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搜索结果：“jwh 250”

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Imatinib (Gleevec)

Catalog No. A10259
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PDGFR 抑制剂

Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂，抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6，0.1和0.1 μM。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Takafumi Shima, .et al. Glucose transporter-1 inhibition overcomes imatinib resistance in gastrointestinal stromal tumor cells, Oncol Rep, 2022, 47: 7 PMID: 34738628
- 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
- BM Duggan, .et al. RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice, Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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Ketanserin (Vulketan Gel)

Catalog No. A10497
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5-HT2A serotonin receptor 拮抗剂

Ketanserin (Vulketan Gel)是大鼠和人5-HT2A血清素受体拮抗剂，Ki为2.5 nM。了解更多

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Granisetron Hydrochloride

Catalog No. A10437
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5-HT3 receptor 拮抗剂

Granisetron Hydrochloride是血清素5-ht3受体拮抗剂。了解更多

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Phenoxybenzamine hydrochloride

Catalog No. A10719
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α-adrenergic (AR) 拮抗剂/CaM 抑制剂

Phenoxybenzamine hydrochloride是一种细胞可渗透的，非特异性的，不可逆的α-肾上腺素（AR）拮抗剂，也可作为CaM抑制剂。了解更多

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Olanzapine (LY170053)

Catalog No. A10667
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5-HT Receptors/D2 dopamine receptor 拮抗剂

Olanzapine (LY170053)对5-HT2血清素和D2多巴胺受体拮抗剂具有高亲和力。了解更多

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Paliperidone

Catalog No. A10691
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Dopamine Receptor 拮抗剂

Paliperidone (Invega)是一种非典型的抗精神病药。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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Telmisartan

Catalog No. A10905
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AT1 拮抗剂

Telmisartan是一种抑制血管紧张素II AT1受体的血管紧张素II受体拮抗剂。了解更多

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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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LDE225 (NVP-LDE225, Sonidegib)

Catalog No. A10520
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Smo 拮抗剂

LDE225 (NVP-LDE225)是一种强效、选择性和口服生物可利用的平滑(SMO)拮抗剂，通过平滑受体(SMO)的拮抗作用抑制hedgehog (Hh)信号通路。了解更多

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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INCB 3284 dimesylate

Catalog No. A11104
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HCCR2 拮抗剂

INCB 3284 dimesylate是一种有效的选择性hCCR2拮抗剂，对单核细胞趋化因子分子与hCCR2的结合和趋化活性表现出强烈的拮抗作用。了解更多

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Biperiden HCl

Catalog No. A10147
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Muscarinic receptor antagonist

Biperiden HCl是毒蕈碱受体拮抗剂，对M1亚型表现出一定的选择性。了解更多

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Flumazenil

Catalog No. A10397
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Benzodiazepine 拮抗剂

Flumazenil是竞争性抑制GABA/苯二氮卓受体复合物上苯二氮卓识别位点的活性。Flumazenil在一些活性动物模型中是弱部分激动剂，但在人类中很少或没有激动剂活性。了解更多

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Alvimopan (ADL 8-2698)

Catalog No. A11292
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Opioid 拮抗剂

Alvimopan (ADL 8-2698)表现为外周作用的opioid拮抗剂，Alvimopan竞争性结合胃肠道中的mu-opioid receptor。了解更多

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A 740003

Catalog No. A11316
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P2X7 receptor 拮抗剂

A740003是P2X7受体的新型竞争性拮抗剂（人的IC50值= 40 nM，大鼠的IC50值= 18 nM）。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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Asenapine maleate

Catalog No. A10091
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H1 拮抗剂

Asenapine maleate平对多种受体具有高亲和力（pKi），包括5-羟色胺5-HT1A（8.6），5-HT1B（8.4），5-HT2A（10.2），5-HT2B（9.8），5-HT2C（10.5），5 -HT5A（8.8），5-HT6（9.5）和5-HT7（9.9）受体，肾上腺素α1（8.9），α2A（8.9），α2B（9.5）和α2C（8.9）受体，多巴胺D1（ 8.9），D2（8.9），D3（9.4）和D4（9.0）受体以及组胺H1（9.0）和H2（8.2）受体。了解更多

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- Keisuke Obara, .et al. Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles, Biol Pharm Bull, 2021, 44, 1140-1150
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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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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

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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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ICI 118,551 hydrochloride

Catalog No. A13225
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β2 adrenergic 拮抗剂

ICI 118,551 hydrochloride是选择性的β2 adrenergic receptor 拮抗剂,结合 β2，β1 和 β3 肾上腺素能受体的Ki 值分别为 0.7，49.5 和 611 nM。了解更多

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Reversine

Catalog No. A13250
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human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂

Reversine是一种有效的人A3腺苷受体拮抗剂，Ki为0.66μM，是一种泛光A/B/C激酶抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞去分化。了解更多

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- Hazheen K, .et al. BuGZ facilitates loading of spindle assembly checkpoint proteins to kinetochores in early mitosis, J Biol Chem, 2020, August 20
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S1RA (E-52862)

Catalog No. A12504
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sigma-1 receptor 拮抗剂

S1RA是一种选择性sigma-1受体拮抗剂，据报道其结合亲和力为Ki = 17.0±7.0 nM，对sigma-2受体具有选择性，并且对其他170种受体，酶，转运蛋白和离子通道具有选择性。了解更多

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AM251

Catalog No. A12914
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CB1 receptor 拮抗剂

AM251是有效的CB1受体拮抗剂（IC50 = 8 nM，Ki = 7.49 nM），其选择性是CB2受体的306倍。了解更多

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- Potential for pharmacological manipulation of human embryonic stem cells. Br J Pharmacol. 2013 May; 169(2): 269–289.
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SB 399885 HCl

Catalog No. A14102
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5-HT6 拮抗剂

SB 399885 hydrochloride是一种有效的，脑渗透剂和口服活性的SR-6拮抗剂。它对SR-6的选择性比其他血清素受体高200倍（对于人类重组，天然大鼠和天然人类SR-6受体，pKi值分别为9.11、8.81和9.02）。了解更多

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SB225002

Catalog No. A14209
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CXCR2 拮抗剂

SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。了解更多

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BX471

Catalog No. A14409
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CCR1 拮抗剂

BX471是一种有效的选择性非肽CCR1拮抗剂（对于人CCR1，Ki = 1 nM），对CCR1的选择性是CCR2，CCR5和CXCR4的250倍。了解更多

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Flavoxate

Catalog No. A12900
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muscarinic AChR antagonist

Flavoxate结合并抑制毒蕈碱受体，从而通过改变脑干的排尿中心来抑制排尿反射并增加膀胱容量。了解更多

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