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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
142 Results for "
structure-activity relationship
" in MedChemExpress (MCE) Product Catalog:
Products (142)
142 Results for "structure-activity relationship" in MCE Product Catalog:
Cat. No.: HY-179232
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ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .
Cat. No.: HY-179246
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Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
CXT29 is an orally active COX-2 inhibitor and a thromboxane A2 receptor (TP) antagonist. CXT29 exhibits COX inhibitory activity and selectivity, with IC50 values of 13 and 722 nM for COX-2 and COX-1 respectively. CXT29 inhibits platelet aggregation induced by U-46619 (HY-108566) (a TP agonist), with an IC50 of 96 nM. CXT29 effectively inhibits the production of TXB₂ and PGE₂, significantly reducing platelet aggregation and inflammatory pain in mice. CXT29 can be used for research on inflammatory pain and cardiovascular diseases .
Cat. No.: HY-179683
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MRP1-IN-2 (Compound 21) is a selective MRP1 inhibitor with a relatively weak inhibitory effect on P-gp. MRP1-IN-2 exhibits a strong accumulation effect of calcein, with its EC50 value being 177 nM. MRP1-IN-2 enhances the activity of Doxorubicin (HY-15142A) on drug-resistant cells. MRP1-IN-2 can be used for the study of multidrug-resistant cancers .
Cat. No.: HY-179708
CAS No.: 3086979-57-6
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Cbz-QFR-kbt is a ketone-based benzothiazole ketone inhibitor of TMPRSS2, with an IC50 value of 0.42 nM. Cbz-QFR-kbt also has inhibitory activity against Matriptase, Hepsin, HGFA, and Factor Xa, with IC50 values of 1, 1.3, 85, and 85 nM respectively. Cbz-QFR-kbt shows significant inhibitory effects against SARS-CoV-2 and H1N1 (IC50 = 60 nM). Cbz-QFR-kbt can be used in antiviral research .
Cat. No.: HY-180122
CAS No.: 146877-36-3
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(Rac)-Azide-deoxy-ascomycin-O-ethylene, a nitrogen-containing compound, is a derivative of a macrolide-type immunosuppressant.
Cat. No.: HY-180845
CAS No.: 2931879-67-1
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TGR5 agonist 9 is a highly selective and orally active TGR5 allosteric agonist with EC₅₀ values for hTGR5 and mTGR5 of 0.48 and 0.49 μM, respectively. TGR5 agonist 9 can recruit β-arrestin 1 (EC₅₀ = 78.8 μM) and β-arrestin 2 (EC₅₀ = 12.3 μM), and has a higher efficacy in cAMP accumulation (EC₅₀ = 0.48 μM). TGR5 agonist 9 exhibits a significant hypoglycemic effect in the ICR mouse model. TGR5 agonist 9 can be used for research on diabetes .
Cat. No.: HY-119781
CAS No.: 198710-92-8
Synonyms: PF1191
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Kaitocephalin (PF1191) is an ionotropic glutamate receptor (NMDAR) antagonist with Ki values of 7.8, 590, and 14000 nM for NMDAR, AMPAR, and KAR, respectively. Kaitocephalin protects neurons by inhibiting excitotoxicity, exhibiting neuroprotective effects. Kaitocephalin can be used in research on neurological diseases such as Alzheimer's disease .
Cat. No.: HY-151500C
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JBSNF-00002 is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
Cat. No.: HY-175818
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APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis .
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5β-Cholanic acid-3,6-dione (3,6-Diketo-LCA) is a similar substance to Lithocholic acid (LCA) (HY-B0172). 5β-Cholanic acid-3,6-dione cannot activate the Vitamin D receptor (VDR), and can be used as a negative control for studying the relationship between LCA derivatives and VDR .
Cat. No.: HY-179457
CAS No.: 3079942-94-9
CC-11 is an orally active small molecule drug conjugate (SMDC) that links the PI3K/mTOR inhibitor with the extracellular heat shock protein 90 (EHSP90) targeting ligand through a cleavable linker. CC-11 exhibits strong HSP90 binding activity (IC50 = 15 nM) and inhibits PI3Kα kinase activity (IC50 = 0.54 nM). CC-11 has anti-proliferative activity against colon cancer cells. CC-11 shows significant efficacy in the HCT-116 xenograft tumor model. CC-11 can be used for research on colon cancer .
