“alpha ergocryptine”的搜索结果
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1alpha, 25-Dihydroxy VD2-D6是氘化的维生素D形式。
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1alpha, 24, 25-Trihydroxy VD2是维生素D类似物。
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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。
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PPAR 激动剂
Rosiglitazone (BRL-49653)是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。
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Anti-Diabetic Agent
Acarbose是一种肠道alpha-glucosidase抑制剂,用于治疗2型糖尿病以及某些国家的前驱糖尿病。
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PPAR alpha/gamma agonist
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively.
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PPARα/γ dual agonist
Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
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PPAR-α antagonist
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively.
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PPARα antagonist
GW 6471 is a potent PPARα antagonist.
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dual α/γ PPAR activator
Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
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LXRα and full LXRβ agonist
LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
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PPAR agonist
Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).
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PPARα/PPARγ dual agonist
LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively.
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HSP90??/HSP90?? inhibitor
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
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ACCA inhibitor
TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
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Terphenyllin is a naturally abundant p-terphenyl metabolite isolated from the coral derived fungus Aspergillus candidus, has signi?cant α-glucosidase inhibitory activity.
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Tacalcitol通过调节钙促进正常的骨骼发育。
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1alpha-Hydroxy VD4可有效诱导单核细胞白血病U937,P39/TSU和P31/FUJ细胞分化。
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alpha-glucosidase 抑制剂
Voglibose是缬氨酰胺的N取代衍生物,对α-葡萄糖苷酶具有出色的抑制活性,并且对高血糖症和由高血糖症引起的各种疾病具有抗药性。
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alpha-glucosidase I 抑制剂
Celgosivir是一种用于潜在治疗HCV感染的α-葡萄糖苷酶I抑制剂。
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HSP90 抑制剂
CUDC-305 (DEBIO-0932) 是一种新型的热休克蛋白90(HSP90)抑制剂,对HSP90 alpha/beta具有很强的亲和力,对HSP90α和HSP90β的IC50值分别为100和103nM。具有很高的口服生物利用度,并且对多种癌细胞系均具有强大的抗增殖活性(平均IC50为220 nmol/L)。包括许多对护理标准(SOC)药物有抵抗力的非小细胞肺癌(NSCLC)细胞系。
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- Aykut Ozgur, .et al. Debio-0932, a second generation oral Hsp90 inhibitor, induces apoptosis in MCF-7 and MDA-MB-231 cell lines, Mol Biol Rep, 2021, Apr;48(4):3439-3449 PMID: 33999319