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GPCR / G Protein /
Orexin Receptors

Orexin Receptors

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Nemorexant

Catalog No. A12685
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Orexin receptor antagonist

Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively. 了解更多

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GSK1059865

Catalog No. A12401
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orexin 1 receptor antagonist

GSK1059865 is a potent orexin 1 receptor antagonist. 了解更多

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- 最新产品
TCS-OX2-29 HCl

Catalog No. A17136
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OX2 receptor 拮抗剂

TCS-OX2-29 HCl是一种选择性OX2受体拮抗剂，IC50值为40 nM。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-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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SB-674042

Catalog No. A15233
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OX1 receptor 拮抗剂

SB-674042是有效的选择性非肽orexin OX1受体拮抗剂（Kd = 3.76 nM），对OX1的选择性比OX2受体高100倍。了解更多

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SB-408124 HCl

Catalog No. A15231
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OX Receptor 拮抗剂

SB408124 Hydrochloride是OX1受体的非肽拮抗剂，全细胞和膜的Ki分别为57 nM和27 nM。表现出比OX2受体高50倍的选择性。了解更多

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ACT-335827

Catalog No. A13778
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OX1 拮抗剂

ACT-335827是选择性orexin受体1拮抗剂。了解更多

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Almorexant HCl

Catalog No. A14286
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OX1/OX2 拮抗剂

Almorexant HCl是一种活性双重食欲素受体拮抗剂，对OX1和OX2受体3的IC50为6.6 nM和3.4 nM。了解更多

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- Ryan J Keenan, .et al. Differential sleep/wake response and sex differences following acute suvorexant, MK-1064 and zolpidem administration in the rTg4510 mouse model of tauopathy, Br J Pharmacol, 2022, Jul;179(13):3403-3417 PMID: 35112344
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JNJ-10397049

Catalog No. A14104
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OX2 receptor 拮抗剂

JNJ-10397049是orexin-2受体（OX2R）的有效，选择性且可生物利用的拮抗剂（OX2R的KB = 4.5 nM，OX1R的1.1μM）。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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Almorexant

Catalog No. A12503
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OX 拮抗剂

Almorexant (ACT078573)是一种有效的竞争性双重食欲素1受体(OX1)/orexin 2受体（OX2）拮抗剂，对于OX1和OX2的Ki值分别为1.3和0.17 nM。了解更多

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TCS 1102

Catalog No. A13439
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Dual orexin receptor 拮抗剂

TCS 1102是一种有效的双重食欲素受体拮抗剂（OX2和OX1受体的Ki值分别为0.2和3 nM）。了解更多

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SB 334867

Catalog No. A12786
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OX1 receptor 拮抗剂

SB 334867是一种选择性的非肽orexin OX1受体拮抗剂。对于分别表达人OX1和OX2受体的CHO细胞中的细胞内Ca2 +释放抑制，pKb值为7.2和<5。体内全身给药后，阻断orexin-A诱导的美容和进食。了解更多

Product Citations (1)

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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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SB-649868

Catalog No. A12651
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Orexin 拮抗剂

SB-649868是葛兰素史克（GlaxoSmithKline）开发的一种食欲素OX1和OX 2受体拮抗剂 (作用于 OX1 和 OX2 受体，pKi 分别为 9.4 和 9.5)。。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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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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SB-334867 free base

Catalog No. A16695
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orexin OX1 receptor antagonist

SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. 了解更多

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