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Non-peptidic

" in MedChemExpress (MCE) Product Catalog:

50

Inhibitors & Agonists

2

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108579
    UCL 1684 dibromide

    		Potassium Channel Cardiovascular Disease
    UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness .
    UCL 1684 dibromide
  • HY-160239
    HFI-437

    		Aminopeptidase Neurological Disease
    HFI-437 is a potent non-peptidic insulin-regulated aminopeptidase (IRAP) inhibitor with a Ki of 20 nM. HFI-437 is a cognitive enhancer .
    HFI-437
  • HY-33009
    AS057278

    		Others Neurological Disease
    AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia .
    AS057278
  • HY-143216
    Ensitrelvir
    5+ Cited Publications

    S-217622

    		 SARS-CoV Virus Protease Infection
    Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) .
    Ensitrelvir
  • HY-143216A
    Ensitrelvir fumarate
    5+ Cited Publications

    S-217622 fumarate

    		 SARS-CoV Virus Protease Infection
    Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) .
    Ensitrelvir fumarate
  • HY-114091
    PF-00356231 hydrochloride
    1 Publications Verification

    		 MMP Inflammation/Immunology
    PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively .
    PF-00356231 hydrochloride
  • HY-151197
    HIV protease-IN-1

    		HIV Protease Infection
    HIV protease-IN-1 (compound 1·succinate) is a potent HIV protease non-peptidic inhibitor, can be used to research AIDS .
    HIV protease-IN-1
  • HY-U00188
    A81988

    Abbott81988

    		 Angiotensin Receptor Cardiovascular Disease Endocrinology
    A81988 is a potent, competitive, non-peptidic antagonist of angiotensin AT1 receptors.
    A81988
  • HY-101580
    Paliroden

    SR 57667

    		 Others Neurological Disease
    Paliroden is an orally bioactive neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophines, used for treatment of Alzheimer's Disease and Parkinson's.
    Paliroden
  • HY-125182
    SMCypI C31

    		Cyclophilin HCV Infection
    SMCypI C31 is a non-peptidic cyclophilin inhibitor with potent peptidyl-prolyl cis/trans isomerases (PPIase) inhibitory activity (IC50 of 0.1 µM). SMCypI C31 shows pangenotype anti-HCV activity with EC50s ranging from 1.20 to 7.76 μM for genotype 1a, 1b, 2a, 3a, and 5a HCV subgenomic replicons (HCV-SGRs) and chimeric genotype 2a/4a HCV-SGRs. SMCypI C31 disrupts the cyclophilin A-NS5A interaction .
    SMCypI C31
  • HY-137322
    THX-B

    		Neurotensin Receptor Neurological Disease Metabolic Disease
    THX-B is a potent and non-peptidic p75 NTR (neurotrophin receptor p75) antagonist. THX-B can be used in the research of diabetic kidney disease, neurodegenerative and inflammatory disorders .
    THX-B
  • HY-18006
    NKP608
    1 Publications Verification

    		 Neurokinin Receptor Neurological Disease Endocrinology
    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.
    NKP608
  • HY-18694
    CGS 27023A

    		MMP Inflammation/Immunology
    CGS 27023A is a non-peptidic and orally active MMP inhibitor with the Ki values of 43, 33, 20 and 8 nM for MMP-3, MMP-1, MMP-2 amd MMP-9, respectively. CGS 27023A can be used for study of arthritis .
    CGS 27023A
  • HY-108624
    CYM 50769

    		Neuropeptide B/W Receptor Cardiovascular Disease Inflammation/Immunology
    CYM 50769 is a non-peptidic selective antagonist of neuropeptides B and W receptor 1 (NPBWR1). CYM 50769 can attenuates the NPW-23-induced cell proliferation in ATDC5. CYM 50769 can be used for researching endochondral bone formation .
    CYM 50769
  • HY-12168
    Tanomastat

    BAY 12-9566

    		 MMP Cancer
    Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
    Tanomastat
  • HY-10472
    LY2811376
    10+ Cited Publications

    		 Beta-secretase Neurological Disease
    LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
    LY2811376
  • HY-106982
    Ezlopitant

    CJ-11,974

    		 Neurokinin Receptor Neurological Disease Metabolic Disease
    Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research .
    Ezlopitant
  • HY-12168B
    (Rac)-Tanomastat

    (Rac)-BAY 12-9566

    		 MMP Cancer
    (Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
    (Rac)-Tanomastat
  • HY-114091A
    PF-00356231

    		MMP Inflammation/Immunology
    PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively .
    PF-00356231
  • HY-123270
    RP23618

    		CCR Infection Inflammation/Immunology
    RP23618 is a non peptidic RANTES antagonist with the IC50 of 3 μM. RP23618 inhibit RANTES-induced chemotaxis of THP-1 cells .
    RP23618
  • HY-101317A
    TAN-67

    SB-205607

    		 Opioid Receptor Metabolic Disease
    TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
    TAN-67
  • HY-101706
    CGP48369

    		Angiotensin Receptor Cardiovascular Disease Endocrinology
    CGP48369 is a nonpeptidic angiotensin II receptor antagonist, used for anti-hypertensive research.
    CGP48369
  • HY-138984
    GRT2932Q

    		Opioid Receptor Neurological Disease
    GRT2932Q is a nonpeptidic opioid receptor-like 1 (ORL1) agonist .
    GRT2932Q
  • HY-10658
    AC-7954

    		Urotensin Receptor Cardiovascular Disease
    AC-7954 is a selective nonpeptidic urotensin receptor agonist (EC50: 300 nM at the human UII receptor) .
    AC-7954
  • HY-129648
    AC-7954 free base

