Search Result
Results for "
metabolically stable
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-121524
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Microtubule/Tubulin
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Cancer
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DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research .
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- HY-128604
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ROR
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Cancer
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XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM .
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- HY-121557
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- HY-143406
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Fungal
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Infection
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Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo .
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- HY-U00271
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- HY-103338
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- HY-135880A
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- HY-135880
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- HY-137614
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- HY-103342
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- HY-137615
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- HY-137618
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- HY-137619
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- HY-137620
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- HY-137626
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- HY-137627
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- HY-117178
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Others
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Metabolic Disease
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TA 0910 acid-type is a metabolite of TA 0910. TA-0910 is a metabolically stable analogue of thyrotropin releasing hormone (TRH) .
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- HY-124175
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Others
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Endocrinology
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16-Phenoxy prostaglandin F2α ethyl amide is a metabolically stable PGF2α analogue containing a acetamide structure .
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- HY-139132
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Apoptosis
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Cancer
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Met-F-AEA is a metabolically stable anandamine analogue. Met-F-AEA inhibits cell growth by activating apoptosis. Met-F-AEA has antitumor activity .
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- HY-102036
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Btk
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Inflammation/Immunology
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G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis .
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- HY-114481
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IKE
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Ferroptosis
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Cancer
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Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc - and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity .
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- HY-110092
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P2Y Receptor
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Metabolic Disease
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PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors .
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- HY-151879
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- HY-101032
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RIP kinase
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Inflammation/Immunology
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RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting
protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome .
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- HY-108651
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UTPγS trisodium
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P2Y Receptor
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Metabolic Disease
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Uridine-5'-O-(3-thiotriphosphate) trisodium, a stable analogue of UTP, is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability .
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- HY-103237
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Adenosine Deaminase
|
Neurological Disease
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L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitory adenosine deaminase (ADA) activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation .
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- HY-137603
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UTPγS
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P2Y Receptor
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Metabolic Disease
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Uridine-5'-O-(3-thiotriphosphate) (UTPγS), a stable analogue of UTP, is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability .
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- HY-15402
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BMS 207940
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Endothelin Receptor
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Cardiovascular Disease
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Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model .
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- HY-136059
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Keap1-Nrf2
Autophagy
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Cardiovascular Disease
Cancer
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Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator .
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- HY-137608
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UDP-β-S
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P2Y Receptor
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Cardiovascular Disease
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Uridine 5'-O-thiodiphosphate (UDP-β-S) is a stable analog of UDP. As a selective agonist of P2Y6 receptor, Uridine 5'-O-thiodiphosphate has higher metabolic stability and can be used in the study of cardiovascular diseases .
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- HY-W749209
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Endogenous Metabolite
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Sodium Acetate-1,2-13C2 is a stable isotope labeled compound with biomarker and metabolic tracking activity. Sodium Acetate-1,2-13C2 is often used in biochemical research for the analysis of metabolic pathways. Sodium Acetate-1,2-13C2 is also used in medical imaging and compound development to improve the understanding of biological processes.
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- HY-13847
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mTOR
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Cancer
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GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
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- HY-139063
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16-Phenoxy tetranor PGF2α
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Others
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Metabolic Disease
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16-phenoxy tetranor Prostaglandin F2α (16-phenoxy tetranor PGF2α) is a metabolically stable analog of PGF2α. It binds to the FP receptor on ovine luteal cells with much greater affinity (440%) than PGF2α.
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- HY-159582
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Others
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Cardiovascular Disease
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ACKR3 agonist 1 (compound 27) is a selective ACKR3 agonist (EC50=69 nM, Emax=82%) that inhibits platelet aggregation. ACKR3 agonist 1 is metabolically stable and non-cytotoxic, and has the potential to inhibit platelet-mediated thrombosis .
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- HY-W750600
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Methyl cyanide-15N
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Endogenous Metabolite
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Acetonitrile-15N (Methyl cyanide-15N) is a stable isotope labeled organic compound with important applications in metabolic research and molecular labeling. Acetonitrile-15N is used in biolabeling experiments to track metabolic pathways and help understand the chemical reaction mechanisms in organisms. Acetonitrile-15N is also widely used in environmental science to study the migration and transformation processes of pollutants.
