮抗剂的作用。了解更多

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Troglitazone

Catalog No. A11981
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PPARγ 激动剂

Troglitazone是一种选择性PPARγ受体激动剂（鼠和人PPARγ受体的EC50值分别为780和555 nM）。了解更多

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- Julien Allard, .et al. Drug-induced Hepatic Steatosis in Absence of Severe Mitochondrial Dysfunction in HepaRG Cells: Proof of Multiple Mechanism-Based Toxicity, Cell Biol Toxicol, 2020, Jun 14 PMID: 32535746
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Guanfacine hydrochloride

Catalog No. A15098
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α2A-adrenoceptor 激动剂

Guanfacine hydrochloride是一种抗高血压药，是一种选择性的α2A肾上腺素受体激动剂，Kd为31 nM，选择性是α2B肾上腺素受体的60倍。了解更多

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Hexestrol

Catalog No. A10451
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Estrogen/progestogen Receptor 激动剂

Hexestrol是一种致癌的合成雌激素，可抑制微管聚合和带状结构的形成。它是脂质过氧化的抑制剂。了解更多

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Carvedilol

Catalog No. A11843
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β2-adrenergic receptor

Carvedilol是具有抗氧化特性的β1和β2肾上腺素能受体（AR）激动剂。了解更多

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Pimavanserin (ACP-103)

Catalog No. A14434
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5-HT2A receptor 激动剂

Pimavanserin (ACP-103)是一种有效的选择性5-HT2A受体反向激动剂，在基于细胞的功能测定中，平均pIC50为8.7。了解更多

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GW4064

Catalog No. A11141
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FXR 激动剂

GW4064是选择性的非甾体类法尼醇X受体（FXR）激动剂（EC50 = 15 nM）。了解更多

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- Dong-Hyun Kim, .et al. The critical role of FXR is associated with the regulation of autophagy and apoptosis in the progression of AKI to CKD, Cell Death Dis, 2021, Apr; 12(4): 320 PMID: 33767132
- Takae K, .et al. Evidence for the involvement of FXR signaling in ovarian granulosa cell function, J Reprod Dev, 2018, Nov 16 PMID: 30449821
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Nalfurafine hydrochloride

Catalog No. A12579
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opioid κ-selective 激动剂

Nalfurafine hydrochloride是一种κ-opioid激动剂。了解更多

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- Alexander R French, .et al. Sex- and β-arrestin-dependent effects of kappa opioid receptor-mediated ethanol consumption, Pharmacol Biochem Behav, 2022, May;216:173377 PMID: 35364122
- Wen-Wen Zhang, .et al. Peripheral ablation of type III adenylyl cyclase induces hyperalgesia and eliminates KOR-mediated analgesia in mice, JCI Insight, 2022, Feb 8;7(3):e153191 PMID: 34914639
- A Dunn, .et al. Modulation of Cocaine-Related Behaviors by Low Doses of the Potent KOR Agonist Nalfurafine in Male C57BL6 Mice, Psychopharmacology (Berl), 2020, May 20 PMID: 32435819
- Dunn AD, .et al. Signaling Properties of Structurally Diverse Kappa Opioid Receptor Ligands: Toward in Vitro Models of in Vivo Responses, ACS Chem Neurosci, 2019, Aug 21;10(8):3590-3600 PMID: 31313902
- Anika Mann, .et al. Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists, Sci Signal, 2019, Mar 26;12(574). pii: eaau8072 PMID: 30914485
- Snyder LM, .et al. Kappa Opioid Receptor Distribution and Function in Primary Afferents, Neuron, 2018, Sep 19;99(6):1274-1288.e6 PMID: 30236284
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Eptapirone

Catalog No. A15923
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5HT(1A) receptor 激动剂

Eptapirone是一种有效的，选择性的，高效的5-HT1A受体激动剂，具有显着的抗焦虑和抗抑郁潜力。了解更多

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Ramelteon (TAK-375)

Catalog No. A10777
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MT1/MT2-Receptor 激动剂

Ramelteon (TAK-375)是melatonin受体激动剂，对褪黑激素MT1（IC50 = 28.5±8.55 pM）和MT2（20.1±9.25 pM）受体均具有高亲和力，并且相对于MT3受体具有选择性。了解更多

