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Agonists Inhibitors

" in MedChemExpress (MCE) Product Catalog:

805

Inhibitors & Agonists

1

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2

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4

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83

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4

Inhibitory Antibodies

82

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76

Isotope-Labeled Compounds

3

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3

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-171115
    Pyrone-211

    		GPR84 Aldose Reductase Metabolic Disease
    Pyrone-211 is a potent GPR84 agonist and AKR1C3 inhibitor. Pyrone-211 participates in an expanded polyamine pathway .
    Pyrone-211
  • HY-N0234
    Bavachinin
    3 Publications Verification

    7-O-Methylbavachin; Bavachinin A

    		 Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cancer
    Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
    Bavachinin
  • HY-146356
    Adenylyl cyclase type 2 agonist-1

    		Adenylate Cyclase Inflammation/Immunology
    Adenylyl cyclase type 2 agonist-1 (Compound 73) is a potent agonist of adenylyl cyclase type 2 (AC2) with the EC50 of 90 nM. Adenylyl cyclase type 2 agonist-1 inhibits expression of Interleukin-6, making it a potential lead compound against respiratory diseases .
    Adenylyl cyclase type 2 agonist-1
  • HY-14598R
    Diethylstilbestrol (Standard)

    		Estrogen Receptor/ERR Apoptosis Autophagy Endocrinology Cancer
    Diethylstilbestrol (Standard) is the analytical standard of Diethylstilbestrol. This product is intended for research and analytical applications. Diethylstilbestrol (Stilbestrol) is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor. .
    Diethylstilbestrol (Standard)
  • HY-14598
    Diethylstilbestrol
    3 Publications Verification

    		 Estrogen Receptor/ERR Apoptosis Autophagy Endocrinology Cancer
    Diethylstilbestrol is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor. .
    Diethylstilbestrol
  • HY-N0234R
    Bavachinin (Standard)

    		Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
    Bavachinin (Standard)
  • HY-161999
    α-Glucosidase-IN-73

    		Glycosidase Metabolic Disease Inflammation/Immunology
    α-Glucosidase-IN-73 (compound 16b) is an α-Glucosidase inhibitor with IC50 of 0.158 μM. α-Glucosidase-IN-73 can activate PPAR γ. α-Glucosidase-IN-73 can be used in anti-diabetic and anti-inflammatory studies .
    α-Glucosidase-IN-73
  • HY-146275
    LXRβ agonist-3

    		LXR Cancer
    LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma .
    LXRβ agonist-3
  • HY-173474
    ERβ agonist-1

    		Estrogen Receptor/ERR Androgen Receptor Cancer
    ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
    ERβ agonist-1
  • HY-159582
    ACKR3 agonist 1

    		CXCR Cardiovascular Disease
    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 .
    ACKR3 agonist 1
  • HY-173622
    PPARγ agonist 18

    		PPAR Metabolic Disease Endocrinology
    PPARγ agonist 18 is a PPARγ inhibitor (KD: 3.75 μM). PPARγ agonist 18 can inhibit CDK5-mediated phosphorylation of PPARγ at Ser245. PPARγ agonist 18 can be used in insulin resistance research .
    PPARγ agonist 18
  • HY-110161
    sst2 Receptor agonist-1

    		Somatostatin Receptor Cardiovascular Disease Endocrinology
    sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect .
    sst2 Receptor agonist-1
  • HY-170992
    Autophagy agonist-1

    		Autophagy CDK Atg8/LC3 PINK1/Parkin Cancer
    Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC50s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells .
    Autophagy agonist-1
  • HY-163862
    PPARα agonist 3

    		PPAR Reactive Oxygen Species Inflammation/Immunology
    PPARα agonist 3 (Compound A229) is a PPARα agonist (EC50: 590 nM). PPARα agonist 3 inhibits TBHP or 4-HNE (HY-113466)-induced production of ROS .
    PPARα agonist 3
  • HY-172147
    SSTR4 agonist 5

    		Somatostatin Receptor Neurological Disease
    SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
    SSTR4 agonist 5
  • HY-162466
    ABA receptor agonist 1

    		Proton Pump Others
    ABA receptor agonist 1 (compound 4c) is a receptor agonist for abscisic acid (ABA). ABA receptor agonist 1 can inhibit seed germination and seedling growth of Arabidopsis and rice, stomatal closure and drought resistance of wheat and soybean .
    ABA receptor agonist 1
  • HY-12095
    CB1 inverse agonist 2

    		Cannabinoid Receptor Neurological Disease
    CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
    CB1 inverse agonist 2
  • HY-148922
    PPARα/γ agonist 2

    		PPAR Metabolic Disease
    PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
    PPARα/γ agonist 2
  • HY-153798
    GLP-1 receptor agonist 10

    		GLP Receptor Metabolic Disease
    GLP-1 receptor agonist 10 (compound 42) is an agonist of GLP Receptor. GLP-1 receptor agonist 10 inhibits food intake and reduces glucose excursion in mice. GLP-1 receptor agonist 10 can be used in the study of type 2 diabetes (T2DM) and obesity .
    GLP-1 receptor agonist 10
  • HY-144126
    S1P1 agonist 5

