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Fibrosis model

" in MedChemExpress (MCE) Product Catalog:

138

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3

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1

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14

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6

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13

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2

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1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-Y0698
    Thioacetamide
    4 Publications Verification

    Acetothioamide; TAA; Thiacetamide

    Necroptosis Neurological Disease Inflammation/Immunology Cancer
    Thioacetamide (TAA) is an indirect hepatotoxin and causes parenchymal cell necrosis. Thioacetamide requires metabolic activation by microsomal CYP2E1 to thioacetamide-S-oxide initially and then to thioacetamide-S-dioxide, which is a highly reactive metabolite, and its reactive metabolites covalently bind to proteins and lipids thereby causing oxidative stress and centrilobular necrosis. Thioacetamide can induce chronic liver fibrosis, encephalopathy and other events model .
    Thioacetamide
  • HY-150298
    Soquelitinib
    3 Publications Verification

    CPI-818

    Itk Inflammation/Immunology Cancer
    Soquelitinib (CPI-818) is an orally active and highly selective covalent interleukin-2-inducible kinase (ITK) inhibitor. Soquelitinib is active in six different models of T cell-mediated inflammatory and immune disease, including acute and chronic asthma, pulmonary fibrosis, systemic sclerosis (scleroderma), psoriasis, and acute graft versus host disease with Th2 cytokine product inhibition. Soquelitinib increases tumor infiltration of normal CD8 + cells that possess enhanced T effector function .
    Soquelitinib
  • HY-158426
    2-APQC
    1 Publications Verification

    Sirtuin Cardiovascular Disease
    2-APQC is an orally active and selective agonist of Sirtuin-3 (SIRT3) (Kd=2.756 μM), antagonizes Isoproterenol/ISO (HY-B0468)-induced cytotoxicity. 2-APQC activates the SIRT3-PYCR1 axis to enhance mitochondrial proline metabolism and inhibit the ROS-p38MAPK pathway by inhibiting signaling pathways such as mTOR-p70S6K, JNK, and TGF-β/Smad3. 2-APQC also activates the AMPK-Parkin axis to alleviate myocardial hypertrophy and fibrosis and protect cardiac function. 2-APQC can be used in the study of heart failure .
    2-APQC
  • HY-148799

    EDG-5506

    Myosin Others
    Sevasemten is an orally active, selective allosteric inhibitor of skeletal muscle myosin that protects skeletal muscle from contraction-induced injury. Sevasemten decreases muscle damage biomarkers and fibrosis while increasing muscle strength and activity in in Duchenne muscular dystrophy disease models .
    Sevasemten
  • HY-174990

    15-PGDH Metabolic Disease Inflammation/Immunology
    HW201877 is a potent and orally active 15-prostaglandin dehydrogenase (15-PGDH) inhibitor with an IC50 of 3.6 nM. HW201877 demonstrates robust cellular efficacy in elevating PGE2 levels in A549 cells and exhibits remarkable efficacy in animal models of tissue injury and fibrosis. HW201877 can be used for the study of inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF) and Crohn’s disease (CD) .
    HW201877
  • HY-N2995
    Poricoic acid A
    1 Publications Verification

    Poricoic acid A(F)

    NF-κB Keap1-Nrf2 AMPK TGF-beta/Smad Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin .
    Poricoic acid A
  • HY-P4860
    Adropin (34-76) (human, mouse, rat)
    1 Publications Verification

    Akt Gli JNK PKA Metabolic Disease
    Adropin (34-76) is a secretory domain of Adropin. Adropin (34-76) can inhibit cAMP level and glucose production in hepatocytes, and has a hypoglycemic effect. Adropin (34-76) plays an antifibrotic role by inhibiting the GLI1 signaling pathway .
    Adropin (34-76) (human, mouse, rat)
  • HY-P99351

    Anti-MMP9 Reference Antibody (andecaliximab)

    MMP Cancer
    Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) .
    Andecaliximab
  • HY-N1548
    Prunasin
    1 Publications Verification

