“alpha ergocryptine”的搜索结果
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GABAAα5 modulator
Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
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integrin α5β1 antagonist
ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
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p38α inhibitors
R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.
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αvβ3 integrin antagonist
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide αvβ3 integrin antagonist with an IC50 of 80 nM.
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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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VDR activator
Alfacalcidol-D6, a deuterated Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3), is a non-selective VDR activator medication.
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HIF1α inhibitor
EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
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α-glucoside hydrolase inhibitor
Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
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integrin αvβ3 antagonist
Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.
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oxytocin receptor ligand
Oxytocin (α-Hypophamine) is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
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PGF2α/LTB4 production inhibitor
Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
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neuronal nicotinic receptor agonist
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
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β3-adrenergic receptor agonist
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
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IRE1α inhibitor
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
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IRE1α RNase kinase inhibitor
KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 ?M. KIRA6 can trigger an apoptotic response.
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Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.
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HIF-1α/von Hippel-Lindau interaction inhibitor
ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 ?M.
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IRE1α inhibitor
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
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TNFα inhibitor
C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
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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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MD2-TLR4 inhibitor
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
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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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3,5-Diiodothyropropionic acid is a thyroid hormone analog, induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (TR), with Ka of 2.40 and 4.06 M-1 for TRα1 and TRβ1, respectively.
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IKKα/IKKβ inhibitor
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively.
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ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.
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- Sen He, .et al. The potential endocrine disruption mechanism of anthelmintic drug niclosamide by activating estrogen receptors and estrogen-related receptors, Toxicology, 2021, May 4;457:152805 PMID: 33961950
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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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PI3Kα/δ inhibitor
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
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6-?Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.
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α7 nAChR Modulator
BNC375 is a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs.
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oral α and β tubulin inhibitor
VERU-111 is a novel, oral α and β tubulin inhibitor that blocks tubulin polymerization and is not a substrate for multi-drug resistance mechanisms.
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α7 nAChR modulator
-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.
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p38α MAPK inhibitor
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
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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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alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
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α2-receptor agonist
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
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platelet adhesion inhibitor
Limaprost(OP1206) is a PGE1 analog and potent platelet adhesion inhibitor.
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adrenergic alpha-1 agonist
Midodrine is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.
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Adrenergic alpha-1 agonist
Midodrine hydrochloride is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. It improves clinical outcome of chronic hypotension.
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alpha-adrenergic blocking agent
Moxisylyte hydrochloride is an alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents.
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alpha-1 adrenergic agonist
Methoxamine Hydrochloride is an alpha-1 adrenergic agonist that causes prolonged peripheral vasoconstriction.
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nicotinic receptor agonist
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
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α-adrenoceptor agonist
Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.
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α2 adrenoceptor antagonist
Piperoxan hydrochloride is an α2 adrenoceptor antagonist.
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α4β1/α9β1 抑制剂
R-BC154是高亲和力的荧光α4β1/α9 9β1抑制剂。
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α9β1/α4β1 integrin 抑制剂
BOP sodium salt是新型的双重alpha9beta1/alpha4beta1整联蛋白抑制剂。
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Lipoic acid是衍生自辛酸的有机硫化合物。ALA通常在动物体内制成,并且对于有氧代谢至关重要。
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Alpha-galactosidase 抑制剂
Deoxygalactonojirimycin Hydrochloride是一种有效且选择性的Alpha-gal A(Alpha-半乳糖苷酶)抑制剂。
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alpha-1A/alpha-1B-adrenoceptor 拮抗剂
Tamsulosin是一种α1a-选择性α受体阻滞剂,用于对症治疗前列腺增生(BPH)。
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Hyodeoxycholic (HDCA) acid是二级胆汁酸,是肠道细菌的代谢副产物之一。
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RARβ agonist
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist.
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