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搜索结果：“ab fubinaca”

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Abacavir

Catalog No. A11115
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Transcriptase 抑制剂

Abacavir是一种核苷类似物逆转录酶抑制剂（NRTI）；鸟苷类似物用于治疗艾滋病毒和艾滋病。了解更多

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Clofarabine

Catalog No. A10228
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DNA/RNA Synthesis 抑制剂

Clofarabine具有抗肿瘤活性的第二代嘌呤核苷类似物。了解更多

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- Xie J, .et al. Optimization of a clofarabine-based drug combination regimen for the preclinical evaluation of pediatric acute lymphoblastic leukemia, Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Fludarabine Phosphate (Fludara)

Catalog No. A10395
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Fludarabine Phosphate (Fludara)是一种用于治疗血液恶性肿瘤(血细胞癌，如白血病和淋巴瘤)的化疗药物。氟达拉滨通过干扰核糖核苷酸还原酶和dna聚合酶来抑制DNA合成。它对分裂细胞和静止细胞都有活性。了解更多

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Fludarabine (Fludara)

Catalog No. A10396
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STAT 抑制剂

Fludarabine或fludarabine(fludara)是一种用于治疗血液恶性肿瘤(血细胞癌，如白血病和淋巴瘤)的化疗药物。Fludarabine通过干扰核糖核苷酸还原酶和DNA聚合酶来抑制DNA合成。它对分裂细胞和静止细胞都有活性。了解更多

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- Irene Dell'Anno, .et al. Drug-repositioning screening identified fludarabine and risedronic acid as potential therapeutic compounds for malignant pleural mesothelioma, Invest New Drugs, 2020, Dec 9 PMID: 33300108
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Lopinavir (ABT-378)

Catalog No. A10537
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HIV Protease 抑制剂

Lopinavir (ABT-378)是HIV蛋白酶的抑制剂。了解更多

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Metformin HCl

Catalog No. A10573
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Metformin HCl降低肝细胞中高血糖症，主要通过抑制肝糖原的产生（肝脏糖异生作用)发挥作用。了解更多

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- Matthew A Schaller, .et al. Ex vivo SARS-CoV-2 infection of human lung reveals heterogeneous host defense and therapeutic responses, JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. In vitro infection of human lung tissue with SARS-CoV-2: Heterogeneity in host defense and therapeutic response, bioRxiv, 2021, January 21
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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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Rifabutin

Catalog No. A10790
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RNA polymerase 抑制剂

Rifabutin是一种主要用于治疗肺结核的杀菌抗生素。它的作用是基于阻断细菌的DNA依赖性RNA聚合酶。了解更多

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- Matt D Johansen, .et al. Rifabutin is bactericidal against intracellular and extracellular forms of Mycobacterium abscessus, Antimicrob Agents Chemother, 2020, Aug 17;AAC.00363-20 PMID: 32816730
- Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Dinah Binte Aziz, .et al. Rifabutin Is Active against Mycobacterium abscessus Complex, Antimicrob Agents Chemother, 2017, Jun; 61(6): e00155-17 PMID: 28396540
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Chlormezanone (Trancopal)

Catalog No. A10201
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Chlormezanone (Trancopal)是一种非苯二氮卓类药物，用于治疗焦虑症。已经建议将其用于治疗肌肉痉挛。氯甲酮与中央苯并二氮杂receptor受体结合，后者与GABA受体发生变构作用。这增强了抑制性神经递质GABA的作用，增强了对网状激活系统的抑制作用，并阻断了在刺激网状通路后发生的皮质和边缘觉醒。了解更多

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Dabrafenib (GSK2118436A)

Catalog No. A11381
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Raf 抑制剂

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- 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
- Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- 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
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Crotamiton

Catalog No. A10243
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Crotamiton是一种用作杀ab药（用于治疗sc疮）和一般止痒药（抗瘙痒药）的药物。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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Clarithromycin