Cat. No.: HY-180452
CAS No.: 2998560-77-1
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HAT-IN-10 (Compound 12a) is an anti-human African trypanosomiasis (HAT) agent, with an EC50 value of 0.23 μM for T. brucei. HAT-IN-10 can be used for research on HAT .
Cat. No.: HY-180539
CAS No.: 380887-90-1
JT71 is an inhibitor of the transcriptional activator MrkH of type III fimbriae in Klebsiella pneumoniae. JT71 reduces the activity of the mrkA promoter in Klebsiella pneumoniae, effectively inhibiting the formation of biofilms by Klebsiella pneumoniae, while not affecting the cell's viability. JT71 can be used for research on Klebsiella pneumoniae infections .
Cat. No.: HY-179249
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Fluoroneplanocin A-8N (Compound 3a) is an inhibitor targeting SAH hydrolase (IC50 = 1.51 μM) and viral RNA polymerase. Fluoroneplanocin A-8N exhibits broad-spectrum anti-SARS-CoV-2 and dengue virus activity, with EC50 values of 12.2 and 37.4 μM respectively. Fluoroneplanocin A-8N has no cytotoxicity. Fluoroneplanocin A-8N can be used for anti-positive-strand viruses .
Cat. No.: HY-179445
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Nav1.7-IN-20 (Compound 3AG) is an orally active Nav1.7 channel inhibitor with an IC50 of 3.1 μM. Nav1.7-IN-20 demonstrates analgesic efficacy in a complete Freund's adjuvant (CFA) inflammatory pain model. Nav1.7-IN-20 can be used for pain research .
Cat. No.: HY-180541
EGFR-IN-190 (Compound 3o) is an inhibitor that targets both EGFR (IC₅₀ = 0.028 μM) and COX-2 (IC₅₀ = 0.208 μM). EGFR-IN-190 exhibits potent inhibitory activity against MCF-7 cells and induces apoptosis (apoptosis). EGFR-IN-190 can be used for research on breast cancer .
Cat. No.: HY-179637
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RNAP-σ interaction-IN-4 (Compound 3a) is an inhibitor of the RNA polymerase-sigma factor interaction (RNAP-σ) with MIC values against S. pneumoniae and S. aureus of 1 μg/mL and 2 μg/mL, respectively. RNAP-σ interaction-IN-4 exhibits strong bactericidal properties by interfering with the interaction of β′CH−σ and disrupting the transcription of bacteria. RNAP-IN-2 shows significant efficacy in sepsis models. RNAP-σ interaction-IN-4 can be used to study Gram-positive bacterial infections caused by multi-drug resistant strains .
Cat. No.: HY-179419
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Glucokinase activator 10, a thiazole-based compound, is a liver-selective and orally active glucokinase activator with an EC50 of 42 nM. Glucokinase activator 10 exhibits significant glucose lowering in acute diet-induced obese mouse oral glucose tolerance (OGTT) test. Glucokinase activator 10 can be used for the study of metabolic disorders .
Cat. No.: HY-P11258
CAS No.: 3090686-88-4
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
Cat. No.: HY-179293
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SARS-CoV-2 PLpro-IN-3 (Compound 15) is a covalent inhibitor of the SARS-CoV-2 papain-like protease (PLpro), with an IC50 of 25 nM. SARS-CoV-2 PLpro-IN-3 has similar inhibitory activity against SARS-CoV PLpro (IC50 = 59 nM), but shows no inhibitory effect on human ubiquitin-specific protease 7 (USP7). The EC50 of SARS-CoV-2 PLpro-IN-3 in inhibiting SARS-CoV-2 replication in cells is 96 nM, significantly reducing the viral titer and viral RNA levels. SARS-CoV-2 PLpro-IN-3 can be used for studying SARS-CoV-2 drug resistance mutations .
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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
