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搜索结果：“MK 1775”

“MK 1775”的搜索结果

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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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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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MK-0974 (Telcagepant)

Catalog No. A11255
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CGRP receptor 拮抗剂

MK-0974 (Telcagepant)是人和恒河猴CGRP受体的有效和选择性拮抗剂。了解更多

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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-2894

Catalog No. A11497
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EP4 receptor 拮抗剂

MK-2894是一种高度有效和选择性的第二代EP4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

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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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Vorapaxar (SCH 530348)

Catalog No. A12832
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PAR-1 拮抗剂

Vorapaxar (SCH 530348)是一种有效的口服活性凝血酶受体（PAR-1）拮抗剂，Ki为8.1 nM。了解更多

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- Cansu Tekin, .et al. Macrophage-secreted MMP9 induces mesenchymal transition in pancreatic cancer cells via PAR1 activation, Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. PAR1 signaling on tumor cells limits tumor growth by maintaining a mesenchymal phenotype in pancreatic cancer, Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. Thrombin contributes to protective immunity in pneumonia-derived sepsis via fibrin polymerization and platelet-neutrophil interactions, J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. Plasmin reduces fibronectin deposition by mesangial cells in a protease-activated receptor-1 independent manner, Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. Inflammatory Function of CX3CR1+ CD8+ T Cells in Treated HIV Infection Is Modulated by Platelet Interactions, J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. Elevated Angiopoietin-2 Level in Patients With Continuous-Flow Left Ventricular Assist Devices Leads to Altered Angiogenesis and Is Associated With Higher Non-Surgical Bleeding, Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
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Fosaprepitant dimeglumine

Catalog No. A11069
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neurokinin-1 receptor 拮抗剂

Fosaprepitant是一种选择性的神经激肽-1（NK-1）受体拮抗剂。了解更多

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MK-3697

Catalog No. A12633
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OX2 拮抗剂

MK-3697是一种高效的，口服生物利用的选择性orexin 2受体拮抗剂，Ki值为0.95nM。了解更多

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MK-3207

Catalog No. A15165
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CGRP Receptor 拮抗剂

MK-3207是一种有效且口服可生物利用的CGRP受体拮抗剂（IC50 = 0.12 nM；Ki = 0.024 nM）；对人类AM1，AM2，CTR和AMY3具有高度选择性。了解更多

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MK-1064

Catalog No. A16360
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OX2 拮抗剂

MK-1064是一种有效的，选择性的，口服活性的Orexin OX2受体拮抗剂，可用于治疗失眠。了解更多

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MK-6096 (Filorexant)

Catalog No. A13168
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Orexin receptor 拮抗剂

MK-6096 (Filorexant)是目前正处于失眠临床开发中的口服生物利用型有效且选择性可逆的OX（1）R和OX（2）R拮抗剂。MK-6096表现出对人OX（1）R和OX（2）R的有效结合和拮抗作用（结合时<3 nM，FLIPR中为11 nM），对超过170个受体和酶。了解更多

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MK-2894 sodium salt

Catalog No. A11498
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EP4 antagonist

MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist. 了解更多

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Serlopitant

Catalog No. A21582
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Neurokinin-1 (NK-1) receptor antagonist

Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. 了解更多

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Ubrogepant

Catalog No. A21670
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CGRP antagonist

Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine. 了解更多

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Taranabant racemate

Catalog No. A21699
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CB1 antagonist/inverse agonist

Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1. 了解更多

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