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Naxagolide

Catalog No. A13087
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D2 激动剂

Naxagolide是一种多巴胺D2受体激动剂，用于治疗锥体外系疾病。了解更多

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Varenicline

Catalog No. A10966
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nAChR partial agonist

Varenicline是烟碱样受体部分激动剂。了解更多

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TTNPB

Catalog No. A13007
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RAR 激动剂

TTNPB增强了化学诱导的多能干细胞（CiPSC）的重编程效率。了解更多

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Salmeterol Xinafoate

Catalog No. A14223
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β2-adrenoceptor 激动剂

Salmeterol Xinafoate是一种长效的β2-肾上腺素能受体激动剂，具有抗炎作用。了解更多

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AM 580

Catalog No. A11792
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RARα 激动剂

AM 580是视黄酸的类似物，可作为选择性RARα激动剂。了解更多

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IB-MECA

Catalog No. A14345
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Adenosine A3-R 激动剂

IB-MECA已被证明是一种有效的选择性腺苷A3-R激动剂，腺苷A3-R，腺苷A1-R和腺苷A2A-R的Ki值分别为1.1、54和56 nM。了解更多

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- Sameshima T, .et al. Small-scale panel comprising diverse gene family targets to evaluate compound promiscuity, Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
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Clomipramine HCl

Catalog No. A10231
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5-HT Receptor 激动剂

Clomipramine HCl是下列转运蛋白的阻滞剂：5-羟色胺转运蛋白 (SERT)(Ki = 0.14 nM)，去甲肾上腺素转运蛋白（NET）(Ki = 54 nM)，多巴胺转运蛋白（DAT）(Ki = 3，020 nM)，甘氨酸转运蛋白（GlyT/LeuT）。了解更多

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GW0742

Catalog No. A14958
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PPAR 激动剂

GW0742是PPARδ的选择性激动剂，EC50值为1.1 nM。了解更多

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Kaempferol

Catalog No. A10495
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ERRα and ERRγ inverse 激动剂

Kaempferol被发现抑制Ki为0.3-0.5 μM的牛主动脉肌球蛋白轻链激酶，并且还被发现通过新的ERK-NFκB-cMyc-p21途径抑制VEGF表达和体外血管生成。了解更多

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Almotriptan malate (Axert)

Catalog No. A11799
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5-HT Receptor 激动剂

Almotriptan malate (Axert)是一种选择性的5-羟色胺1B/1D（5-HT1B/1D）受体激动剂，用于治疗成人偏头痛。了解更多

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- Li Li, .et al. Delineating a serotonin 1B receptor circuit for appetite suppression in mice, J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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LM22A-4

Catalog No. A15494
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TrkB 激动剂

LM22A-4是有效的原肌球蛋白相关激酶B（TrkB）激动剂（IC50 = 47 nM）。了解更多

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ADL5859 HCl

Catalog No. A11072
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Opioid Receptor 激动剂

ADL5859 HCl是高效的选择性δ阿片受体激动剂，Ki值为0.84 nM，ED50值为20 nM。了解更多

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Lithocholic acid

Catalog No. A12547
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FXR 激动剂

Lithocholic acid是胆汁酸，用作去污剂以溶解脂肪以供吸收。了解更多

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BML-284 (Wnt agonist 1)

Catalog No. A15851
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Wnt 激动剂 1

BML-284 (Wnt agonist 1)是细胞可渗透的Wnt信号传导活化剂。它诱导β-catenin和TCF依赖性转录活性，EC50值为0.7 uM。了解更多

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GW3965 HCl

Catalog No. A11204
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LXR-like receptors 激动剂

GW3965 HCl是一种选择性的口服活性肝X受体（LXR）完全激动剂。了解更多

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- Mohácsik P, .et al. A Transgenic Mouse Model for Detection of Tissue-Specific Thyroid Hormone Action, Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
- Pencheva N, .et al. Broad-spectrum therapeutic suppression of metastatic melanoma through nuclear hormone receptor activation., Cell., 2014, 156(5):986-1001 PMID: 24581497
- Bin Dong, .et al. High-fructose diet downregulates long-chain acyl-CoA synthetase 3 expression in liver of hamsters via impairing LXR/RXR signaling pathway, J Lipid Res., 2013, May; 54(5): 1241-1254. PMID: 23427282
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Lorcaserin