    		LPL Receptor Inflammation/Immunology
    S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
    S1P1 agonist 5
  • HY-162850
    DOR agonist 2

    		Opioid Receptor TNF Receptor NF-κB ERK Neurological Disease Inflammation/Immunology
    DOR agonist 2 (Compound 3) is a Delta Opioid Receptor agonist. DOR agonist 2 can inhibit the expression of TNF-α, prevent NF-κB transport to the nucleus, and activate the G protein-mediated ERK1/2 pathway. DOR agonist 2 can be used in the study of neurodegenerative diseases .
    DOR agonist 2
  • HY-158180
    A3AR agonist 4

    		Adenosine Receptor Inflammation/Immunology
    A3AR agonist 4 is an A3 adenosine receptor (A3AR) agonist (Ki: 1.24 nM for hA3AR). A3AR agonist 4 inhibits cAMP production with an EC50 of 0.17 nM. A3AR agonist 4 can be used for research of inflammation and pain .
    A3AR agonist 4
  • HY-149833
    ERRγ inverse agonist 2

    		Estrogen Receptor/ERR Infection Metabolic Disease
    ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities .
    ERRγ inverse agonist 2
  • HY-144604
    FPR2 agonist 2

    		Formyl Peptide Receptor (FPR) Infection Neurological Disease
    FPR2 agonist 2 is a potent and permeates the blood?brain barrier FPR2 agonist with an EC50 of 0.13 μM, 1.1 μM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity .
    FPR2 agonist 2
  • HY-153265
    TAS2R14 agonist-2

    		Taste Receptor Metabolic Disease
    TAS2R14 agonist-2 (compound 28.1) is a potent and selective TAS2R14 inhibitor with an EC50 value of 72 nM .
    TAS2R14 agonist-2
  • HY-172087
    VDR agonist 3

    		VD/VDR Inflammation/Immunology
    VDR agonist 3 (Compound E15) is a potent vitamin D receptor (VDR) agonist. VDR agonist 3 can effectively inhibit HSC activation through VDR. VDR agonist 3 significantly reduces liver fibrosis without causing hypercalcemia in a CCl4-induced mouse liver fibrosis model .
    VDR agonist 3
  • HY-171069
    FFA2 agonist-1

    		Free Fatty Acid Receptor Metabolic Disease
    FFA2 agonist-1 (Compound 4) is the agonist for Free fatty acid receptor 2 (FFA2/GPR43) with an EC50 of 81 nM. FFA2 agonist-1 exhibits activity in β-arrestin-2 recruitment assay and cAMP inhibition assay with EC50 of 1.2 μM and 0.53 μM. FFA2 agonist-1 leads to appetite regulating peptide YY (PYY) mucosal responses, inhibits the fat accumulation, intestinal functions and food intake, and can be used for obesity research .
    FFA2 agonist-1
  • HY-155116
    5-HT6 agonist 1

    		5-HT Receptor Neurological Disease
    5-HT6 agonist 1 (Compound 19) is a 5-HT6 agonist (Ki: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability .
    5-HT6 agonist 1
  • HY-142703
    RORγt inverse agonist 28

    		ROR Inflammation/Immunology
    RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .
    RORγt inverse agonist 28
  • HY-142806
    RORγt inverse agonist 26

    		ROR Inflammation/Immunology
    RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .
    RORγt inverse agonist 26
  • HY-168438
    ERBB agonist-1

    		EGFR Akt ERK Cardiovascular Disease
    ERBB agonist-1 (Compound EF-1) is an agonist for ERBB4, that activates the ERBB4 signaling pathway by inducing dimerization of the ERBB4 receptor with an EC50 of 10.5 μM. ERBB agonist-1 induces phosphorylation of Akt and ERK1/2, reduces the collagen expression in cardiac fibroblasts, inhibits H2O2-induced cardiomyocyte death and Ang II (HY-13948)-induced cardiomyocyte hypertrophy. ERBB agonist-1 prevents fibrosis and exhibits cardioprotective efficacy in mouse models .
    ERBB agonist-1
  • HY-151799
    P62-RNF168 agonist-1

    		p62 E1/E2/E3 Enzyme Apoptosis Cancer
    P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
    P62-RNF168 agonist-1
  • HY-P10302
    GLP-1R/GIPR agonist-1

    		GLP Receptor Insulin Receptor Metabolic Disease
    GLP-1R/GIPR AgonIST-1 is a double-receptor agonist for GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulin releasing peptide). GLP-1R/GIPR agonist-1 lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
    GLP-1R/GIPR agonist-1
  • HY-P10302A
    GLP-1R/GIPR agonist-1 (soduim)

    		GLP Receptor Metabolic Disease
    GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
    GLP-1R/GIPR agonist-1 (soduim)
  • HY-135982
    GPR81 agonist 1
    2 Publications Verification

