“alpha ergocryptine”的搜索结果
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5α-Pregnane-3β,6α-diol-20-one is a mitogenic metabolite of progesterone, and it can be produced in starved androgen-responsive prostate cancer cells.
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ERα degrader
PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader.
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HIF-2α inhibitor
HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay. IC50 value: ?? 500 nM Target: HIF-2α.
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ERRα inverse agonist
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
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Fmoc-Ser(O-α-D-GalNAc(OAc)3)-OH is a drug for cancer.
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type II PDGFRα kinase inhibitor
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
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IFN-α and IFNAR interaction inhibitor
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
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ERRα Degrader
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
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13-atom linker PROTAC
SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16??nM, but is far less effective at degrading p38δ (DC50=299?nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5??M.
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modulator of estrogen receptor ER-alpha36
SNG-1153 is a modulator of estrogen receptor ER-alpha36.
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alpha2-Adrenergic receptor agonist
Flutonidine is an alpha2-Adrenergic receptor agonist.
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human-specific STING agonist
STING agonist-1 (G10) is a novel human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses.
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Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays.
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HIF-2alpha inhibitor
PT2977 is HIF-2alpha inhibitor with an IC50 of 9 nM.
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Integrin alpha4beta1 抑制剂
BIO-1211是整联蛋白alpha4beta1抑制剂。
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Estrogen receptor 激动剂
(R)-Equol是ER&alpha和ER&beta的激动剂,Kis分别为27.4和15.4 nM。
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- Gao X, .et al. Dual Function of a Novel Bacterium, Slackia sp. D-G6: Detoxifying Deoxynivalenol and Producing the Natural Estrogen Analogue, Equol, Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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αV integrins 抑制剂
CWHM 12可以抑制所有5个alpha V整联蛋白。CWHM12不仅以与遗传删除方法相同的方式预防纤维化,还可以防止肝和肺中现有纤维化的进展,并逆转了由纤维化对这些器官造成的某些损害。
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Nrf2 activator
Oltipraz抑制HIF-1alpha活性和HIF-1alpha依赖性肿瘤生长,这可能是由于S6K1抑制结合H2O2清除作用导致HIF-1alpha稳定性降低所致。
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Bmi1/Ring1A 抑制剂
PRT 4165是Bmi1/Ring1A抑制剂,Bmi1/Ring1A是多梳抑制复合物1(PRC1)的亚基。它可以防止Bmi1/Ring1A介导的泛素化和拓扑异构酶2alpha的药物诱导降解。
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Cell adhesion 抑制剂
K-7174 dihydrochloride是一种新型的细胞粘附抑制剂;抑制由IL-1beta或TNF-alpha诱导的血管细胞粘附分子1(VCAM-1)的表达。
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Cell adhesion 抑制剂
K-7174是一种新型的细胞粘附抑制剂;抑制由IL-1beta或TNF-alpha诱导的血管细胞粘附分子1(VCAM-1)的表达。
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PI3K 抑制剂
PI-103 Hydrochloride是对重组PI3K亚型p110alpha(IC50 = 2 nM),p110beta(IC50 = 3 nM),p110delta(IC50 = 3 nM)和p110gamma(IC50 = 15 nM)具有低IC50值的有效抑制剂,对mTOR的效力较低/DNA-PK,IC50为30 nM/23 nM。
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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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Topo II 抑制剂
BNS-22是Topo II的有效小分子抑制剂(Topo II alpha和Topo II beta的IC50分别为2.8 M和0.42 M)。
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alpha2-adrenoceptor 激动剂
Dexmedetomidine hydrochloride是美托咪啶的活性异构体,它充当有效的,高度选择性的α2-AR(α2-肾上腺素受体)激动剂。
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HIF-1alpha 抑制剂
PX-478 HCl是HIF-1alpha抑制剂,也是具有潜在抗肿瘤活性小分子。PX-478对已建立的人类肿瘤异种移植物具有出色的活性,可提供具有HIF-1水平正相关的延长的生长延迟的肿瘤消退。PX-478是高度水溶性的分子,具有良好的i.v.,i.p.和p.o.抗肿瘤活性。
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alpha1/beta adrenergic receptors 拮抗剂
Labetalol HCl是选择性α1-肾上腺素能受体和非选择性β-肾上腺素能受体的双重拮抗剂。
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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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α4β1/α4β7 integrin 拮抗剂
Firategrast (SB 683699)是一种口服可生物利用的alpha4 beta1/alpha4 beta7整联蛋白拮抗剂,旨在减少淋巴细胞向中枢神经系统(CNS)的运输。
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- Higuchi S, .et al. Inhibition of the integrin signal constitutes a mouse iPS cell niche, Dev Growth Differ, 2016, Sep;58(7):586-99 PMID: 27633818
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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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Lidocaine (Alphacaine)是一种麻醉剂和Ib类抗心律失常药。在失活状态下阻断电压门控钠通道。
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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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dual 5alpha-reductase 抑制剂
Dutasteride (Avodart)是双重的5-a还原酶抑制剂,可抑制睾丸激素转化为二氢睾丸激素(DHT)。
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- Makoto Ishikawa, .et al. Additive neuroprotective effects of 24(S)-hydroxycholesterol and allopregnanolone in an ex vivo rat glaucoma model, Sci Rep, 2018, 8: 12851 PMID: 30150786
- Makoto Ishikawa, .et al. TSPO activation modulates the effects of high pressure in a rat ex vivo glaucoma model, Neuropharmacology, 2016, Dec; 111: 142-159 PMID: 27596950
- Makoto Ishikawa, .et al. Neurosteroids Are Endogenous Neuroprotectants in an Ex Vivo Glaucoma Model, Invest Ophthalmol Vis Sci., 2014, 55(12): 8531-8541 PMID: 25406290
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PI3K 抑制剂
A66的S对映异构体是PI 3-激酶(PIK3CA)的p110alpha亚型的有效抑制剂。无细胞试验中IC50为32 nM,作用于p110α比作用于其他I类PI3K亚型选择性高100多倍。
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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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α-2,3-sialyltransferase inhibitor
α-2,3-sialyltransferase-IN-1 (Lith-O-Asp analog) is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM.
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p38α inhibitor
p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
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α-Tocopherol phosphate is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
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alpha-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
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antioxidant
α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
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TNF-α inhibitor
TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.
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MAPK14 inhibitor
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
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α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
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alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
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antifungal
(L)-alpha-Terpineol is a monoterpene alcohol. It is one of the components responsible for the antifungal activity of Melaleuca alternifolia (tea tree) essential oil. α-Terpineol may be used in the synthesis of α-terpinyl esters of acetic acid and acetic anhydride via lipase-mediated esterification.
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antioxidation agent
DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB.
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GABAA α5 inverse agonist
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively).
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(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
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ligand for the α2δ subunit of voltage-gated calcium channels
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
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(2S)-Octyl-α-hydroxyglutarate ((2S)-Octyl-2-HG) is a modified form of S-isomer 2-Hydroxyglutarate.
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