Catalog No. A12378
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5-HT2C 激动剂

Lorcaserin是一种新的选择性人5-羟色胺2c激动剂。了解更多

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- Tanishka S Saraf, .et al. Evaluation of lorcaserin as an anticonvulsant in juvenile Fmr1 knockout mice, Epilepsy Res, 2021, Sep;175:106677 PMID: 34130255
- Josua Jordi, .et al. High-throughput screening for selective appetite modulators: A multibehavioral and translational drug discovery strategy, Sci Adv, 2018, Oct; 4(10): eaav1966 PMID: 30402545
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Elafibranor

Catalog No. A15454
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PPAR 激动剂

Elafibranor是过氧化物酶体增殖物激活的受体-α和-δ的激动剂，可诱导非酒精性脂肪性肝炎消退，而不会使纤维化恶化。了解更多

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- Joost Boeckmans, .et al. Transcriptomics Reveals Discordant Lipid Metabolism Effects between In Vitro Models Exposed to Elafibranor and Liver Samples of NAFLD Patients after Bariatric Surgery, Cells, 2022, 11(5), 893 PMID: 35269515
- Tomasz Kostrzewski, .et al. Modelling human liver fibrosis in the context of non-alcoholic steatohepatitis using a microphysiological system, Commun Biol, 2021, 4: 1080 PMID: 34526653
- Joost Boeckmans, .et al. Flow cytometric quantification of neutral lipids in a human skin stem cell-derived model of NASH, MethodsX, 2020, 7: 101068 PMID: 33024711
- Joost Boeckmans, .et al. Human hepatic in vitro models reveal distinct anti-NASH potencies of PPAR agonists, Cell Biol Toxicol, 2020, Jul 1 PMID: 32613381
- Joost Boeckmans, .et al. Transcriptomics data of a human in vitro model of non-alcoholic steatohepatitis exposed to elafibranor, Data in Brief, 2019, June 3 PMID: 31294056
- Boeckmans J, .et al. Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH, Pharmacol Res, 2019, Apr 24. pii: S1043-6618(18)31850-4 PMID: 31028903
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GSK1292263

Catalog No. A10439
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GPR119 激动剂

GSK-1292263是一种新型GPR119激动剂。了解更多

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- Inoue A, .et al. Illuminating G-Protein-Coupling Selectivity of GPCRs, Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
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GS-9620

Catalog No. A13251
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TLR7 激动剂

GS-9620是Toll样受体7的有效选择性口服活性小分子激动剂。了解更多

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- Yu-Geun Ji, .et al. Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study, J Pharm Biomed Anal, 2019, 12 November, 112987
- Zhikuan Zhang, .et al. Structural Analyses of Toll-like Receptor 7 Reveal Detailed RNA Sequence Specificity and Recognition Mechanism of Agonistic Ligands, Cell Reports, 2018, 25(12): 3371-3381.e5 PMID: 30566863
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Lixisenatide

Catalog No. A14076
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GLP-1 receptor 激动剂

Lixisenatide抑制胰高血糖素释放，显着降低餐后胰高血糖素。对糖尿病（T2DM）有促进作用。了解更多

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Pioglitazone (Actos)

Catalog No. A11680
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PPARγ 激动剂

Pioglitazone (Actos)是选择性刺激核受体过氧化物酶体增殖物激活的受体γ（PPAR-γ），并在较小程度上刺激PPAR-α。了解更多

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NS-304 (Selexipag)

Catalog No. A13880
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prostacyclin receptor 激动剂

NS-304 (Selexipag)是一种选择性的前列环素IP1受体激动剂（人和大鼠IP受体的Ki值为260和2100 nM，EP1-4，DP，FP和TP受体的Ki值为> 10μM）。了解更多

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WIN 55,212-2 mesylate

Catalog No. A11932
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CB receptor 激动剂

WIN 55,212-2 mesylate是一种有效的cannabinoid receptor激动剂，在神经性疼痛的大鼠模型中具有有效的镇痛作用。它通过受体介导的信号激活p42和p44 MAP激酶。了解更多