    		 Hydroxycarboxylic Acid Receptor (HCAR) Metabolic Disease
    GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a .
    GPR81 agonist 1
  • HY-159146
    PPARα agonist 4

    		PPAR STING Reactive Oxygen Species Neurological Disease Inflammation/Immunology
    PPARα agonist 4 (compound BH400) is a PPARα agonist (EC50= 1.2 μM). PPARα agonist 4 also inhibits STING (IC50: 8.1 μM). PPARα agonist 4 reduces the CoCl2-induced production of ROS and LPS-induced secretion of IL-6. The PPARα agonist 4 restores the decreased expression of PCG1α induced by LPS .
    PPARα agonist 4
  • HY-142937
    RORγt agonist 2

    		ROR Inflammation/Immunology
    RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17) .
    RORγt agonist 2
  • HY-142938
    RORγt agonist 3

    		ROR Inflammation/Immunology
    RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23) .
    RORγt agonist 3
  • HY-173393
    LXRα agonist 1

    		LXR Cancer
    LXRα agonist 1 (Compound 40) is a selective LXRα agonist (EC50: 42 nM). LXRα agonist 1 also has a certain agonistic effect on LXRβ (EC50: 266 nM). LXRα agonist 1 promotes target gene transcription by stabilizing the ligand binding domain (LBD) of LXRα. LXRα agonist 1 exhibits potent antitumor effects in hepatocellular carcinoma cells when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the study of lipotoxic cancers .
    LXRα agonist 1
  • HY-10013
    Taranabant
    2 Publications Verification

    MK-0364

    		 Cannabinoid Receptor Metabolic Disease
    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
    Taranabant
  • HY-149429
    PPARδ agonist 9

    		PPAR Metabolic Disease
    PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) .
    PPARδ agonist 9
  • HY-169404
    PPARγ agonist 15

    		PPAR Metabolic Disease
    PPARγ agonist 15 (Compound 7c) is an agonist for PPARγ. PPARγ agonist 15 inhibits the expression of alpha-amylase (HPA) and alpha-glucosidase (HLAG) with IC50 of 28.35 µM and 26.21 µM. PPARγ agonist 15 enhances glucose uptake in the L6 myotube cell. PPARγ agonist 15 improves glucose homeostasis, insulin sensitivity, and lipid metabolism in rat Streptozotocin (HY-13753)-induced diabetes model .
    PPARγ agonist 15
  • HY-159944
    PPARγ agonist 14

    		PPAR Neurological Disease Metabolic Disease Inflammation/Immunology
    PPARγ agonist 14 (compound 3) is a PPARy agonist (EC50=2.4 μM) with anti-diabetic activity. PPARγ agonist 14 can improve intracellular glucose uptake, promote insulin release, and lower blood sugar. In addition, PPARγ agonist 14 also improves mitochondrial function, reduces oxidative stress, and inhibits inflammatory factors. PPARγ agonist 14 can be used in the study of neurodegenerative diseases, neuroinflammatory diseases, and other diseases .
    PPARγ agonist 14
  • HY-149899
    VDR agonist 2

    		VD/VDR Others
    VDR agonist 2 (compound 16i) is a VDR (vitamin D receptor) agonist that can effectively inhibit TGF-β1-induced activation of hepatic stellate cells (HSC). VDR agonist 2 has significant anti-hepatic fibrosis effects both in vitro and in vivo .
    VDR agonist 2
  • HY-142699
    SSTR4 agonist 2

    		Somatostatin Receptor Inflammation/Immunology
    SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107) .
    SSTR4 agonist 2
  • HY-168719
    PPARγ agonist 16

    		PPAR Inflammation/Immunology
    PPARγ agonist 16 (Compound 4G) is the agonist for PPARγ, that competitively binds to LBD domain of PPARγ with IC50 of 1790 nM. PPARγ agonist 16 inhibits the ear swelling in mouse model, and exhibits anti-hyperglycemic in Streptozotocin (HY-13753)-induced mouse diabetes mellitus model .
    PPARγ agonist 16
  • HY-15380
    PNU‐142721

    		HIV Reverse Transcriptase Infection
    PNU-142721 is a reverse transcriptase inhibitor and PXR agonist that effectively inhibits various type I HIV variants .
    PNU‐142721
  • HY-155705
    BMP agonist 1

    		TGF-β Receptor GSK-3 β-catenin Others
    BMP agonist 1 (compound 2 b) is a small-molecule agonist of bone morphogenic protein (BMP). BMP induces C2C12 cell differentiation with BMP and highly depends on active BMP signaling. BMP agonist 1 inhibits GSK3β, increases β-catenin signaling and synergistically regulates Id2and Id3 expression. BMP agonist 1 is used in diseases and defects of the skeleton research .
    BMP agonist 1
  • HY-151932
    FXR agonist 3

    		FXR Inflammation/Immunology
    FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level .
    FXR agonist 3
  • HY-107319
    Almitrine mesylate

    Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate

    		 Potassium Channel Cardiovascular Disease Neurological Disease
    Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca 2+-dependent K + channel.
    Almitrine mesylate

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