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搜索结果：“glucagon receptor”

“glucagon receptor”的搜索结果

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FTY720 (Fingolimod)

Catalog No. A10408
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S1P Receptor 拮抗剂

FTY720 (Fingolimod)是ISP-1(肉豆蔻酸)的衍生物，ISP-1是中国草药Iscaria sinclarii的真菌代谢物，也是鞘氨醇的结构类似物。了解更多

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- Tina Sepasi, .et al. Targeted gene delivery to the brain using CDX-modified chitosan nanoparticles, BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. Effects of immunomodulatory drug Fingolimod (FTY720) on Chlamydia dissemination and pathogenesis, Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. Inulooligosaccharides in Atractylodis lanceae rhizoma and Atractylodis rhizoma of hochuekkito formula are essential for regulation of the pulmonary immune system of immuno-compromised mice, Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. 14-3-3 signal adaptor and scaffold proteins mediate GPCR trafficking, Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. Peyer's patch-immunomodulating glucans from sugar cane enhance protective immunity through stimulation of the hemopoietic system, Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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Bicalutamide (Casodex)

Catalog No. A10142
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Androgen Receptor 拮抗剂

Bicalutamide (Casodex)是一种口服非甾体抗雄激素，用于治疗前列腺癌和多毛症。了解更多

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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Amisulpride

Catalog No. A10067
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Dopamine Receptor 拮抗剂

Amisulpride是一种非典型抗精神病药，用于治疗精神分裂症的精神病和双相情感障碍的躁狂发作。了解更多

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Agomelatine

Catalog No. A10048
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5-HT Receptor 拮抗剂

Agomelatine是一种褪黑素激动剂（MT1和MT2受体）和5-HT2C拮抗剂。了解更多

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Ki16425

Catalog No. A10501
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LPA Receptor 拮抗剂

ki16425是对LPA1和LPA3具有选择性的LPA受体拮抗剂，对人LPA1、LPA2和LPA3受体分别显示Ki值为0.34、6.5和0.93 μM。了解更多

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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. Lateral access mechanism of LPA receptor probed by molecular dynamics simulation, PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. Illuminating G-Protein-Coupling Selectivity of GPCRs, Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA6, Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. Generalized pruritus in primary sclerosing cholangitis: implications of histamine release by lysophosphatidic acid., Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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Cyproterone acetate

Catalog No. A11409
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Androgen Receptor 拮抗剂

Cyproterone acetate是17-羟孕酮的合成衍生物，可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。了解更多

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Aprepitant (MK-0869)

Catalog No. A10083
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neurokinin-1 receptor 拮抗剂

Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示，阿瑞匹坦通过阻止P物质降落在大脑神经元受体上，从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性，它们也可用于预防化学疗法引起的恶心和呕吐。了解更多

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- Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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5-hydroxymethyl tolterodine (PNU 200577)

Catalog No. A11166
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muscarinic receptor 拮抗剂

5-hydroxymethyl tolterodine (PNU 200577)是托特罗定的代谢产物，tolterodine是一种用于治疗尿失禁的毒蕈碱受体拮抗剂。了解更多

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BRL-15572 dihydrochloride

Catalog No. A11178
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5-HT1D receptor 拮抗剂

BRL-15572是一种选择性的h5-HT1D拮抗剂，相对于h5-HT1B表现出60倍的选择性，对一系列其他受体类型的亲和力很小或没有亲和力。了解更多

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Naftopidil 2HCl

Catalog No. A10619
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5-HT1A and α1-adrenergic receptor 拮抗剂

Naftopidil 2HCl是选择性5-HT1A和α1-肾上腺素能受体拮抗剂，IC50分别为0.1μM和0.2μM。了解更多

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Puerarin (Kakonein)

Catalog No. A10759
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5-HT2C receptor 拮抗剂

Puerarin (Kakonein)是几种已知的异黄酮之一。Puerarin是5-HT2C受体和苯二氮卓类拮抗剂。Puerarin正在研究作为一种自微乳化药物递送系统。了解更多

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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Zibotentan (ZD4054)

