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LY2608204

Catalog No. A11406
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GK activator

LY2608204是治疗2型糖尿病的有效药物。是葡萄糖激酶（GK）活化剂，EC50为42 nM。了解更多

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JNJ 26854165

Catalog No. A10491
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p53 activator

JNJ-26854165是P53激活剂之一，与AraC或阿霉素协同作用，诱导P53介导的凋亡，可能为急性白血病的治疗提供新的治疗途径。了解更多

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- Chang SJ, .et al. Proteomic investigating the cooperative lethal effect of EGFR and MDM2 inhibitors on ovarian carcinoma, Arch Biochem Biophys, 2018, Jun 1;647:10-32 PMID: 29655550
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A-769662

Catalog No. A11071
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AMPK 激活剂

A-769662是AMP激活的蛋白激酶（AMPK）的新激活剂。了解更多

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- Daniel Missailidis, .et al. Dysregulated Provision of Oxidisable Substrates to the Mitochondria in ME/CFS Lymphoblasts, Int J Mol Sci., 2021, Feb; 22(4): 2046 PMID: 33669532
- Lieberthal W, .et al. AMPK-mediated activation of Akt protects renal tubular cells from stress-induced apoptosis in vitro and ameliorates ischemic AKI in vivo, Am J Physiol Renal Physiol, 2019, 2019 PMID: 30995114
- Kikuchi H, .et al. Failure to sense energy depletion may be a novel therapeutic target in chronic kidney disease, Kidney Int, 2018, Nov 13. pii: S0085-2538(18)30635-5 PMID: 30455054
- Schneider H, .et al. AMPK Dilates Resistance Arteries via Activation of SERCA and BKCa Channels in Smooth Muscle, Hypertension, 2015, Jul;66(1):108-16 PMID: 26034200
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Dimebon 2HCl

Catalog No. A10312
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Neuroprotectant

Dimebon dihydrochloride是一种非选择性的抗组胺药，具有增强认知能力。了解更多

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Apoptosis Activator 2

Catalog No. A11944
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Apoptosis Activator

Apoptosis Activator 2 强烈诱导caspase-3激活，PARP裂解和DNA片段化，导致细胞破坏（依赖Apaf-1），IC50为约4μM，对HMEC，PREC或MCF-10A细胞无效。了解更多

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CK-1827452 (Omecamtiv mecarbil)

Catalog No. A11206
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Myosin activator

CK-1827452 (Omecamtiv mecarbil)是选择性的心脏特异性肌球蛋白激活剂。了解更多

Product Citations (11)

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- Oleg Lookin, .et al. Omecamtiv mecarbil attenuates length-tension relationship in healthy rat myocardium and preserves it in monocrotaline-induced pulmonary heart failure, Clin Exp Pharmacol Physiol, 2021, Aug 29 PMID: 34459025
- Gabor A. Fulop, .et al. Omecamtiv mecarbil evokes diastolic dysfunction and leads to periodic electromechanical alternans, Basic Res Cardiol, 2021, 116(1): 24 PMID: 33844095
- Wanjian Tang, .et al. Dilated cardiomyopathy mutation in the converter domain of human cardiac myosin alters motor activity and response to omecamtiv mecarbil, J Biol Chem, 2019, October 2 PMID: 31578282
- Thinh T. Kieu, .et al. Omecamtiv Mecarbil Slows Myosin Kinetics in Skinned Rat Myocardium at Physiological Temperature, Biophysical Journal, 2019, 2019 PMID: 31103235
- Alexandre J. S. Ribeiro, .et al. Multi-Imaging Method to Assay the Contractile Mechanical Output of Micropatterned Human iPSC-Derived Cardiac Myocytes, Circ Res, 2017, May 12; 120(10): 1572-1583 PMID: 28400398
- Anja M. Swenson, .et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle, J Biol Chem, 2017, Mar 3; 292(9): 3768-3778 PMID: 28082673
- Nánási P Jr, .et al. Omecamtiv mecarbil activates ryanodine receptors from canine cardiac but not skeletal muscle, Eur J Pharmacol, 2017, Aug 15;809:73-79 PMID: 28506910
- Horv??th B, .et al. Frequency-dependent effects of omecamtiv mecarbil on cell shortening of isolated canine ventricular cardiomyocytes, Naunyn Schmiedebergs Arch Pharmacol, 2017, Dec;390(12):1239-1246 PMID: 28940010
- Szentandrassy N, .et al. Dose-dependent electrophysiological effects of the myosin activator omecamtiv mecarbil in canine ventricular cardiomyocytes, J Physiol Pharmacol, 2016, Aug;67(4):483-489 PMID: 27779469
- L Nagy, .et al. The novel cardiac myosin activator omecamtiv mecarbil increases the calcium sensitivity of force production in isolated cardiomyocytes and skeletal muscle fibres of the rat, Br J Pharmacol, 2015, Sep; 172(18): 4506-4518 PMID: 26140433
- Larissa Butler, .et al. Enhanced characterization of contractility in cardiomyocytes during early drug safety assessment, Toxicol Sci, 2015, Jun;145(2):396-406 PMID: 25820236
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RITA (NSC 652287)