    DNA/RNA Synthesis Inflammation/Immunology
    Prunasin is an orally active cyanogenic glucoside and the main metabolite of Amygdalin (HY-N0190). Prunasin can specifically inhibit rat DNA polymerase β (IC50: 98 μM). Prunasin has anti-inflammatory and anti-fibrotic activities. Prunasin can be used in the research of diseases such as liver fibrosis .
    Prunasin
  • HY-138304
    CC-90001
    3 Publications Verification

    JNK Inflammation/Immunology
    CC-90001 is a potent, selective and orally active inhibitor of c-Jun N-terminal kinase (JNK). CC-90001 shows 12.9-fold selectivity for JNK1 over JNK2 in a cell-based model. CC-90001 can be used for the research of idiopathic pulmonary fibrosis .
    CC-90001
  • HY-149136

    Integrin TGF-beta/Smad Inflammation/Immunology
    MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety .
    MORF-627
  • HY-107830

    Endogenous Metabolite Collagen Infection Metabolic Disease
    Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
    Methyl cholate
  • HY-P991363

    Myosin STAT Inflammation/Immunology
    AX-202 is a humanized IgG4 monoclonal antibody targeting S100A4. AX-202 neutralizes the activity of S100A4. AX-202 effectively reverses established fibrosis and reduces inflammation and fibrosis-related biomarkers in a mouse model of skin fibrosis. AX-202 is applicable for the research of fibrotic and inflammatory diseases .
    AX-202
  • HY-103370

    BA 7602-06

    Chloride Channel Inflammation/Immunology
    Talniflumate (BA 7602-06) is the proagent of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase . Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome .
    Talniflumate
  • HY-135644
    Rencofilstat
    1 Publications Verification

    CRV431

    Cyclophilin Sirtuin Nuclear Factor of activated T Cells (NFAT) Interleukin Related Cancer
    Rencofilstat (CRV431) is an orally active pan-cyclophilin inhibitor with IC50 values of 2.5 nM, 3.1 nM, 2.8 nM, 7.3 nM for Cyp A, CypB, Cyp D and Cyp G, respectively. Rencofilstat reduces fibrosis and tumor growth in models of chronic liver disease. Rencofilstat can be used for the study of nonalcoholic steatohepatitis (NASH), hepatocellular carcinoma and viral hepatitis-induced liver disease .
    Rencofilstat
  • HY-47888

    Integrin Inflammation/Immunology
    PLN-1474 (compound 1) is an orally active and selective ανβ1 integrin inhibitor with an IC50 value of <50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or researching a fibrotic or cirrhotic disease or disorder.
    PLN-1474
  • HY-P99053
    Tralokinumab
    2 Publications Verification

    CAT354

    Interleukin Related Apoptosis Caspase Cadherin Inflammation/Immunology
    Tralokinumab (CAT354) is a humanized IgG4 monoclonal antibody that specifically binds to and neutralizes IL-13. Tralokinumab can be used in the research of diseases such as asthma, atopic dermatitis, and pulmonary fibrosis .
    Tralokinumab
  • HY-132850

    BLD-2660

    Proteasome Interleukin Related Infection Inflammation/Immunology
    Dazcapistat (BLD-2660) is an orally active small-molecule inhibitor of calpain 1, 2, and 9 (calpain 1, 2, 9). Dazcapistat reduces the expression/production level of IL-6 in injured lung tissue and alleviates fibrosis . Dazcapistat exerts anti-fibrotic effects in various animal models of fibrosis in the skin, liver and lung . Dazcapistat can be used in research related to coronavirus disease 2019 (COVID-19) and idiopathic pulmonary fibrosis .
    Dazcapistat
  • HY-168906

    Bradykinin Receptor PI3K Akt TNF Receptor ERK Neurological Disease Inflammation/Immunology
    BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
    BI-113823
  • HY-109106A

