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Results for "

Non-peptidic

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aminopeptidase (1) Angiotensin Receptor (2) Apoptosis (2) Autophagy (1) Beta-secretase (1) Elastase (2) GLP Receptor (1) GnRH Receptor (2) HCV (1) HIV Protease (1) IAP (1) IFNAR (2) Isotope-Labeled Compounds (1) Melanocortin Receptor (1) MMP (4) Neurokinin Receptor (2) Neuropeptide Y Receptor (1) Neurotensin Receptor (1) NF-κB (1) Opioid Receptor (1) PD-1/PD-L1 (1) Potassium Channel (1) Protease Activated Receptor (PAR) (2) Proteasome (1) SARS-CoV (4) Urotensin Receptor (1) Virus Protease (2)
By Research Areas:	Cancer (10) Cardiovascular Disease (5) Endocrinology (6) Infection (5) Inflammation/Immunology (9) Metabolic Disease (4) Neurological Disease (11)

By Targets:

Aminopeptidase (1)

Angiotensin Receptor (2)

Apoptosis (2)

Autophagy (1)

Beta-secretase (1)

Elastase (2)

GLP Receptor (1)

GnRH Receptor (2)

HCV (1)

HIV Protease (1)

IAP (1)

IFNAR (2)

Isotope-Labeled Compounds (1)

Melanocortin Receptor (1)

MMP (4)

Neurokinin Receptor (2)

Neuropeptide Y Receptor (1)

Neurotensin Receptor (1)

NF-κB (1)

Opioid Receptor (1)

PD-1/PD-L1 (1)

Potassium Channel (1)

Protease Activated Receptor (PAR) (2)

Proteasome (1)

SARS-CoV (4)

Urotensin Receptor (1)

Virus Protease (2)

By Research Areas:

Cancer (10)

Cardiovascular Disease (5)

Endocrinology (6)

Infection (5)

Inflammation/Immunology (9)

Metabolic Disease (4)

Neurological Disease (11)

Inhibitors & Agonists

Natural
Products

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 I_Na. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness .

HY-160239

HFI-437

Aminopeptidase Neurological Disease

HFI-437 is a potent non-peptidic insulin-regulated aminopeptidase (IRAP) inhibitor with a K_i of 20 nM. HFI-437 is a cognitive enhancer .
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 .
HY-U00188

A81988

Abbott81988
Angiotensin Receptor Cardiovascular Disease Endocrinology

A81988 is a potent, competitive, non-peptidic antagonist of angiotensin AT₁ receptors.

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

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 .

A81988 Abbott81988	Angiotensin Receptor	Cardiovascular Disease Endocrinology
A81988 is a potent, competitive, non-peptidic antagonist of angiotensin AT₁ receptors.

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.

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 .

HY-125182

SMCypI C31	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 .

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) .

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) .

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 .

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 .

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.

HY-135195

Boc5	GLP Receptor	Metabolic Disease
Boc5 is a non-peptidic glucagon-like peptide-1 receptor agonist. Boc5 causes sustained glycemic control and weight loss in diabetic mice. Boc5 can be used in research of diabetic .

HY-108624

CYM 50769	Others	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 .

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 K_i 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 .

HY-10472

LY2811376 5+ 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.

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 .

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 K_i 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 .

HY-12130

CP 154526

Others Neurological Disease

CP 154526, a non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity .

CP 154526	Others	Neurological Disease
CP 154526, a non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity .

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 .

HY-101706

CGP48369

Angiotensin Receptor Cardiovascular Disease Endocrinology

CGP48369 is a nonpeptidic angiotensin II receptor antagonist, used for anti-hypertensive research.
HY-138984

GRT2932Q

Opioid Receptor Neurological Disease

GRT2932Q is a nonpeptidic opioid receptor-like 1 (ORL1) agonist .
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) .

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

GRT2932Q	Opioid Receptor	Neurological Disease
GRT2932Q is a nonpeptidic opioid receptor-like 1 (ORL1) agonist .

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

HY-110123

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

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).

HY-149774

GC-78-HCl	SARS-CoV
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 .

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 .

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 .

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 .

HY-101317

TAN-67 dihydrobromide SB-205607 dihydrobromide
TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a K_i value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke .

HY-145086

R-PSOP	Others	Metabolic Disease
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the K_is 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 .

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 K_i 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 .

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 K_i 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 .

HY-19745

BMS-202 10+ 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 K_D of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity .

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 .

HY-12836A

IFN alpha-IFNAR-IN-1 hydrochloride Maximum Cited Publications 19 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) .

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 .

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 .

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 .

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].

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) .

HY-19306

SB-267268
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with K_is 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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-17473

Embelin 4 Publications Verification Embelic acid; Emberine; NSC 91874	Quinones Classification of Application Fields Source classification Benzene Quinones Plants Embelia laeta (Linn.) Mez Myrsinaceae Disease Research Fields Cancer	IAP NF-κB Apoptosis Autophagy
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 .

Cat. No.	Product Name	Chemical Structure

HY-16474S

Relugolix-d6
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

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].

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