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- Greish K, .et al. Synthetic cannabinoids nano-micelles for the management of triple negative breast cancer, J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922
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SAG

Catalog No. A13627
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SMO 激动剂

SAG是一种含氯苯并噻吩的化合物，可作为SMO激动剂（EC50 = 3 nM），但在高浓度（> 1 uM）下抑制刺猬信号。了解更多

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Imiquimod (Aldara)

Catalog No. A10469
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TLR7 激动剂

Imiquimod (Aldara)是一种杂环咪唑并喹啉酰胺，用作免疫反应调节剂。了解更多

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- David Diaz-Carballo, .et al. Enhanced antitumoral activity of TLR7 agonists via activation of human endogenous retroviruses by HDAC inhibitors, Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Kunishita Y, .et al. TRIM21 Dysfunction Enhances Aberrant B-Cell Differentiation in Autoimmune Pathogenesis, Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
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L-165,041

Catalog No. A11983
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PPARδ 激动剂

L-165,041是有效的PPARδ激动剂（Ki = 6 nM）；与其他亚型相比，对小鼠和人类PPARδ受体的选择性显示> 100倍。了解更多

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Balaglitazone

Catalog No. A15013
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PPAR-γ partial 激动剂

Balaglitazone是PPAR-γ（γ）的新型局部激动剂。了解更多

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Rosiglitazone maleate

Catalog No. A10809
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PPAR 激动剂

Rosiglitazone maleate是一种噻唑烷二酮类抗高血糖药，是PPARγ的高亲和、选择性的激动剂。了解更多

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Salmeterol

Catalog No. A11788
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beta2-adrenergic receptor 激动剂

Salmeterol是一种长效β2-肾上腺素能受体激动剂。了解更多

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JNJ 63533054

Catalog No. A15449
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GPR139 激动剂

JNJ 63533054是一种有效的选择性GPR139激动剂，EC50值为16nM。了解更多

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MCOPPB 3HCl

Catalog No. A10561
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NOP receptor 激动剂

MCOPPB 3HCl是一种用作伤害感受器受体的有效和选择性激动剂的化合物，pKi为10.07。了解更多

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T0901317

Catalog No. A12652
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LXR/FXR 激动剂

T0901317是有效的，高亲和力的肝X受体（LXR）激动剂（EC50~50 nM，LXR-β和LXR-β的Kd值分别为7和22 nM）。了解更多

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- Tian Yongsong, .et al. Tritium hydrogen-isotope exchange with electron-poor tertiary benzenesulfonamide moiety; application in late-stage labeling of T0901317, J Labelled Comp Radiopharm, 2022, Feb;65(2):36-44 PMID: 34957593
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Tretinoin

Catalog No. A10944
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RAR 激动剂

Tretinoin 是视黄酸受体的内源性激动剂，RAR-α，RAR-β和RAR-γ受体的IC50值为14 nM。了解更多

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PNU 282987

Catalog No. A11233
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α7 nAChR 激动剂

PNU 282987 (PNU-282,987)可作为神经烟碱乙酰胆碱受体α7亚型的有效选择性激动剂。了解更多

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lorcaserin hydrochloride (APD-356)

Catalog No. A12598
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serotonin 2C receptor 激动剂

lorcaserin hydrochloride (APD-356)是血清素2C受体激动剂，可指示与减少热量饮食和增加体育锻炼以减轻慢性体重成人管理。了解更多

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- Li Li, .et al. Delineating a serotonin 1B receptor circuit for appetite suppression in mice, J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
- Henrik H. Hansen, .et al. Whole-brain activation signatures of weight-lowering drugs, Mol Metab, 2021, May;47:101171 PMID: 33529728
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Betamethasone dipropionate

Catalog No. A10130
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Glucocorticoid Receptor 激动剂

Betamethasone Dipropionate是糖皮质激素类固醇，具有抗炎和免疫抑制特性。了解更多

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Siramesine

Catalog No. A13036
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Sigma-2 receptor 激动剂

Siramesine是一种溶酶体去污剂，诱导细胞保护性自噬体积累。了解更多

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