Catalog No. A11931
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p53 activator

RITA，也称为NSC 652287，是一种三环噻吩衍生物，与MDM2结合，破坏MDM2-p53复合物，随后激活p53，并诱导凋亡。了解更多

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- M Kobayashi, .et al. Nutlin-3a Suppresses Poly (ADP-ribose) Polymerase 1 by Mechanisms Different From Conventional PARP1 Suppressors in a Human Breast Cancer Cell Line, Oncotarget, 2020, May 5;11(18):1653-1665 PMID: 32405340
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PAC-1

Catalog No. A11090
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Caspase activator

PAC-1是procaspase-3的激活剂，可诱导癌细胞凋亡，EC50为2.08μM。了解更多

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- 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
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AMG-073 HCl (Cinacalcet HCl)

Catalog No. A10219
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CaSR activator

AMG-073 HCl（Cinacalcet HCl）是一种用于治疗甲状旁腺功能亢进的化合物，称为拟钙剂，通过增加甲状旁腺钙敏感受体（CaR）对细胞外钙的敏感性来减少甲状旁腺激素（PTH）的合成和分泌。了解更多

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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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SRT1720 HCl

Catalog No. A10862
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SIRT1 Activator

SRT1720 HCl是一种抑制剂，旨在作为瑟土因亚型SIRT1的小分子活化剂。了解更多

Product Citations (7)

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- Eleni Pitsillou, .et al. Interaction of small molecules with the SARS-CoV-2 main protease in silico and in vitro validation of potential lead compounds using an enzyme-linked immunosorbent assay, Comput Biol Chem, 2020, 89: 107408 PMID: 33137690
- Jie Ren, .et al. Melatonin prevents chronic intermittent hypoxia-induced injury by inducing sirtuin 1-mediated autophagy in steatotic liver of mice, Sleep Breath, 2018, Nov 8 PMID: 30411173
- Rowlands BD, .et al. Acetate metabolism does not reflect astrocytic activity, contributes directly to GABA synthesis, and is increased by silent information regulator 1 activation, J Neurochem, 2017, Mar;140(6):903-918 PMID: 27925207
- Adam Khader, .et al. SRT1720, a sirtuin 1 activator, attenuates organ injury and inflammation in sepsis, J Surg Res, 2017, Nov;219:288-295 PMID: 29078895
- Adam Khader, .et al. Sirtuin 1 Stimulation Attenuates Ischemic Liver Injury and Enhances Mitochondrial Recovery and Autophagy, Crit Care Med, 2016, Aug; 44(8): e651-e663 PMID: 26963320
- Benjamin D. Rowlands, .et al. Silent information regulator 1 modulator resveratrol increases brain lactate production and inhibits mitochondrial metabolism, whereas SRT1720 increases oxidative metabolism., J Neurosci Res., 2015, Jul;93(7):1147-56 PMID: 25677687
- Khader A, .et al. Sirtuin 1 activation stimulates mitochondrial biogenesis and attenuates renal injury after ischemia-reperfusion., Transplantation, 2014, 98(2):148-56 PMID: 24918615
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Resveratrol

Catalog No. A10785
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Resveratrol具有广泛的靶标，包括环氧合酶（COX，IC50 = 1.1μM），脂氧合酶（LOX，IC50 = 2.7μM），激酶，sirtuins和其他蛋白质。它具有抗癌，抗炎，降低血糖和其他有益的心血管作用。了解更多

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- Ha T. Tran, .et al. Resveratrol ameliorates the chemical and microbial induction of inflammation and insulin resistance in human placenta, adipose tissue and skeletal muscle, PLoS One, 2017, 12(3): e0173373 PMID: 28278187
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Tenovin-1

Catalog No. A11943
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p53 activator

Tenovin-1是p53转录活性的小分子激活剂，可防止MDM2介导的p53降解。了解更多

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