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dysfunction-associated Steatohepatitis

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37

Inhibitors & Agonists

3

Peptides

1

Inhibitory Antibodies

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-172317

    FAP Metabolic Disease
    AZD2389 is a potent and orally active FAP inhibitor. AZD2389 can be used for the study of metabolic dysfunction-associated steatohepatitis .
    AZD2389
  • HY-P990964

    BOS-580; LLF580

    FGFR Metabolic Disease Inflammation/Immunology
    Efimosfermin alfa is a genetically engineered FGF21 variant. Efimosfermin alfa exerts its function by activating the FGFR1c/β-Klotho complex. Efimosfermin alfa is applicable to researches on metabolic dysfunction-associated steatohepatitis, obesity and mild hypertriglyceridemia .
    Efimosfermin alfa
  • HY-143712
    Allolithocholic acid
    1 Publications Verification

    Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR Metabolic Disease Inflammation/Immunology Cancer
    Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .
    Allolithocholic acid
  • HY-160929

    CS-0159

    FXR Inflammation/Immunology
    Linafexor (CS-0159) is a FXR agonist and bile acid homeostasis modulator. Linafexor exerts its effects by activating FXR, a regulator of liver function. Linafexor is applicable to research related to primary sclerosing cholangitis (PSC). Linafexor is also suitable for research in the field of metabolic dysfunction-associated steatohepatitis (MASH) .
    Linafexor
  • HY-177705

    ACSL Family Drug Derivative Metabolic Disease Cancer
    ACSL5-IN-2 (Compound B) is an Acyl CoA synthetase 5 (ACSL5) inhibitor. ACSL5-IN-2 can block the conversion of long-chain fatty acids (such as palmitic acid and oleic acid) into acyl-CoA, and intervene in the fatty acid metabolism pathway. ACSL5-IN-2 can inhibit cancer cells growth. ACSL5-IN-2 can be used for the research of cancer and metabolic disease, such as colon cancer and dysfunction-associated Steatohepatitis .
    ACSL5-IN-2
  • HY-N8599
    Cichoriin
    2 Publications Verification

    Amylases Glycosidase Lipase Dipeptidyl Peptidase p38 MAPK PPAR P2Y Receptor NOD-like Receptor (NLR) SARS-CoV Pyroptosis GLUT Angiotensin-converting Enzyme (ACE) NF-κB Infection Metabolic Disease Inflammation/Immunology
    Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC50 values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y14R (IC50 = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2 .
    Cichoriin
  • HY-168046

    Thyroid Hormone Receptor Metabolic Disease
    ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC50 of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease .
    ALG-055009
  • HY-177704

    ACSL Family Drug Derivative Metabolic Disease Cancer
    ACSL5-IN-1 (Compound A) is an ACSL5 inhibitor with body weight-reducing activity. ACSL5-IN-1 inhibits ACSL5, an enzyme linked to fatty acid metabolism. ACSL5-IN-1 reduces body weight in diet-induced obesity mice. ACSL5-IN-1 can be used for the research of obesity, metabolic dysfunction-associated steatohepatitis, metabolic syndrome, non-alcoholic fatty liver disease, type 2 diabetes, acute myeloid leukemia, colorectal cancer, and breast cancer .
    ACSL5-IN-1
  • HY-158766

    3-Succinylated cholic acid

    Endogenous Metabolite Bacterial Infection Inflammation/Immunology
    3-sucCA is an orally available bacterial bile acid that exerts anti-MASH effects by promoting the growth of Akkermansia muciniphila. By remodeling the intestinal microbiota and promoting the growth of Akkermansia, 3-sucCA can improve intestinal barrier damage and reduce chronic low-level inflammation, thereby alleviating the progression of metabolic dysfunction-associated steatohepatitis (MASH). 3-sucCA accelerates the synthesis of cell wall peptidoglycan and has in vivo efficacy in the mouse MAFL-MASH model. 3-sucCA levels are low in the MAFLD model and are mainly used in the study of MASH .
    3-sucCA
  • HY-171454

    GPR119 Metabolic Disease Inflammation/Immunology
    DA-1241 is a GPR119 agonist. DA-1241 reduces macrophage differentiation through downregulation of NFκB signaling by activating GPR119. DA-1241, alone and in combination with a DPP4 inhibitor, reduces liver inflammation and restores inflammation-related liver gene expression. DA-1241 can be used for the research of metabolic dysfunction-associated steatohepatitis (MASH) .
    DA-1241
  • HY-161247

