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Results for "

orally active nonpeptide

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aminopeptidase (1) Angiotensin Receptor (4) Apoptosis (9) Bacterial (5) Bradykinin Receptor (3) Caspase (1) CCR (1) CFTR (3) Cholecystokinin Receptor (8) Complement System (1) CRFR (2) CXCR (1) Endothelin Receptor (10) GCGR (2) GHSR (2) GnRH Receptor (4) Integrin (6) Isotope-Labeled Compounds (2) Neurokinin Receptor (2) Neurotensin Receptor (3) Nuclear Factor of activated T Cells (NFAT) (2) Oxytocin Receptor (1) PGE synthase (1) Prolyl Endopeptidase (PREP) (3) Protease Activated Receptor (PAR) (1) Reactive Oxygen Species (1) SARS-CoV (1) Somatostatin Receptor (2) Thrombopoietin Receptor (10) Vasopressin Receptor (2)
By Research Areas:	Cancer (22) Cardiovascular Disease (25) Endocrinology (23) Infection (7) Inflammation/Immunology (20) Metabolic Disease (14) Neurological Disease (15)
Click Chemistry:	Alkynes (3)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-123744

PD-156707	Endothelin Receptor	Cardiovascular Disease
PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist .

HY-15778

AVE 0991 10+ Cited Publications	Angiotensin Receptor	Cardiovascular Disease Endocrinology
AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC₅₀ of 21 nM .

HY-123617

AZ8838	Protease Activated Receptor (PAR)	Inflammation/Immunology
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK_i of 6.4 for hPAR2 .

HY-14128

NBI-34041 SB-723620	CRFR	Neurological Disease
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC₅₀ of 58.9 nM and a K_i of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.

HY-116567

OPC-51803	Vasopressin Receptor	Metabolic Disease
OPC-51803 is an orally active nonpeptide vasopressin V₂ receptor agonist. OPC-51803 can be used for the research of micturition disorders that result in frequent micturition, such as that from polyuria, nocturnal polyuria, and some kinds of urinary incontinence .

HY-19191

L-159282 MK 996	Angiotensin Receptor	Cardiovascular Disease Endocrinology
L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.

HY-100269

Chymase-IN-1	Others	Inflammation/Immunology
Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC₅₀ of 29 nM.

HY-10308

Lefradafiban	Others	Metabolic Disease
Lefradafiban is an orally active glycoprotein IIb/IIIa receptor antagonist. Lefradafiban can be metabolized to its active form, Fradafiban, a non-peptide GP IIb/IIIa receptor antagonist .

HY-135500

ACT-373898	Endothelin Receptor	Endocrinology
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .

HY-19214

Elisartan HN 65021	Angiotensin Receptor	Cardiovascular Disease Endocrinology
Elisartan is an orally active non-peptide pro-agent of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.

HY-50844

Ibutamoren Mesylate 5 Publications Verification MK-677; MK-0677	GHSR	Endocrinology
Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.

HY-107533

T-98475	GnRH Receptor	Endocrinology
T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC₅₀ of 0.2 nM .

HY-10199A

Ibutamoren MK-677 free base; MK-0677 free base	GHSR	Metabolic Disease
Ibutamoren (MK-677) is an orally active growth hormone secretagogue receptor (GHSR) agonist and a nonpeptide growth hormone secretagogue. Ibutamoren can be used for metabolic research .

HY-168087

GSK3335103	Integrin	Cardiovascular Disease
GSK3335103 is an orally active, non-peptide α_vβ₆ integrin inhibitor (pIC₅₀=8). GSK3335103 can be used in the study of pulmonary fibrosis .

HY-10309

Sibrafiban RO 48-3657	Integrin	Cardiovascular Disease
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation .

HY-109093

Linzagolix KLH-2109; OBE-2109	GnRH Receptor	Inflammation/Immunology Cancer
Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research .

HY-14184

Macitentan 10+ Cited Publications ACT-064992	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-19947

PF-06291874 1 Publications Verification Glucagon receptor antagonists-4	GCGR	Metabolic Disease
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .

HY-19307

SB-273005	Integrin	Inflammation/Immunology
SB-273005 is a potent nonpeptide and orally active integrin antagonist with K_is of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively .

HY-10315

Elarofiban RWJ-53308	Integrin	Cardiovascular Disease
Elarofiban (RWJ-53308) is a nonpeptide, orally active antagonist for fibrinogen receptor α_IIbβ₃ (GPIIb/IIIa), with an IC₅₀ of 0.15 nM. Elarofiban has the potential for platelet mediated thrombotic disorders research .

HY-12080

BX471 Maximum Cited Publications 13 Publications Verification ZK-811752	CCR	Inflammation/Immunology Endocrinology
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a K_i of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

HY-14184A

Macitentan (n-butyl analogue)	Endothelin Receptor	Cardiovascular Disease Endocrinology
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

HY-147416

Vipoglanstat BI 1029539; GS-248; OX-MPI	PGE synthase	Infection Cancer
Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity .

HY-100301

FR167344 free base	Bradykinin Receptor	Inflammation/Immunology Endocrinology
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC₅₀ value of 65 nM and no binding affinity for the B1 receptor.

HY-14184S

Macitentan-d4 ACT-064992-d₄	Isotope-Labeled Compounds Endothelin Receptor Apoptosis	Cardiovascular Disease
Macitentan-d₄ is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].

HY-103226

SC-57461A 1 Publications Verification	Aminopeptidase	Inflammation/Immunology
SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC₅₀s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively .

HY-15778A

AVE 0991 sodium salt 10+ Cited Publications	Angiotensin Receptor	Cardiovascular Disease Endocrinology
AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ ¹²⁵I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC₅₀ of 21 nM .

HY-14789

(R)-Elagolix NBI-56418	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Endocrinology Cancer
Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-14369

Elagolix sodium NBI-56418 sodium	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Endocrinology Cancer
Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-19374

BAY-27-9955	GCGR	Metabolic Disease
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC₅₀ value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .

HY-122237

ATZ-1993	Endothelin Receptor	Cardiovascular Disease
ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pK_i values of 8.69, 7.20, respectively. ATZ-1993 has the potential for the research of intimal hyperplasia after balloon denudation of the carotid artery .

HY-14184R

Macitentan (Standard)	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-110155A

(Rac)-LM11A-31 dihydrochloride	Others	Neurological Disease
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 ^NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist .

HY-10315A

Elarofiban diTFA	Integrin	Cardiovascular Disease
Elarofiban diTFA is the salt form of Elarofiban (HY-10315) with two TFA. Elarofiban diTFA is a nonpeptide, orally active antagonist for fibrinogen receptor α_IIbβ₃ (GPIIb/IIIa), with an IC₅₀ of 0.15 nM. Elarofiban diTFA has the potential for platelet mediated thrombotic disorders research .

HY-108482

CP-96,345	Neurokinin Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
CP-96,345 is a specific, highly potent, and orally active tachykinin and substance P receptor non-peptide inhibitor. CP-96,345 prevents the drop in blood pressure evoked by substance P and neurokinin A. CP-96,345 can be used for researching neurogenic inflammation .

HY-106840A

L-365260 hemihydrate 1 Publications Verification	Cholecystokinin Receptor	Neurological Disease Metabolic Disease
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .

HY-B1330

Proglumide	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .

HY-103354

Proglumide sodium	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .

HY-109155

Paltusotine 1 Publications Verification CRN00808	Somatostatin Receptor	Endocrinology Cancer
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine can be used in research on acromegaly and neuroendocrine tumors .

HY-109155A

Paltusotine hydrochloride CRN00808 hydrochloride	Somatostatin Receptor	Neurological Disease Endocrinology
Paltusotine (CRN00808) hydrochloride is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine hydrochloride has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine hydrochloride can be used in research on acromegaly and neuroendocrine tumors .

HY-106301

Devazepide 3 Publications Verification L-364,718; MK-329	Cholecystokinin Receptor	Metabolic Disease
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC₅₀s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .

HY-103354A

Proglumide hemicalcium	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities .

HY-106203

Crinecerfont SSR-125543	CFTR	Metabolic Disease
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106203A

Crinecerfont hydrochloride SSR-125543 hydrochloride	CFTR	Metabolic Disease
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15011

L-372662 1 Publications Verification	Oxytocin Receptor	Others
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a K_i value of 4.8. The K_d value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V_1aR .

HY-16981

SB-332235	CXCR	Inflammation/Immunology
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC₅₀ of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells .

HY-19676

Pralnacasan VX-740; HMR 3480	Caspase	Inflammation/Immunology
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a K_i of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment .

HY-15041

NVP-SAA164	Bradykinin Receptor	Inflammation/Immunology
NVP-SAA164 is an orally active nonpeptide kinin B₁ receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .

HY-106840

L-365260 1 Publications Verification	Cholecystokinin Receptor	Neurological Disease Metabolic Disease
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .

HY-103377

Antalarmin hydrochloride 2 Publications Verification	CRFR	Inflammation/Immunology Endocrinology
Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a K_i of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome .

Cat. No.	Product Name	Chemical Structure

HY-14184S

Macitentan-d4
Macitentan-d₄ is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].

HY-15306S

Eltrombopag-13C4

1 Publications Verification

Eltrombopag- ¹³C₄ (SB-497115- ¹³C₄) is ^{13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .}

HY-13463BS

Avatrombopag-d8 hydrochloride

Avatrombopag-d₈ (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].

Cat. No.	Product Name		Classification

HY-106203A

Crinecerfont hydrochloride SSR-125543 hydrochloride		Alkynes
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106203

Crinecerfont SSR-125543		Alkynes
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106203B

(R)-Crinecerfont (R)-SSR-125543		Alkynes
(R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .

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