Catalog No. A10225
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cytochrome P4503A4 抑制剂

Clarithromycin是一种大环内酯类抗生素。它通过干扰细菌的蛋白质合成来防止细菌生长。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
- 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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GNF 2

Catalog No. A11439
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Bcr-Abl 抑制剂

GNF 2是一种Bcr-abl抑制剂，在表达Bcr-abl的细胞中抑制增殖并诱导凋亡。了解更多

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Ginkgolide A

Catalog No. A11739
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Ginkgolide A是银杏的提取物，是γ-氨基丁酸(GABA)拮抗剂，Ki为14.5 μM。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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Emtricitabine

Catalog No. A10349
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NRT 抑制剂

Emtricitabine是一种用于治疗HIV感染的核苷逆转录酶抑制剂 (NRTI) 。了解更多

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CP 945598 HCl (Otenabant HCl)

Catalog No. A11942
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CB1 拮抗剂

CP 945598 HCl (Otenabant HCl)是一种有效且高度选择性的CB1拮抗剂。了解更多

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Zotarolimus

Catalog No. A11950
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mTOR 抑制剂

Zotarolimus是一种免疫抑制剂，可以抑制FKBP-12结合的IC50为2.8nM。。它是雷帕霉素的半合成衍生物。它设计用于以磷酸胆碱为载体的支架。了解更多

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Dopamine hydrochloride

Catalog No. A10331
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Dopamine hydrochloride (abbreviated as DA)是儿茶酚胺家族中的一种简单的有机化学物质，是一种单胺类神经递质，一种由神经细胞释放以向其他神经细胞发送信号的化学物质。了解更多

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Furosemide

Catalog No. A10412
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Furosemide是GABAA受体的非竞争性拮抗剂，对含α6受体的选择性比含α1受体高约100倍。了解更多

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Gabapentin

Catalog No. A10413
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Gabapentin (Neurontin)是一种药剂，特别是加巴类似物。了解更多

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Retigabine (Ezogabine)

Catalog No. A11922
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Retigabine是一种新型的抗痉挛剂，在大范围的惊厥模型具有活性。其发挥活性的机制主要是开放神经元的KCNQ2-5电压门控钾离子通道。了解更多

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- Sotatsu Tonomura, .et al. Function of KCNQ2 channels at nodes of Ranvier of lumbar spinal ventral nerves of rats, Mol Brain, 2022, Jul 20;15(1):64 PMID: 35858950
- Vigil FA, .et al. Prevention of brain damage after traumatic brain injury by pharmacological enhancement of KCNQ (Kv7, ??M-type??) K+ currents in neurons, J Cereb Blood Flow Metab, 2019, Jul 4:271678X19857818 PMID: 31272312
- Joseph Lombardo, .et al. Nonreciprocal mechanisms in up- and downregulation of spinal motoneuron excitability by modulators of KCNQ/Kv7 channels, J Neurophysiol, 2016, Nov 1; 116(5): 2114-2124 PMID: 27512022
- Sonya M. Bierbower, .et al. Augmentation of M-Type (KCNQ) Potassium Channels as a Novel Strategy to Reduce Stroke-Induced Brain Injury, J Neurosci, 2015, Feb 4; 35(5): 2101-2111 PMID: 25653366
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Rimonabant (SR141716)

Catalog No. A11547
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Rimonabant是CB1的选择性拮抗剂，在hCB1转染的HEK 293膜中的IC50为13.6 nM，EC50为17.3 nM。了解更多

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Gabapentin Hydrochloride

Catalog No. A10414
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Gabapentin Hydrochloride是一种加巴类似物。了解更多

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Laquinimod (ABR-215062)

Catalog No. A11128
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Laquinimod (ABR-215062) 是有效的免疫调节剂。了解更多

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Troxacitabine (SGX-145)

Catalog No. A11232
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Troxacitabine (SGX-145)是具有抗癌活性的核苷类似物。了解更多

