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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
118 Results for "
Orphan Receptor
" in MedChemExpress (MCE) Product Catalog:
Products (118)
118 Results for "Orphan Receptor" in MCE Product Catalog:
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16
16 Cited Publications
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
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ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 μM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 μM). ML-180 has the potential for LRH-1-dependent cancers .
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2 Cited Publications
Art. -Nr.: HY-18618A
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SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with Ki values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
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2
2 Cited Publications
Art. -Nr.: HY-P2537
CAS. Nr.: 229961-08-4
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1
1 Cited Publications
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DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
1
1 Cited Publications
ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 blocks the PI3K/AKT/mTOR signaling pathway in a ROR1-dependent manner. ARI-1 upregulates cleaved-PARP and p-P38. ARI-1 induces Apoptosis. ARI-1 has anticancer activity against non-small cell lung cancer .
1
1 Cited Publications
MRL-871 (compound 3) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 12.7 nM. MRL-871 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells .
1
1 Cited Publications
Art. -Nr.: HY-P1438
CAS. Nr.: 412938-75-1
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1 Cited Publications
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(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells .
Art. -Nr.: HY-162617
CAS. Nr.: 885896-26-4
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PSB-KK1415 is a selective agonist for human orphan G protein-coupled receptor GPR18, with EC50 of 19.1 nM .
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GPR109 receptor agonist-1 is a highly selective agonist of the human orphan G protein-coupled receptor GPR109b, and does not activate the mouse homologous receptor PUMA-G. GPR109 receptor agonist-1 functionally modulates the human GPR109b receptor via the cAMP signaling pathway, with an EC50 of 400 nM. GPR109 receptor agonist-1 inhibits isoproterenol (HY-B0468)-stimulated lipolysis in human subcutaneous adipocytes, with efficacy comparable to that of Niacin (HY-B0143), and does not act on β-adrenergic receptors. GPR109 receptor agonist-1 can be used in studies related to dyslipidemia and atherosclerosis .
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NR2F2-IN-1 (free base) is a COUP-TFII (orphan nuclear receptor NR2F2) inhibitor with antitumor activity against prostate cancer. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators including FOXA1. NR2F2-IN-1 (free base) can be used for the research of prostate cancer .
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CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
Synonyms: BI 730357
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Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases .
Art. -Nr.: HY-P2210
CAS. Nr.: 501036-69-7
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TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