    5-HT Receptor Metabolic Disease
    5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
    5-HT2A antagonist 2
  • HY-156065

    Keap1-Nrf2 Reactive Oxygen Species (ROS) Interleukin Related Metabolic Disease
    S217879 is an orally active and selective NRF2 activator. S217879 activates the NRF2 pathway by specifically disrupting the KEAP1 (Kd: 4.15 nM)-NRF2 interaction, and upregulates the antioxidant response. S217879 also ameliorates steatohepatitis and reduces the degree of liver fibrosis. S217879 can be used in the research of metabolic dysfunction-associated steatotic liver disease and nonalcoholic steatohepatitis .
    S217879
  • HY-178015

    Thyroid Hormone Receptor Metabolic Disease Inflammation/Immunology
    THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. THR-β agonist 11 shows potent cholesterol-lowering activity in cholesterol-fed rats. THR-β agonist 11 significantly reduces serum total TG, LDL-cholesterol, liver total TC and TG levels, and alleviates hepatic steatosis, inflammation and fibrosis in HFD-CCl4-induced Metabolic dysfunction-associated steatohepatitis (MASH) model mice. THR-β agonist 11 can be used for the study of metabolic dysfunction-associated steatohepatitis (MASH) and other fibrotic diseases .
    THR-β agonist 11
  • HY-172661

    Thyroid Hormone Receptor Interleukin Related LDLR Infection Metabolic Disease
    KYLO-0603 is an orally active, selective THR-β agonist (EC50 : 31.07 nM). KYLO-0603 has significant activity in lowering serum cholesterol and low-density lipoprotein cholesterol. KYLO-0603 upregulates the expression of THR-regulated genes (including iodothyronine deiodinase 1 (Dio1), malic enzyme 1 (Me1), and thyroid hormone response (Thrsp) gene) and inhibits the expression of inflammatory and fibrotic genes (low-density lipoprotein receptor (LDL-R) gene) by activating THR-β receptors. KYLO-0603 can be used to treat metabolic dysfunction-associated steatohepatitis (MASH) and liver fibrosis research .
    Kylo-0603
  • HY-P11208C

    GABA Receptor Inflammation/Immunology
    mNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .
    mNLS-CPP-WSTF TFA
  • HY-P11208

    GABA Receptor Inflammation/Immunology
    mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .
    mNLS-CPP-WSTF
  • HY-175676

    Thyroid Hormone Receptor Metabolic Disease Inflammation/Immunology
    THR-β agonist 10 is an orally active and selective THR-β agonist, with an EC50 of 11 nM. THR-β agonist 10 significantly reduces ALT (Alanine Aminotransferase), TC (Total Cholesterol), and LDL-C (Low-Density Lipoprotein Cholesterol) levels, and improves steatosis, ballooning, inflammation and fibrosis in the metabolic dysfunction-associated steatohepatitis (MASH) mouse model. THR-β agonist 10 can be used for the study of MASH .
    THR-β agonist 10
  • HY-170369

    Mitochondrial Metabolism Metabolic Disease
    SHO1122147 (Compound 7m) affects the mitochondrial electron transport chain, exhibits mitochondrial uncoupling activity (EC50=3.6 μM), and increases the oxygen consumption rate (OCR=69%) and promotes cellular respiration. SHO1122147 is orally active, and can be used in reaearch of obesity and metabolic dysfunction-associated steatohepatitis (MASH) .
    SHO1122147
  • HY-168629

    FXR Metabolic Disease
    FXR agonist 9 (compound 26) is an oral active and selectivity FXR partial agonist with the EC50 of 0.09 µM (75.13 % maximum efficacy). FXR agonist 9 ameliorates pathological features in HFD and CCl4(HY-Y0298)-induced metabolic dysfunction-associated steatohepatitis mice .
    FXR agonist 9
  • HY-174887

    Thyroid Hormone Receptor AMPK Acetyl-CoA Carboxylase Mitochondrial Metabolism Metabolic Disease
    THR-β agonist 9 is a potent, selective, and His435 mutation-sensitive THR-β (EC50: 3.2 nM) agonist. THR-β agonist 9 has moderate selectivity (approximately 10-fold) and good activation capacity (EC50: 134.2 nM to 515.5 nM) for multiple His435 mutants (H435A, H435Y, and H435R). THR-β agonist 9 has the potential to be used in the study of dyslipidemia, metabolic dysfunction-associated steatohepatitis (MASH), or resistance to thyroid hormone (RTH) .
    THR-β agonist 9
  • HY-174858