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Aripiprazole (Abilify)

Catalog No. A11801
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5-HT1A receptor 激动剂

Aripiprazole (Abilify)是人5-HT1A受体部分激动剂，Ki为4.2 nM。了解更多

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- Jaime Osuna-Luque, .et al. Behavioral Mechanisms That Depend on Dopamine and Serotonin in Caenorhabditis elegans Interact With the Antipsychotics Risperidone and Aripiprazole, J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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Loteprednol Etabonate

Catalog No. A10539
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Loteprednol Etabonate是一种眼科皮质类固醇。它被用作抗炎剂。了解更多

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Phenytoin (Lepitoin)

Catalog No. A10721
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Phenytoin (Lepitoin)是钠通道蛋白抑制剂。了解更多

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Primidone (Mysoline)

Catalog No. A10754
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Primidone (Mysoline)是抗惊厥药。增强GABAA受体功能。了解更多

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Terbinafine hydrochloride (Lamisil)

Catalog No. A10912
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Terbinafine hydrochloride (Lamisil)是烯丙胺类抗真菌药的一种，是通过角鲨烯环氧酶抑制作用合成麦角固醇的特异性抑制剂。了解更多

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Otamixaban (FXV 673)

Catalog No. A11517
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factor Xa 抑制剂

Otamixaban (FXV 673)是一种静脉内直接因子Xa抑制剂。了解更多

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- Tim Hempel, .et al. Synergistic inhibition of SARS-CoV-2 cell entry by otamixaban and covalent protease inhibitors: preclinical assessment of pharmacological and molecular properties, Chemical Science, 2021, 12, 12600-12609
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Ivabradine HCl (Procoralan)

Catalog No. A11868
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Ivabradine Hydrochloride,也称为S-16257，是缓动剂伊伐布雷定的盐酸盐制剂。了解更多

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Tonabersat (SB-220453)

Catalog No. A11593
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gap-junction modulator

Tonabersat (SB-220453)是一种新颖的苯并吡喃衍生物，是一种gap-junction调节剂。了解更多

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Ixabepilone

Catalog No. A11449
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microtubule 抑制剂

Ixabepilone是epothilone B类似物。了解更多

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- Dong-Sheng Cao, .et al. A Multi-Scale Systems Pharmacology Approach Uncovers the Anti-Cancer Molecular Mechanism of Ixabepilone, Eur J Med Chem, 2020, Aug 1;199:112421 PMID: 32428794
- Hoque M, .et al. Changes in cell morphology guide identification of tubulin as the off-target for protein kinase inhibitors, Pharmacol Res, 2018, Aug;134:166-178 PMID: 29944980
- APRIL L. RISINGER, .et al. Breast Cancer Cell Lines Exhibit Differential Sensitivities to Microtubule-targeting Drugs Independent of Doubling Time, Anticancer Res, 2015, Nov; 35(11): 5845-5850. PMID: 26504006
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Cevipabulin (TTI-237)

Catalog No. A12591
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Cevipabulin (TTI-237)是一种抗微管剂，是三唑并嘧啶衍生物的合成小分子，具有潜在的抗肿瘤活性。TTI-237具有不同于其他长春花生物碱化合物作用的新颖作用机理，可在长春花部位特异性结合微管蛋白，并促进微管蛋白聚合成微管。了解更多

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(+)-Bicuculline

Catalog No. A12590
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GABAA 拮抗剂

(+)-Bicuculline是一种经典的GABAA拮抗剂。了解更多

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- Maryam Adenike Salaudeen, .et al. Anticonvulsant Activity of Tapinanthus dodoneifolius (DC.) Danser in Chicks and Mice: A Potential Source of Novel Anticonvulsant Agent, J Pharmacy and Drug Innovations, 2022, 3(4)
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Abarelix Acetate