    		Urotensin Receptor Cardiovascular Disease
    AC-7954 free base is a selective nonpeptidic urotensin receptor agonist (EC50: 300 nM at the human UII receptor) .
    AC-7954 free base
  • HY-110123
    ML-00253764 hydrochloride

    		Melanocortin Receptor Endocrinology Cancer
    ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 µM and 0.103 µM, respectively .
    ML-00253764 hydrochloride
  • HY-168048
    ZINC09518833

    		Proteasome Cancer
    ZINC09518833 is a α-ketoamide nonpeptidic proteasome inhibitor with an IC50 value of 12.4 μM. ZINC09518833 binds both primed and nonprimed sites of the proteasome. ZINC09518833 is promising for research of multiple myeloma (MM) .
    ZINC09518833
  • HY-12836
    IFN alpha-IFNAR-IN-1

    		IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
    IFN alpha-IFNAR-IN-1
  • HY-149774
    GC-78-HCl

    		SARS-CoV Infection
    GC-78-HCl is an orally and nonpeptidic SARS-CoV-2 M pro inhibitor, with an IC50 of 0.19 μM for enzyme. GC-78-HCl has excellent antiviral activity and favorable pharmacokinetic properties .
    GC-78-HCl
  • HY-113824
    RID-F

    Ridaifen-F

    		 Proteasome Cancer
    RID-F (Ridaifen-F), a Tamoxifen (HY-13757A) derivative, is a nonpeptidic proteasome inhibitor. RID-F inhibits human 20S proteasome activity, with IC50s of 0.64, 0.34, and 0.43 μM for CT-L, T-L, and PGPH, respectively .
    RID-F
  • HY-120528
    GB-110

    		Protease Activated Receptor (PAR) Inflammation/Immunology Cancer
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM .
    GB-110
  • HY-120528A
    GB-110 hydrochloride
    1 Publications Verification

    		 Protease Activated Receptor (PAR) Inflammation/Immunology Cancer
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM .
    GB-110 hydrochloride
  • HY-101317
    TAN-67 dihydrobromide

    SB-205607 dihydrobromide

    		 Opioid Receptor Neurological Disease
    TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke .
    TAN-67 dihydrobromide
  • HY-10722
    DX-9065a

    		Factor Xa Cardiovascular Disease
    DX-9065a is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a Ki of 41 nM for human FXa. DX-9065a has low activity against other serine proteases. DX-9065a has strong anticoagulant actions .
    DX-9065a
  • HY-145086
    R-PSOP

    		Others Metabolic Disease
    R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
    R-PSOP
  • HY-15652
    Freselestat

    ONO-6818; ONO-PO-736

    		 Elastase Inflammation/Immunology
    Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
    Freselestat
  • HY-15652A
    Freselestat quarterhydrate

    ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate

    		 Elastase Inflammation/Immunology
    Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
    Freselestat quarterhydrate
  • HY-19745
    BMS-202
    15+ Cited Publications

    		 PD-1/PD-L1 Apoptosis Cancer
    BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity .
    BMS-202
  • HY-124637
    ALE-0540

    		Others Neurological Disease
    ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC50 values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the treatment of pain .
    ALE-0540
  • HY-19745B
    BMS-202 hydrochloride

    		PD-1/PD-L1 Apoptosis Cancer
    BMS-202 hydrochloride is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 hydrochloride binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 hydrochloride has antitumor activity .
    BMS-202 hydrochloride
  • HY-12836A
    IFN alpha-IFNAR-IN-1 hydrochloride
    Maximum Cited Publications
    20 Publications Verification

    		 IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. IFN alpha-IFNAR-IN-1 hydrochloride inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) (IC50=2-8 μM) .
    IFN alpha-IFNAR-IN-1 hydrochloride
  • HY-17473
    Embelin
    4 Publications Verification

    Embelic acid; Emberine; NSC 91874

    		 IAP NF-κB Apoptosis Autophagy Cancer
    Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
    Embelin
  • HY-107732
    JNJ-5207787

    		Neuropeptide Y Receptor Neurological Disease
    JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors .
    JNJ-5207787
  • HY-16474
    Relugolix

    TAK-385

    		 GnRH Receptor Endocrinology Cancer
    Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
    Relugolix
  • HY-16474R
    Relugolix (Standard)

    		GnRH Receptor Endocrinology Cancer
    Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
    Relugolix (Standard)
  • HY-16474S
    Relugolix-d6

    TAK-385-d6

    		 Isotope-Labeled Compounds GnRH Receptor Endocrinology Cancer
    Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
    Relugolix-d6
  • HY-155527
    SARS-CoV-2 Mpro-IN-9

    		SARS-CoV Infection
    SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 M pro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM) .
    SARS-CoV-2 Mpro-IN-9
  • HY-17473R
    Embelin (Standard)

    		IAP NF-κB Apoptosis Autophagy Cancer
    Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
    Embelin (Standard)
  • HY-19306
    SB-267268

    		Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression .
    SB-267268
  • HY-163913
    SARS-CoV-IN-5

    		SARS-CoV Infection
    SARS-CoV-IN-5 (compound 49) is a highly selective, nonpeptidic and noncovalent 3CL pro inhibitor with IC50s of 38 nM, 21.1 nM and 86 nM for 3CL pro of SARS-CoV-1, SARS-CoV-2, Bat coronavirus WIV1, respectively. SARS-CoV-IN-5 inhibits the replication of the SARS-CoV-2 delta variant with an EC50 of 0.272 μM. SARS-CoV-IN-5 significantly reduces the lung viral copies in a K18-hACE2 transgenic mouse model. SARS-CoV-IN-5 has good target-specific and potential broad-spectrum anticoronavirus activities against SARS-CoV-1, WIV1, MERS, HCoV-OC43, HCoV-229E, and HKU9 .
    SARS-CoV-IN-5

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