    SK-1403; AJT240; PLS240

    CaSR Endocrinology
    Upacicalcet sodium is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet sodium reduces serum intact parathyroid hormone (iPTH) and serum Ca 2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet sodium sodium improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet sodium sodium inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet sodium is useful for studying SHPT .
    Upacicalcet sodium
  • HY-156430

    MMP Cancer
    MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
    MMP-7-IN-3
  • HY-155657

    Src Inflammation/Immunology
    BT424 is a specific HCK inhibitor. BT424 can regulate macrophage activation and autophagy in vitro. BT424 ameliorates inflammation and kidney fibrosis in UUO model .
    BT424
  • HY-13706A

    TM30089

    Prostaglandin Receptor Inflammation/Immunology
    CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model .
    CAY10471
  • HY-151481

    FXR Metabolic Disease
    FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
    FXR antagonist 1
  • HY-P990107

    TGF-β Receptor Cancer
    Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
    Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8)
  • HY-148230

    Interleukin Related HIF/HIF Prolyl-Hydroxylase Autophagy Others
    TFEB Decoy ODN sodium is a synthetic oligonucleotide with a hairpin ring structure, which were designed to inhibit Transcription factor EB (TFEB). TFEB decoy ODN inhibited fibrosis and autophagy in a UUO mouse model. The TFEB decoy ODNs also showed anti-inflammatory effects.
    TFEB Decoy ODN sodium
  • HY-146434
    TGFβ-IN-2
    1 Publications Verification

    TGF-beta/Smad Inflammation/Immunology
    TGFβ-IN-2 is an orally active TGF-β inhibitor. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 demonstrates excellent anti-fibrotic efficacy in Bleomycin (HY-108345)-induced pulmonary fibrosis model. TGFβ-IN-2 can be used for the study of pulmonary fibrosis .
    TGFβ-IN-2
  • HY-162267

    LPL Receptor Inflammation/Immunology
    LPAR1 antagonist 1 (compound 18) is a potent, oral active and selective LPAR1 antagonist with the IC50 of 3.3 nM. LPAR1 antagonist 1 can be used for study of fibrosis .
    LPAR1 antagonist 1
  • HY-178821

    ROCK TGF-beta/Smad STAT Inflammation/Immunology
    ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research .
    ROCK2-IN-12
  • HY-158315

    Dipeptidyl Peptidase Inflammation/Immunology
    NZ-97 is an inhibitor for dipeptidyl peptidase 4 (DPP4) with an IC50 of 18 nM. NZ-97 exhibits a low initial plasma exposure with Cmax of 0.13 µM, which is eliminated in 8 h. NZ-97 ameliorates damage in the Lipopolysaccharides (HY-D1056)-induced lung injury and Bleomycin (HY-108345)-induced lung fibrosis in mice model .
    NZ-97
  • HY-120268A

    SphK Inflammation/Immunology
    SLM6031434 hydrochloride is the hydrochloride salt form of SLM6031434 (HY-120268). SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD) .
    SLM6031434 hydrochloride
  • HY-143237

    Phosphodiesterase (PDE) Others
    ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research .
    ATX inhibitor 11
  • HY-124072

    Cyclophilin LPL Receptor MDM-2/p53 Apoptosis Reactive Oxygen Species (ROS) Cancer
    HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis .
    HL001
  • HY-167745

    Discoidin Domain Receptor Neurological Disease
    DDR1-IN-9 is a selective inhibitor of DDR1 with significant kinase activity suppression, exhibiting a Kd value of 4.7 nM and an IC50 value of 9.4 nM. DDR1-IN-9 demonstrates reduced potency against a diverse panel of 400 nonmutated kinases, indicating its specificity. Additionally, DDR1-IN-9 shows favorable pharmacokinetic properties and potential therapeutic effects in a model of pulmonary fibrosis.
    DDR1-IN-9
  • HY-171804

    FP-020

    MMP Inflammation/Immunology
    Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC50: < 10  nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin (HY-108345) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma .
    Linvemastat
  • HY-173235