    PROTACs ASK1 p38 MAPK Metabolic Disease
    dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH) (Pink: ASK1 ligand 1 (HY-174860); Blue: E3 ligand (S,R,S)-AHPC (HY-125845); Black: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861) .
    dASK1-VHL
  • HY-168713

    FXR Metabolic Disease
    LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
    LZ-007
  • HY-172883

    FABP PPAR Metabolic Disease Inflammation/Immunology
    ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC50 s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
    ABP/PPAR modulator 1
  • HY-172883A

    FABP PPAR Metabolic Disease Inflammation/Immunology
    (E/Z)-ABP/PPAR modulator 1 is a mixture of the E and Z isomers of ABP/PPAR modulator 1 (HY-172883). ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC50 s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
    (E/Z)-ABP/PPAR modulator 1
  • HY-173265

    Cyclophilin Metabolic Disease Inflammation/Immunology
    CypB-IN-1 (Compound 11) is an inhibitor of cyclophilin B (cyclophilin B) with a Kd value of 12 nM. CypB-IN-1 can be applied to the research field of metabolic dysfunction-associated steatohepatitis (MASH) and the liver fibrosis diseases resulting from it .
    CypB-IN-1
  • HY-159881

    Mitophagy Metabolic Disease
    SHS206 (compound 6n) is an orally active mitochondrial uncoupler that reduces hepatic triglyceride levels. SHS206 exhibits in vivo efficacy in the GAN mouse model and shows inhibitory effects on metabolic dysfunction-associated steatohepatitis (MASH) .
    SHS206
  • HY-172122

    FXR 17β-HSD Metabolic Disease
    FXR/HSD17B13 modulator 1 (compound 6) is a potent modulator of FXR/HSD17B13. FXR/HSD17B13 modulator 1 plays an important roel in metabolic dysfunction-associated steatohepatitis (MASH) research .
    FXR/HSD17B13 modulator 1
  • HY-174133

    17β-HSD Metabolic Disease Inflammation/Immunology
    HSD17B13-IN-104 (Compound 32) is an orally active, highly potent and selective HSD17B13 inhibitor (IC50=2.5 nM). HSD17B13-IN-104 regulates hepatic lipid metabolism by inhibiting the SREBP-1c/FAS pathway. HSD17B13-IN-104 blocks HSD17B13 enzymatic activity to improve hepatic lipid accumulation. HSD17B13-IN-104 is promising for research of metabolic dysfunction-associated steatohepatitis .
    HSD17B13-IN-104
  • HY-179591

    326E

    ATP Citrate Lyase PPAR Metabolic Disease
    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 .
    BGT-002
  • HY-179015

    17β-HSD PPAR Metabolic Disease Inflammation/Immunology
    HSD17B13/PPAR modulator-1 (Compound 17) is a HSD17B13/PPAR multitarget modulator. HSD17B13/PPAR modulator-1 is an inhibitor of HSD17B13, with its IC50 value being 0.91 μM. HSD17B13/PPAR modulator-1 is a PPAR agonist, with the EC50 values for PPARα, PPARδ, and PPARγ being 1.55, 0.12, and 0.01 μM respectively. HSD17B13/PPAR modulator-1 can significantly improve liver function, regulate lipid metabolism, alleviate fibrosis, and exert antioxidant and anti-inflammatory effects in the model of metabolic dysfunction-related steatohepatitis (MASH). HSD17B13/PPAR modulator-1 can be used for the study of MASH .
    HSD17B13/PPAR modulator-1
  • HY-182750

    ATP Citrate Lyase Inflammation/Immunology
    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 .
    ACLY-IN-3
  • HY-182751

    ATP Citrate Lyase Inflammation/Immunology
    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 .
    ACLY-IN-4
  • HY-183279

    FXR AMPK Metabolic Disease
    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 .
    FXR antagonist 4
  • HY-183309

    FXR 17β-HSD Inflammation/Immunology
    FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC50 of 128 nM, human HSD17B13 IC50 of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis .
    FXR/HSD17B13-modulator-2
  • HY-183318

    PPAR Metabolic Disease
    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 .
    PPARα/δ agonist 4
  • HY-183692

    FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Heme Oxygenase (HO) Quinone Reductase Keap1-Nrf2 Cardiovascular Disease Inflammation/Immunology
    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 .
    FXR agonist 18
  • HY-182026

    FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Reactive Oxygen Species (ROS) Inflammation/Immunology
    FXR agonist 17 is an orally active, steroidal FXR agonist with EC50 values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC50 = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis .
    FXR agonist 17

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