Catalog No. A11006
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ETA-receptor 拮抗剂

Zibotentan (ZD4054)是一种有效且特异性的ETA受体（内皮素A受体）拮抗剂（IC50 = 21 nM），对ETB没有抑制活性。了解更多

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- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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MK 3207 HCl

Catalog No. A10598
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CGRP Receptor 拮抗剂

MK 3207 hydrochloride是一种有效的CGRP受体拮抗剂，IC50为0.12 nM。了解更多

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- Marlene Dallmayer, .et al. Targeting the CALCB/RAMP1-axis inhibits growth of Ewing sarcoma, bioRxiv, 2018, 2018
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Tolterodine tartrate (Detrol LA)

Catalog No. A10937
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muscarinic receptor 拮抗剂

Tolterodine tartrate (Detrol LA)是毒蕈碱受体拮抗剂。了解更多

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Ambrisentan (BSF 208075)

Catalog No. A11291
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EndothelinA receptor 拮抗剂

Ambrisentan (BSF 208075)充当内皮素受体拮抗剂，对A型内皮素受体（ETA）具有选择性。了解更多

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- Naoki Dohi, .et al. Quantitative real-time measurement of endothelin-1-induced contraction in single non-activated hepatic stellate cells, PLoS One, 2021, 16(8): e0255656 PMID: 34343209
- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
- Toshiaki Okamoto, .et al. Antifibrotic effects of ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model, World J Hepatol, 2016, Aug 8; 8(22): 933-941 PMID: 27574547
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Tamoxifen Citrate

Catalog No. A10885
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Estrogen receptor 拮抗剂

Tamoxifen Citrate是哺乳动物甾醇异构酶的选择性和有效抑制剂。了解更多

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- Renu Sudhakar, .et al. Bazedoxifene, a Postmenopausal Drug, Acts as an Antimalarial and Inhibits Hemozoin Formation, Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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MRS 2578

Catalog No. A11486
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P2Y6 Receptor 拮抗剂

MRS 2578是P2Y6核苷酸受体的选择性拮抗剂。了解更多

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SB269970 HCl

Catalog No. A11925
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5-HT7 receptor 拮抗剂

SB269970 HCl是有效的选择性5-HT7受体拮抗剂。了解更多

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Memantine hydrochloride

Catalog No. A11708
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NMDA receptor 拮抗剂

Memantine hydrochloride是nmda受体的拮抗剂，与离子通道位点结合。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，Ki分别为0.51 nM和94.9 μM。它被用于治疗帕金森综合征。了解更多

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Orphenadrine citrate

Catalog No. A11712
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NMDA receptor 拮抗剂

Orphenadrine柠檬酸盐是NMDA受体拮抗剂，Ki为6.0μM，还是HERG钾离子通道阻断剂。了解更多

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Lafutidine

Catalog No. A11714
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H2 receptor 拮抗剂

Lafutidine是具有多峰作用机制的第二代H2受体拮抗剂。了解更多

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Aminophylline

Catalog No. A10066
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Adenosine receptor 拮抗剂

Aminophylline是一种非选择性的腺苷受体拮抗剂和磷酸二酯酶抑制剂，能够逆转局部缺血引起的bradyasystole。了解更多

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Cimetidine

Catalog No. A10218
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H2-receptor 拮抗剂

Cimetidine是一种抑制胃酸产生的组胺H2受体拮抗剂。了解更多

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Dyphylline

Catalog No. A10339
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Adenosine receptor 拮抗剂

Dyphylline是黄嘌呤衍生物，具有支气管扩张药和血管扩张药的作用。它充当腺苷受体拮抗剂和磷酸二酯酶抑制剂。了解更多

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Ki16198

Catalog No. A11966
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LPA Receptor 拮抗剂

Ki16198是有效的LPA受体拮抗剂，可抑制LPA1和LPA3诱导的肌醇磷酸生成，Ki分别为0.34μM和0.93μM。了解更多

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Bepotastine Besilate

Catalog No. A11340
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Histamine Receptor 拮抗剂

