“alpha ergocryptine”的搜索结果
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5-alpha reductase 抑制剂
β-Sitosterol是一种植物甾醇,与胆固醇具有相似的化学结构。
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Estrogen receptor degrader
Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
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estrogen receptor degrader
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
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5 alpha-reductase inhibitor
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2.
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PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
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estrogen receptor (ERα) antagonist
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
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Androgen 拮抗剂
17 alpha-propionate是一种新型的局部和外周选择性雄激素拮抗剂。
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aromatase inhibitor
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
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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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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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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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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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