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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
107 Results for "
metabolic dysfunction
" in MedChemExpress (MCE) Product Catalog:
Products (107)
107 Results for "metabolic dysfunction" in MCE Product Catalog:
Cat. No.: HY-184939
CAS No.: 3063509-17-8
Research Areas:
THR-β agonist 12 is an orally active, potent, and highly selective thyroid hormone receptor β (THR-β) agonist (EC50 = 36 nM). THR-β agonist 12 shows no significant activity against THRα and exhibits no cardiotoxicity in vivo. THR-β agonist 12 inhibits lipid synthesis by activating the AMPK-ACC-SREBP1 signaling axis. THR-β agonist 12 can be used on research into metabolic dysfunction-associated steatohepatitis (MASH) and related metabolic diseases .
Cat. No.: HY-179591
CAS No.: 2127387-94-2
Synonyms: 326E
Target:
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BGT-002 (326E) is an orally active dual ACLY inhibitor and PPARα agonist. BGT-002 reduces lipogenesis by inhibiting synthesis and promoting efflux. BGT-002 demonstrates efficacy in ameliorating metabolic dysfunction-associated steatohepatitis (MASH) and improving hyperlipidemia in vivo. BGT-002 can be used for hypercholesterolemia and MASH research .
Cat. No.: HY-182750
Target:
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ACLY-IN-3 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.036 μM and a target Kd of 0.54 μM. ACLY-IN-3 interacts with the allosteric binding site of ACLY to inhibit its activity. ACLY-IN-3 exhibits excellent lipid-lowering effects and alleviates hepatic inflammation and liver fibrosis. ACLY-IN-3 can be used for the research of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-L227
195 compounds
Amino acids are the fundamental components that sustain life activities, playing roles in ATP generation, promoting nucleotide synthesis, and maintaining cellular redox balance. Moreover, dysregulation of amino acid consumption is a significant potential regulatory mechanism leading to impaired anti-tumor immunity in immune cells. The normal functioning of immune cells relies on amino acid metabolic pathways to obtain energy and materials, and upon activation, they reprogram their metabolism to support growth, proliferation, and effector functions. Additionally, metabolic disorders of specific amino acids (such as branched-chain amino acids, glutamine, and arginine) can exacerbate mitochondrial dysfunction and oxidative stress, thereby promoting myocardial fibrosis and cardiac cell damage. Therefore, conducting research related to amino acid metabolism holds promise for discovering potential drugs for diseases related to cancer, immunity, and metabolism.
MCE can provide 195 kinds of metabolites of amino acid metabolic pathways, which can be used for drug screening in various diseases such as cancer, immune disorders, metabolic diseases, mitochondrial-targeted diseases
Cat. No.: HY-180921
CAS No.: 2845278-33-1
Target:
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GS-1291269 is a potent and neutral ketohexokinase (KHK) inhibitor, with IC50s of 0.38 and 2.1 nM against KHK-C and KHK-A, respectively. GS-1291269 demonstrates liver and kidney fructose-1-phosphate (F1P) reduction in a fructose challenge model in rats. GS-1291269 can be used for kidney disease and metabolic-dysfunction-associated steatotic liver disease (MASLD) research .
Cat. No.: HY-153149
CAS No.: 945457-84-1
Synonyms: FM101
Research Areas:
LJ-2698 (FM101) is an orally active adenosine A3 receptor (Adenosine A3 Receptor) antagonist . LJ-2698 blocks adenosine A3 receptor-dependent pro-inflammatory JNK, ERK, and NF-κB signaling pathways. LJ-2698 prevents alveolar cavity enlargement, restores pulmonary function, and inhibits matrix metalloproteinase activity and pulmonary cell apoptosis (apoptosis) in mice . LJ-2698 induces mitochondrial dysfunction, necroptosis, and intrinsic apoptosis. LJ-2698 ameliorates renal injury in mice with diabetic nephropathy, and alleviates diet-induced hepatic inflammation and fibrosis. LJ-2698 can be used in the research of emphysema, diabetic nephropathy, and metabolic dysfunction-associated steatotic liver disease .
Cat. No.: HY-183279
Research Areas:
FXR antagonist 4 (Compound 4l) is an orally active, selective FXR antagonist with an IC50 of 0.70 μM. FXR antagonist 4 binds to FXR, differentially regulates bile acid and lipid transporter genes, and exerts no effect on gluconeogenesis-related genes. FXR modulator 1 activates the AMPK signaling pathway to inhibit fatty acid synthesis. FXR modulator 1 alleviates hepatic steatosis, ballooning degeneration and fibrosis, and improves dyslipidemia. FXR modulator 1 can be used for research on metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-187384
Target:
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GPR35 agonist 7 is a selective GPR35 agonist, with an EC50 of 0.030 μM for hGPR35 and an EC50 of 0.021 μM for mGPR35. GPR35 agonist 7 reduces lipid accumulation. In a high-fat diet-induced MASH mouse model, GPR35 agonist 7 improves hepatic steatosis, corrects lipid metabolism disorders, alleviates hepatic inflammation and attenuates hepatic fibrosis. GPR35 agonist 7 can be used for the research of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-182751
Target:
Research Areas:
ACLY-IN-4 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.022 μM and a Kd of 0.19 μM. ACLY-IN-4 binds to the allosteric binding site of ACLY. ACLY-IN-4 exhibits hypolipidemic, anti-steatotic, insulin sensitivity-improving, anti-oxidative stress, anti-inflammatory and anti-fibrotic activities. ACLY-IN-4 alleviates hepatic steatosis, systemic insulin resistance, oxidative stress, hepatic inflammation and fibrosis. ACLY-IN-4 can be used for the research of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-L064
1,827 compounds
Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH.
Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment.
MCE owns a unique collection of 1,827 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.
Cat. No.: HY-183318
CAS No.: 3108258-69-8
Target:
Research Areas:
PPARα/δ agonist 4 is a potent orally active and selective dual peroxisome proliferator-activated receptor (PPAR) α/δ agonist with EC50s of 0.36 and 1.31 nM, respectively. PPARα/δ agonist 4 exhibits >123-fold selectivity over PPARγ (EC50 = 160.84 nM). PPARα/δ agonist 4 upregulates expression of downstream fatty acid oxidation genes PDK4, CPT1A, and ACADVL. PPARα/δ agonist 4 can be used for the research of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-183692
CAS No.: 3061938-00-6
Target:
FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Heme Oxygenase (HO) Quinone Reductase Keap1-Nrf2
Research Areas:
FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-189008
Target:
Research Areas:
17β-HSD13-IN-1 is a selective 17β-HSD13 inhibitor with a human IC50 of 9 nM, high selectivity over 17β-HSD1, nanomolar cellular activity, broad pH solubility, extended rodent plasma mean residence times, and high oral bioavailability in Mus musculus. 17β-HSD13-IN-1 engages in hydrophobic interactions with specific active-site amino acids of its target enzyme. 17β-HSD13-IN-1 can be used for the research of metabolic dysfunction-associated steatohepatitis (mash) .
Cat. No.: HY-N17383
CAS No.: 2283387-37-9
Cat. No.: HY-179728
Target:
Research Areas:
Amylin agonist 1 is an agonist of amylin receptor 3 (AMY3R), with an EC50 of 6.17 nM for stimulating cellular cAMP production. Amylin agonist 1 is also an agonist of calcitonin receptor (CTR), with an EC50 of 8.58 nM. Amylin agonist 1 can be used for the research of type 2 diabetes and obesity .
Cat. No.: HY-183723
Research Areas:
GAA-4OH is a potent and irreversible dihydroceramide desaturase-1 (DES1) inhibitor with an IC50 of 0.6 μM and a Ki of 139.5 nM. GAA-4OH undergoes oxidation to form a reactive iminoquinone that covalently blocks DES1’s catalytic cavity, causing permanent enzyme inactivation. GAA-4OH modulates sphingolipid balance by reducing ceramide-to-dihydroceramide ratios in liver tissue. GAA-4OH improves liver steatosis, inflammation, fibrosis, and reduces pro-inflammatory and pro-fibrogenic gene expression. GAA-4OH can be used for the research of metabolic dysfunction-associated steatotic liver disease (MASLD) .
Cat. No.: HY-184292
Research Areas:
COX-2-IN-67 is an orally active, blood-brain barrier permeable multi-target inhibitor that potently targets COX-2 (IC50=0.07 μM), hCA IX (Ki=62.7 nM) and hBuChE (IC50=0.47 μM). COX-2-IN-67 alleviates oxidative stress and liver stress, improves glucose homeostasis and insulin sensitivity, and optimizes lipid profiles. Meanwhile, COX-2-IN-67 effectively reduces the levels of neuroinflammatory markers and improves hippocampus-dependent cognitive function in a high-fat diet-induced rat model. COX-2-IN-67 can be used for the research of metabolic dysfunction-associated mild cognitive impairment .
Cat. No.: HY-181761
CAS No.: 3099198-78-1
Target:
Research Areas:
FXR agonist 16 is a FXR agonist with an EC50 of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury .
Cat. No.: HY-182046
CAS No.: 2930131-74-9
Research Areas:
HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, and Kd values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease .
Cat. No.: HY-182469
Target:
Lactate Dehydrogenase AMPK FOXO Interleukin Related Reactive Oxygen Species (ROS) TNF Receptor Bcl-2 Family Caspase Apoptosis
Research Areas:
FuBIG is an iminoguanidine derivative with neuroprotective effects. FuBIGL inhibits L-LDH activation and reduces lactate production. FuBIGL exerts protective effects on inflammatory nerve cells, upregulates the expressions of AMPK, pAMPK and FOXO3, and activates the AMPK pathway in cells. FuBIG exerts anti-inflammatory effects by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10. FuBIG maintains mitochondrial membrane potential, alleviates mitochondrial dysfunction, reduces ROS production, and relieves oxidative stress. FuBIG upregulates Bcl-2, downregulates Bax and Caspase-3, and inhibits cell apoptosis (apoptosis). FuBIG improves metabolic disorders in diabetic mice, decreases the levels of LDL-C, ALT and AST, and increases HDL-C level simultaneously. FuBIG can be used in the research of diabetic neuroinflammation .
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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