Bepotastine Besilate是组胺H1受体激动剂。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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MK-0517 (Fosaprepitant)

Catalog No. A11756
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neurokinin-1 receptor 拮抗剂

MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药，它是NK1拮抗剂。了解更多

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MK-4305 (Suvorexant)

Catalog No. A11500
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OX receptor 拮抗剂

Suvorexant (MK-4305)是OX1R和OX2R的有效，选择性和口服可生物利用的拮抗剂，目前正在临床研究中作为失眠的新疗法。了解更多

Product Citations (9)

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- Richard L Spinieli, .et al. Orexin contributes to eupnea within a critical period of postnatal development, Am J Physiol Regul Integr Comp Physiol, 2021, Oct 1;321(4):R558-R571 PMID: 34405704
- Jacob W Clark, .et al. Manipulation of REM sleep via orexin and GABAA receptor modulators differentially affects fear extinction in mice: effect of stable versus disrupted circadian rhythm, Sleep, 2021, Mar 15;zsab068 PMID: 33720375
- Zhang B, .et al. Hypothalamic orexin and mechanistic target of rapamycin activation mediate sleep dysfunction in a mouse model of tuberous sclerosis complex, Neurobiol Dis, 2019, Oct 9;134:104615 PMID: 31605778
- Obara K, .et al. Assessment of Inhibitory Effects of Hypnotics on Acetylcholine-Induced Contractions in Isolated Rat Urinary Bladder Smooth Muscle, Biol Pharm Bull, 2019, 42(2):280-288 PMID: 30713259
- James B Jaggard, .et al. Hypocretin underlies the evolution of sleep loss in the Mexican cavefish, eLife, 2018, 7: e32637 PMID: 29405117
- Skillman B, .et al. Quantification of suvorexant in blood using liquid chromatography-quadrupole/time of flight (LC-Q/TOF) mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2018, Aug 1;1091:87-95 PMID: 29859493
- Clark L, .et al. On the use of Pichia pastoris for isotopic labeling of human GPCRs for NMR studies, J Biomol NMR, 2018, Aug;71(4):203-211 PMID: 30121871
- Sullinger S, .et al. Identification of Suvorexant in Urine Using Liquid Chromatography-Quadrupole/Time-of-Flight Mass Spectrometry (LC-Q/TOF-MS), J Anal Toxicol, 2017, Apr 1;41(3):224-229 PMID: 28035034
- Carson M, .et al. Quantification of suvorexant in urine using gas chromatography/mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2017, Jan 1;1040:289-294 PMID: 27825624
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Sitaxsentan sodium (TBC-11251)

Catalog No. A11564
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ETA receptor 拮抗剂

Sitaxsentan sodium (TBC-11251)是一种选择性内皮素受体A拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM。了解更多

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Tolvaptan

Catalog No. A11594
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vasopressin receptor 2 拮抗剂

Tolvaptan是一种选择性的竞争性精氨酸加压素受体2拮抗剂，IC50为1.28μM。了解更多

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MPEP

Catalog No. A12589
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mGlu5 receptor 拮抗剂

MPEP是mGlu5受体亚型（IC50 = 36 nM）的有效且高度选择性的非竞争性拮抗剂，并且是mGlu4受体的正构构调节剂。了解更多

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SB-408124

Catalog No. A11567
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OX Receptor 拮抗剂

SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。了解更多

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MDV3100

Catalog No. A10562
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Androgen receptor 拮抗剂

MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。了解更多

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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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JTC-801

Catalog No. A11076
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Opioid Receptor 拮抗剂

JTC-801是nociceptin receptor（也称为ORL-1受体）的选择性拮抗剂。了解更多

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- Lihao Gu, .et al. 10-Hydroxy-2-Decenoic Acid in Royal Jelly Extract Induced Both Filaggrin and Amino Acid in a Cultured Human Three-Dimensional Epidermis Model, Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. Brain opioid and nociceptin receptors are involved in regulation of bombesin-induced activation of central sympatho-adrenomedullary outflow in the rat, Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671

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