“alpha ergocryptine”的搜索结果
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RXRα antagonist
β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
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testosterone 5-alpha-reductase inhibitor
Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor.
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HIF-2α inhibitor
PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
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Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
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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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eukaryotic DNA polymerase α inhibitor
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM.
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triazole DAGL(α) inhibitor
DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
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Smo allosteric activator
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
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p38α MAPK inhibitor
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
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p38α MAPK inhibitor
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
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p38α MAPK inhibitor
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM.
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PPARα antagonist
GW 6471 is a potent PPARα antagonist.
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p38 MAPK α/β inhibitor
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively.
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5-HT2 receptor antagonist
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
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α4 integrin receptor inhibitor
Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
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αVβ3 integrin inhibitor
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
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FFA2 agonist
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
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GABAA α5 modulator
ONO-8590580 is a GABAA α5 negative allosteric modulator.
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α1β3 GABA(A) receptor modulator
LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
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antagonist of RXRα
β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
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TNF-α inhibitor
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor.
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triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist.
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PI3Kα inhibitor
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM).
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p38-α MAPK inhibitor
5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
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alpha-adrenergic agonist
Indanidine is an alpha-adrenergic agonist.
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Nur77 agonist
DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
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α4β2 nicotinic acetylcholine receptor partial agonist
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation.
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GABAA receptor agonist
Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
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PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.
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PPAR-α agonist
Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
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OGT donor substrate
UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a donor substrate of O-GlcNAc transferase (OGT).
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PPARα/ PPARγ1 agonist
Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.
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α5β1-integrin ligand
c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
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5-HT2A/α1-adrenergic receptor antagonist
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
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VHL:HIF-α interaction inhibitor
VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.
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PDGFRα/β inhibitor
GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively.
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RARα agonist
AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
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PI3Kα inhibitor
GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
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ostsynaptic alpha adrenergic receptor antagonist
Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
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D,L-3-Indolylglycine is an unnatural amino acid that is very similar to Tryptophan, with the indole moiety directly attached to the α-position.
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GABAA(α2/3) receptor modulator
AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
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LXRα inhibitor
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
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PDE4 inhibitor
(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
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α-glucosidase inhibitor
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
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anti-cancer agent
Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.
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α-glucosidase inhibitory activities
Tangshenoside I, isolated from the roots of Codonopsis lanceolata, exhibits weak α-glucosidase inhibitory activities in vitro with an IC50 of 1.4 mM.
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α-glucosidase inhibitor
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM.
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TRPV1 antagonist and TNF-alpha production inhibitor
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor.
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GSK3α inhibitor
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor.
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PDGFRα/PDGFRβ inhbitor
JNJ 10198409 is a potent platelet-derived growth factor receptor (PDGFR) inhibitor (IC50 values are 4.2 and 45 nM for PDGFRβ and PDGFRα, respectively). Also inhibits c-Abl, Lck, c-Src and Fyn kinases (IC50 values are 22, 100, 185 and 378 nM respectively).
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