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- HY-118520
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Prostaglandin Receptor
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Endocrinology
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16-Phenoxy tetranor Prostaglandin F2α methyl ester is a metabolically stable form of Prostaglandin F2α that can binds to FP receptor. 16-Phenoxy tetranor Prostaglandin F2α methyl ester serves as prodrug that can be hydrolyzed to generate bioactive free acid .
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- HY-167856
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GPR88
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Neurological Disease
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RTI-122 is a brain-penetrant and potent GPR88 agonist with good metabolic stability (half-life of 5.8 h in mice) and a cAMP EC50 of 11 nM. RTI-122 can be utilized in research on excessive drinking .
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- HY-B0389A
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Glucose-13C6; D-(+)-Glucose-13C6; Dextrose-13C6
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Endogenous Metabolite
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Others
Metabolic Disease
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D-Glucose- 13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose- 13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard .
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- HY-128428
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15(S)-15-Methyl Prostaglandin F2α; 15-Methyl-PGF2α
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Prostaglandin Receptor
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Endocrinology
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Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a metabolically stable synthetic analog of prostaglandin F2α. Carboprost stimulates uterine contractions and induces abortion. Carboprost is used for postpartum hemorrhage due to uterine atony and for the termination of pregnancy in the second trimester .
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- HY-130179
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Apoptosis
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Neurological Disease
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RC-33 hydrochloride is a selective and metabolically stable σ? receptor agonist with activity in enhancing nerve growth factor (NGF)-induced neurite outgrowth. Both enantiomers of RC-33 hydrochloride bind to the σ? receptor with similar affinity and show almost equal effectiveness as σ? receptor agonists. The R-configured enantiomer of RC-33 hydrochloride shows higher liver metabolic stability in the presence of NADPH. RC-33 hydrochloride was selected as the best candidate for further in vivo studies in animal models of amyotrophic lateral sclerosis .
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- HY-15331
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Vitamin D3-26,26,26,27,27,27-d6
|
Isotope-Labeled Compounds
VD/VDR
Bacterial
Endogenous Metabolite
|
Metabolic Disease
|
VD3-d6 (Vitamin D3-26,26,26,27,27,27-d6) is deuterated VD3. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
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- HY-149481
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Dopamine Receptor
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Neurological Disease
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D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders .
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- HY-137544
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16-Phenyl tetranor PGF2α
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Others
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Metabolic Disease
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16-phenyl tetranor Prostaglandin F2α (16-phenyl tetranor PGF2α) is a metabolically stable analog of PGF2α. The affinity of 16-phenyl tetranor PGF2α at the FP receptor of ovine luteal cells is poor (8.7%) compared to PGF2α.
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- HY-152219
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CDK
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Infection
Cancer
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CLK1-IN-2 is metabolically stable Clk1 inhibitor. CLK1-IN-2 has selectivity for Clk1 with an IC50 value of 1.7 nM. CLK1-IN-2 can be used for the research of tumour, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza .
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- HY-143326
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Bacterial
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Infection
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Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes .
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- HY-14921
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Integrin
Others
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Cardiovascular Disease
Inflammation/Immunology
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Elsibucol is a VCAM1 inhibitor for the study of organ transplant rejection. Elsibucol is a metabolically stable propanol derivative with antioxidant, anti-inflammatory and anti-proliferative properties. Elsibucol lowers blood cholesterol levels and reduces oxidative stress and inflammatory responses in injured arteries, thereby inhibiting atherosclerosis and protecting endothelial healing after arterial injury .
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- HY-117507
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5-HT Receptor
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Neurological Disease
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U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity . U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM) .
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- HY-145695
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Cholinesterase (ChE)
Monoamine Oxidase
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Neurological Disease
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Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability .
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- HY-155111
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Phospholipase
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Neurological Disease
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nSMase2-IN-1 is an orally active Neutral sphingomyelinase 2 (nSMase2) inhibitor with an IC50 value of 0.13 ± 0.06 μM. nSMase2-IN-1 is metabolically stable in liver microsomes and orally available with a favorable brain-to-plasma ratio. nSMase2-IN-1 can be used for nervous system disease research .
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- HY-162526
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HIV
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Infection
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HIV capsid modulator 2 (Compound 7t) is a modulator for the HIV capsid (CA) protein. HIV capsid modulator 2 exhibits antiviral activity, which inhibits HIV-1 IIIB strain and HIV-2 ROD strain with EC50 of 0.04 and 0.13 μM. HIV capsid modulator 2 is metabolically stable in human liver microsomes .
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- HY-128428R
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Prostaglandin Receptor
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Endocrinology
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Carboprost (Standard) is the analytical standard of Carboprost. This product is intended for research and analytical applications. Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a metabolically stable synthetic analog of prostaglandin F2α. Carboprost stimulates uterine contractions and induces abortion. Carboprost is used for postpartum hemorrhage due to uterine atony and for the termination of pregnancy in the second trimester .
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- HY-162525
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HIV Protease
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Infection
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GS-9770 is an orally active inhibitor for HIV protease with Ki of 0.16 nM. GS-9770 exhibits antiviral activity aginst HIV-1 strains and HIV-2 strains with EC50 of 1.9-26 nM, and 26 nM. GS-9770 is metabolic stable in human liver microsomes. GS-9770 exhibits good pharmacokinetic characters in Sprague Dawley rats .
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- HY-144738
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Epoxide Hydrolase
FAAH
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Inflammation/Immunology
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Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase .
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- HY-168562
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Sigma Receptor
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Neurological Disease
Cancer
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σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
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- HY-W102449S
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1-(4-(Methylamino)phenyl)ethanone-13C,d3
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Isotope-Labeled Compounds
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Others
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4-Acetyl-N-methylaniline-13C,d3 (1-(4-(Methylamino)phenyl)ethanone-13C,d3) is a 13C and deuterated isotope of 4-Acetyl-N-methylaniline. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
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- HY-P3960
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- HY-129242
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4-Oxo-Tempo
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Others
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Others
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Tempone (4-Oxo-Tempo) is a stable water-soluble nitro radical. Tempone is widely used as a contrast agent for metabolic activity and hypoxic sensitivity in electron spin resonance spectroscopy, magnetic resonance imaging and dynamic nuclear polarization. Tempone reduces superoxide radicals by mimicking the activity of superoxide dismutase (SOD), thereby reducing the formation of hydroxyl radicals and peroxynitrites. Tempone can be used in the study of ischemia-reperfusion injury and acute renal failure .
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- HY-120181
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Isocitrate Dehydrogenase (IDH)
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Cancer
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AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .
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- HY-14923
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AVE 7688
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Angiotensin-converting Enzyme (ACE)
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Metabolic Disease
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Ilepatril, a vasopeptidase inhibitor, was investigated in obese Zucker diabetic fatty (ZDF) rats as a dual inhibitor of angiotensin converting enzyme and neutral endopeptidase for treating Type 2 diabetic nephropathy. Despite stable diabetes (HbA1c >12%), Ilepatril significantly reduced albuminuria in a dose-dependent manner compared to placebo. This study highlights Ilepatril's efficacy in ameliorating nephropathy symptoms in diabetic rats, suggesting its potential as a therapeutic strategy independent of metabolic control for Type 2 diabetic nephropathy .
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- HY-137355
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15(S)-15-Methyl PGD2
|
Prostaglandin Receptor
|
Cardiovascular Disease
Metabolic Disease
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15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. In contrast to PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction and increases systemic blood pressure with much reduced inhibitory activity on ADP-induced platelet aggregation. It also exhibits strong antifertility activity in hamsters (200-fold more potent than PGD2).
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- HY-126291
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Sodium Channel
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Neurological Disease
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GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively .
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- HY-122144
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Teroxirone
|
Endogenous Metabolite
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Cancer
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α-Triglycidyl isocyanurate (Teroxirone) is an antitumor compound with activity to inhibit DNA replication. α-Triglycidyl isocyanurate exerts its anticancer effect by alkylating and cross-linking DNA. α-Triglycidyl isocyanurate is relatively stable in fresh human plasma and whole blood, showing good biocompatibility. The metabolism of α-Triglycidyl isocyanurate mainly occurs in rat liver and is metabolized through an NADPH-independent pathway. The cytotoxicity of α-Triglycidyl isocyanurate can be partially restored under specific conditions, suggesting the complexity of its metabolic pathway .
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- HY-167680
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GSK823093
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Others
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Metabolic Disease
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Denagliptin (GSK823093) is a small molecule dipeptidyl peptidase IV (DPP-4) inhibitor with activity for the suppression of endocrine and metabolic diseases. Denagliptin can be used to study type 2 diabetes. Denagliptin is stable in the solid state but degrades in solution and in mixtures with various excipients. Denagliptin also exhibits degradation in capsules, mainly through cyclization reactions to form (3S,7S,8aS) aminoamines to provide further synthetic materials. The degradation pathway of Denagliptin was elucidated, providing data to support its formulation development and regulatory filings .
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- HY-16632
-
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γ-secretase
Amyloid-β
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Metabolic Disease
|
ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease .
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- HY-16633
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γ-secretase
Amyloid-β
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Metabolic Disease
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ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease .
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- HY-139124
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15(R)-Carboprost; 15(R)-15-methyl PGF2α
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Others
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Metabolic Disease
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15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
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- HY-125782
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15(R)-15-Methyl PGD2
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Prostaglandin Receptor
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Metabolic Disease
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15(R)-15-Methyl prostaglandin D2 (15(R)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1and CRTH2/DP2. 15(R)-15-Methyl prostaglandin D2 is a potent, selective agonist for the CRTH2/DP2 receptor. The EC50 values for eosinophil CD11b expression, actin polymerization, and chemotaxis are 1.4, 3.8, and 1.7 nM, respectively, each of which is approximately 3-5 fold lower than those for PGD2. In contrast the EC50 for the DP1-mediated increase in platelet cAMP by 15(R)-15-methyl PGD2 is >10 μM.
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Cat. No. |
Product Name |
Target |
Research Area |
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0389A
-
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D-Glucose- 13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose- 13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard .
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- HY-15331
-
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VD3-d6 (Vitamin D3-26,26,26,27,27,27-d6) is deuterated VD3. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
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- HY-W102449S
-
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4-Acetyl-N-methylaniline-13C,d3 (1-(4-(Methylamino)phenyl)ethanone-13C,d3) is a 13C and deuterated isotope of 4-Acetyl-N-methylaniline. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
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- HY-W749209
-
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Sodium Acetate-1,2-13C2 is a stable isotope labeled compound with biomarker and metabolic tracking activity. Sodium Acetate-1,2-13C2 is often used in biochemical research for the analysis of metabolic pathways. Sodium Acetate-1,2-13C2 is also used in medical imaging and compound development to improve the understanding of biological processes.
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- HY-W750600
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Acetonitrile-15N (Methyl cyanide-15N) is a stable isotope labeled organic compound with important applications in metabolic research and molecular labeling. Acetonitrile-15N is used in biolabeling experiments to track metabolic pathways and help understand the chemical reaction mechanisms in organisms. Acetonitrile-15N is also widely used in environmental science to study the migration and transformation processes of pollutants.
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- HY-W750796
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Butyric acid-13C4 sodium (Butanoic acid-13C4 sodium) is a stable isotope labeled compound with the activity of promoting cell proliferation and regulating gene expression. Butyric acid-13C4 sodium can be used in metabolic research and compound development to help scientists gain a deeper understanding of the role of short-chain fatty acids in organisms. Butyric acid-13C4 sodium also plays an important role in nutrition and intestinal health research, especially in the regulation of probiotic function and intestinal microbiota.
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Cat. No. |
Product Name |
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Classification |
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- HY-103237
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Nucleosides and their Analogs
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L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitory adenosine deaminase (ADA) activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation .
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