    Galectin Cardiovascular Disease Inflammation/Immunology Cancer
    Galectin-3-IN-6 (Compound 12) is a human and murine galectin-3 (Gal-3) inhibitor, with an IC50 of 12 nM against human galectin-3, an IC50 of 12.6 nM against mutant murine galectin-3 (V160A), and a Kd of 13 nM for human galectin-3, as well as oral bioavailability. Galectin-3-IN-6 reduces the levels of liver fibrosis markers type I collagen and α-smooth muscle actin in mouse models of acute liver injury and fibrosis. Galectin-3-IN-6 can be used for the research of acute liver injury and fibrosis .
    Galectin-3-IN-6
  • HY-137992

    TGF-beta/Smad Inflammation/Immunology
    Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (HY-108345)-induced lung fibrosis mouse model. Aucuparin has anti-inflammatory activity and can inhibit the activation of inflammatory factors by TGF-β .
    Aucuparin
  • HY-P11354

    TGF-β Receptor Apoptosis Interleukin Related Integrin Cadherin Inflammation/Immunology
    THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis .
    THR-123
  • HY-164799

    FXR Inflammation/Immunology
    FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models .
    FXR agonist 12
  • 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-176274

    Fatty Acid Synthase (FASN) Stearoyl-CoA Desaturase (SCD) Reactive Oxygen Species (ROS) Interleukin Related TNF Receptor SOD LDLR Glutathione Peroxidase Metabolic Disease Inflammation/Immunology
    FASN/SCD-IN-1 is a Silybin (HY-N0779A) derivative, an orally active inhibitor of Fatty Acid Synthase (FASN)/Stearoyl-CoA Desaturase (SCD). FASN/SCD-IN-1 has shown in vitro activity in inhibiting lipid deposition, reducing FASN and SCD transcriptional levels, and exhibiting antioxidant, anti-inflammatory, and anti-fibrotic activities. FASN/SCD-IN-1 has demonstrated significant hepatoprotective effects in a rat model of acute liver injury. FASN/SCD-IN-1 ameliorates the pathological features of MASH liver, including steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative steatohepatitis (MASH). FASN/SCD-IN-1 can be used to study MASH .
    FASN/SCD-IN-1
  • HY-123522

    Phosphodiesterase (PDE) Inflammation/Immunology
    PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo .
    PAT-048
  • HY-P11354A

    TGF-β Receptor Apoptosis Interleukin Related Integrin Cadherin Inflammation/Immunology
    THR-123 TFA is an orally active ALK3 peptide agonist. THR-123 TFA has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 TFA suppresses inflammation, Apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 TFA can be used for the study of kidney fibrosis .
    THR-123 TFA
  • HY-P11297

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    AC-SDKP-NH2 is a substrate peptide of Angiotensin converting enzyme (ACE). AC-SDKP-NH2 has anti-inflammatory and anti-fibrotic activities. AC-SDKP-NH2 directly acts on tissues and prevents or reverses them from excessive fibrosis, but fails to reduce blood pressure and left ventricular hypertrophy (LVH). AC-SDKP-NH2 attenuates inflammation and cell differentiation, proliferation and migration, therefore reducing fibrosis in the heart, vessels and kidneys in mice model. AC-SDKP-NH2 can be used for cardiovascular diseases such as hypertension research .
    AC-SDKP-NH2
  • HY-176194

    Collagen c-Fms PDGFR Src Inflammation/Immunology
    Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model .
    Antifibrotic agent 1
  • 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-175033

    Epigenetic Reader Domain Phosphatase c-Myc Apoptosis Inflammation/Immunology
    BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis .
    BRD4-IN-11
  • HY-120268

    SphK Inflammation/Immunology
    SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD) .
    SLM6031434
  • HY-169940

    HDAC Inflammation/Immunology
    Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases .
    Fibrostat
  • HY-109106

    SK-1403 free acid; AJT240 free acid; PLS240 free acid

    CaSR Endocrinology
    Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT .
    Upacicalcet

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