“Tutalthromycin second gen”的搜索结果
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estrogen receptor modulator
4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
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oestrogen receptor antagonist
Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
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progesterone receptor agonist
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
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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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estrogen receptor covalent antagonist
H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).
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estrogen receptor modulators
Pipendoxifene hydrochloride is a selective estrogen receptor modulators (SERMs).
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estrogen receptor antagonist
Fulvestrant R enantiomer (ICI 182780 R enantiomer; ZD 9238 R enantiomer; ZM 182780 R enantiomer) is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
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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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nuclear estrogen receptor modulator
Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator.
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selective estrogen receptor modulator (SERM)
Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
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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 β agonist
Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
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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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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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Estrogen receptor antagonist
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
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Glucocorticoid Receptor Antagonist
OP-3633 is a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (IC50 = 29 nM).
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glucocorticoid receptor agonist
Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma.
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selective Estrogen receptor modulator
Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator.
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Glucocorticoid receptor agonist
GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
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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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Desogestrel是一种合成的孕激素,通常用作联合口服避孕药的孕激素成分。
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Estrogen receptor degrader
GDC-0810 (Brilanestrant)是一种口服可生物利用的选择性雌激素受体降解剂(SERD),在耐他莫昔芬的乳腺癌异种移植物中表现出强大的活性。
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Androgen receptor 拮抗剂
Flutamide是一种抗雄激素药物,其活性代谢洛丽塔与Ki值为55nM的雄激素受体结合,可作用于前列腺癌。
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Estrogen receptor 拮抗剂
(E/Z)-4-hydroxy Tamoxifen是他莫昔芬的活性代谢产物,是一种选择性雌激素受体(ER)调节剂,广泛用于乳腺癌的治疗和化学预防治疗。
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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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androgen receptor modulator
GSK-2881078是一种选择性雄激素受体调节剂(SARM),正在针对肌肉萎缩以改善其身体功能的受试者的肌肉生长和力量进行评估。
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estrogen receptor downregulator and 拮抗剂
AZD9496是一种有效的生物选择性雌激素受体下调剂和拮抗剂。
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Androgen Receptor 拮抗剂
EPI-001是雄激素受体(AR)的拮抗剂,它通过与AR的N末端结构域(NTD)共价结合并阻断AR及其剪接变体(转录因子IC50)的转录活性所需的蛋白质相互作用抑制AR NTD反式激活6μM)
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Androgen receptor 拮抗剂
ODM-201是一种有效且完全的人类AR(hAR)拮抗剂,IC50值为26 nM。
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Estrogen receptor 拮抗剂
Endoxifen是他莫昔芬的次生代谢产物。它是负责他莫昔芬在ER阳性乳腺癌中有效性的主要代谢物。Endoxifen Z-isomer抑制hERG, 这种作用具有浓度依赖性, IC50值为1.6μM。
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- Marina Arino Martin, .et al. Photolytic fate of (E)- and (Z)-endoxifen in water and treated wastewater exposed to sunlight, Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. Photodegradation of (E)- and (Z)-Endoxifen in water by ultraviolet light: Efficiency, kinetics, by-products, and toxicity assessment, Water Res, 2019, Dec 29;171:115451 PMID: 31901682
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Estrogen receptor modulator
Toremifene是正在开发中的第二代选择性雌激素受体调节剂(SERM),用于预防骨质疏松症。
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Androgen receptor modulator
MK-0773是一种选择性雄激素受体调节剂(SARMs),是一种4-氮杂-类固醇,在人体中表现出组织选择性(IC50 = 6.6 nM)。
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Estrogen modulator
Bazedoxifene是雌激素受体的第三代选择性调节剂。
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Acetyl Angiotensinogen (1-14), porcine血管紧张素原基因编码的蛋白质被称为血管紧张素原或血管紧张素原的前体。
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androgen-receptor (AR) 拮抗剂
N-desMethyl EnzalutaMide用于治疗涉及雄激素,雌激素和孕激素受体的疾病。
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estrogen receptor modulator
Ospemifene是一种非激素选择性雌激素受体调节剂(SERM)。
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Androgen receptor (AR) modulator
BMS-564929是一种新型,高效,口服活性,非甾体组织选择性雄激素受体(AR)调节剂,结合到雄激素受体,Ki 为 2.11±0.16 nM。该化合物已被推进临床试验,以治疗与年龄相关的功能衰退。
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estrogen receptor modulator
Acolbifene (EM 652,SCH57068)是第四代选择性的estrogen receptor拮抗剂,LC50 值为 22±3 nM。用于预防高乳腺癌女性的乳腺癌。 盐酸阿科比芬与体内雌激素受体结合,阻断雌激素对乳房的作用。 它是选择性雌激素受体调节剂(SERM)的一种。
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- Sumit Bansal, .et al. Inhibition of Human Sulfotransferase 2A1-Catalyzed Sulfonation of Lithocholic Acid, Glycolithocholic Acid, and Taurolithocholic Acid by Selective Estrogen Receptor Modulators and Various Analogs and Metabolites, J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405
- Lirit N. Franks, .et al. Selective Estrogen Receptor Modulators: Cannabinoid Receptor Inverse Agonists with Differential CB1 and CB2 Selectivity, Front Pharmacol, 2016, 7: 503 PMID: 28066250
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Liquiritigenin是一种植物来源的高选择性雌激素受体β激动剂。
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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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Estrogen receptor 拮抗剂
Tamoxifen Citrate是哺乳动物甾醇异构酶的选择性和有效抑制剂。
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- Renu Sudhakar, .et al. Bazedoxifene, a Postmenopausal Drug, Acts as an Antimalarial and Inhibits Hemozoin Formation, Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- 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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Androgen Receptor 拮抗剂
Cyproterone acetate是17-羟孕酮的合成衍生物,可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。
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Androgen Receptor 激动剂
Andarine (GTX-007)是研究性的选择性雄激素受体调节剂(SARM)。
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Estrogen/progestogen Receptor 激动剂
Hexestrol是一种致癌的合成雌激素,可抑制微管聚合和带状结构的形成。它是脂质过氧化的抑制剂。
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Androgen Receptor 拮抗剂
Bicalutamide (Casodex)是一种口服非甾体抗雄激素,用于治疗前列腺癌和多毛症。
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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- 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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Androgen Receptor 拮抗剂
(R)-Bicalutamide是一种活性的竞争性非甾体雄激素受体拮抗剂,对MDA 453细胞的IC50为0.17μM。
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Androgen receptor 拮抗剂
MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。
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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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Androgen Receptor Modulators
Ostarine (MK-2866,GTX-024)是一种雄激素受体调节剂(SARM)。
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