Catalog No. A12613
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GnRH 拮抗剂

Abarelix acetate是一种合成的肽促性腺激素释放激素受体（GnRH）拮抗剂。了解更多

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Ombrabulin

Catalog No. A12654
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Ombrabulin是康维他汀A4的合成水溶性类似物，源自南非柳树灌木（Combretum caffrum），具有潜在的破坏血管和抗肿瘤活性。了解更多

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Palifosfamide

Catalog No. A12691
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Palifosfamide是具有潜在抗肿瘤活性的合成芥末化合物。了解更多

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Sabutoclax

Catalog No. A12823
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Bcl-2 抑制剂

Sabutoclax (BI-97C1)是pan-Bcl-2抑制剂，包括Bcl-xL，Bcl-2，Mcl-1和Bfl-1，IC50分别为0.31 μM，0.32 μM，0.20 μM和0.62 μM。了解更多

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- Christopher D. Graham, .et al. BH3 mimetics suppress CXCL12 expression in human malignant peripheral nerve sheath tumor cells, Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968
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PP1

Catalog No. A12724
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Src 抑制剂

PP1是Src家族酪氨酸激酶的有效抑制剂。抑制p56lck和p59fynT（IC50值分别为5和6 nM）。在ZAP-70和JAK2上显示的选择性> 8000倍。还适度抑制p38，CSK，PDGF受体，RET衍生的癌蛋白，c-Kit和Bcr-Abl。了解更多

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SGI-110 (Guadecitabine)

Catalog No. A12744
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DNMT 抑制剂

SGI-110 (Guadecitabine)是第二代DNA次甲基化剂。了解更多

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Ouabain

Catalog No. A12755
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a-K-ATPase 抑制剂

Ouabain是一种选择性的Na+，K+-ATPase抑制剂。了解更多

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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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Crisaborole (AN2728)

Catalog No. A12776
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PDE4 抑制剂?

AN2728是一种局部给药的含硼抗炎化合物，可抑制PDE4活性，从而抑制TNFalpha，IL-12，IL-23和其他细胞因子的释放。抑制PDE4的 IC50 值为0.49 μM。了解更多

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Sapacitabine (CYC682)

Catalog No. A12801
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Sapacitabine (CYC682)是一种口服生物可用的嘧啶类似物前药，具有潜在的抗肿瘤活性。了解更多

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- Sally L George, .et al. Therapeutic vulnerabilities in the DNA damage response for the treatment of ATRX mutant neuroblastoma, EBioMedicine, 2020, Aug 23;59:102971 PMID: 32846370
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Mirabegron

Catalog No. A12861
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β3 adrenergic receptor activator

Mirabegron是一种选择性的beta3-adrenoceptor（β3肾上腺素受体）激动剂，EC50为22.4 nM。是有效的膀胱松弛药和糖尿病药物。了解更多

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- Bhavik Patel, .et al. Combination drug therapy against OAB normalizes micturition parameters and increases the release of nitric oxide during chemically induced cystitis, Pharmacol Res Perspect, 2020, 8 (1), e00564 PMID: 32030913
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Razaxaban

Catalog No. A12870
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factor Xa 抑制剂

Razaxaban是凝血因子Xa的选择性，有效和口服生物利用抑制剂。了解更多

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Letaxaban (TAK-442)

Catalog No. A12871
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factor Xa 抑制剂

Letaxaban (TAK-442)是一种有效的，选择性的，口服活性的Xa抑制剂，是一种四氢嘧啶-2（1H）-衍生物。TAK-442在贫血小板的人[半最大抑制浓度（IC（50））：53 nM，TAK-442]和大鼠（IC（50）：32 nM，TAK-442）血浆中抑制内源性FXa活性。了解更多

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Rivaroxaban Diol

Catalog No. A12411
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Rivaroxaban Diol是恶唑烷酮衍生物，经优化可抑制凝血酶原酶复合物中结合的游离因子Xa和因子Xa。了解更多

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