Search Result

Results for "

oral exposure

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Amyloid-β (1) Antibiotic (1) Aryl Hydrocarbon Receptor (3) Bacterial (1) Bradykinin Receptor (2) Collagen (3) Cyclic GMP-AMP Synthase (1) Cytochrome P450 (3) Drug Metabolite (1) EGFR (2) Endogenous Metabolite (2) Enteropeptidase (2) Epoxide Hydrolase (2) ERK (1) Estrogen Receptor/ERR (1) Fatty Acid Synthase (FASN) (1) FGFR (2) Fungal (1) HBV (1) HDAC (1) iGluR (1) Isotope-Labeled Compounds (2) MAP4K (2) nAChR (1) Parasite (1) Phosphodiesterase (PDE) (1) ROCK (2) Serotonin Transporter (1) Sigma Receptor (1) TAM Receptor (1) γ-secretase (2)
By Research Areas:	Cancer (11) Cardiovascular Disease (3) Endocrinology (1) Infection (3) Inflammation/Immunology (12) Metabolic Disease (4) Neurological Disease (10)

By Targets:

5-HT Receptor (2)

Amyloid-β (1)

Antibiotic (1)

Aryl Hydrocarbon Receptor (3)

Bacterial (1)

Bradykinin Receptor (2)

Collagen (3)

Cyclic GMP-AMP Synthase (1)

Cytochrome P450 (3)

Drug Metabolite (1)

EGFR (2)

Endogenous Metabolite (2)

Enteropeptidase (2)

Epoxide Hydrolase (2)

ERK (1)

Estrogen Receptor/ERR (1)

Fatty Acid Synthase (FASN) (1)

FGFR (2)

Fungal (1)

HBV (1)

HDAC (1)

iGluR (1)

Isotope-Labeled Compounds (2)

MAP4K (2)

nAChR (1)

Parasite (1)

Phosphodiesterase (PDE) (1)

ROCK (2)

Serotonin Transporter (1)

Sigma Receptor (1)

TAM Receptor (1)

γ-secretase (2)

By Research Areas:

Cancer (11)

Cardiovascular Disease (3)

Endocrinology (1)

Infection (3)

Inflammation/Immunology (12)

Metabolic Disease (4)

Neurological Disease (10)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15043

ELN-441958	Bradykinin Receptor	Inflammation/Immunology Endocrinology
ELN-441958 is a potent, neutral, competitive and selective bradykinin B₁ receptor antagonist with a K_i of 0.26 nM against native human bradykinin B₁ receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .

HY-W014075

1-Hydroxypyrene	Aryl Hydrocarbon Receptor Cytochrome P450 Collagen	Inflammation/Immunology
1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis .

HY-12769

Mebeverine acid Mebeverine metabolite Mebeverine acid	Drug Metabolite	Neurological Disease
Mebeverine acid (Mebeverine metabolite Mebeverine acid) is a secondary metabolite of Mebeverine. Mebeverine is an antispasmodic agent. Mebeverine acid is a valuable marker of oral exposure to Mebeverine .

HY-W013989

1,3-Dicyclohexylurea	Epoxide Hydrolase	Cardiovascular Disease
1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats .

HY-W014075S

1-Hydroxypyrene-d9	Isotope-Labeled Compounds Aryl Hydrocarbon Receptor Cytochrome P450 Collagen	Inflammation/Immunology
1-Hydroxypyrene-d₉ is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis .

HY-130609A

Aβ42-IN-1 free base	γ-secretase	Neurological Disease
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC₅₀ value of 0.091 μM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease .

HY-142644

ATX inhibitor 7	Phosphodiesterase (PDE)	Inflammation/Immunology
ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.

HY-169199

BAY-405	MAP4K	Cancer
BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration .

HY-148177

Sutidiazine ZY-19489; MMV 253; AZ13721412	Parasite	Infection
Sutidiazine (ZY-19489) is an orally active and antimalarial agent. Sutidiazine inhibits parasitemia-induced infection. Sutidiazine shows short half-lives (approximately 7 h) and an exposure effect .

HY-W014075R

1-Hydroxypyrene (Standard)	Aryl Hydrocarbon Receptor Cytochrome P450 Collagen	Inflammation/Immunology
1-Hydroxypyrene (Standard) is the analytical standard of 1-Hydroxypyrene (HY-W014075). This product is intended for research and analytical applications. 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.

HY-116565

Usmarapride SUVN-D4010	5-HT Receptor	Neurological Disease
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT₄ receptor partial agonist (EC₅₀=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .

HY-130609

Aβ42-IN-1	γ-secretase	Neurological Disease
Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC₅₀?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.

HY-116565A

Usmarapride free base SUVN-D4010 free base	5-HT Receptor	Neurological Disease
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT₄ receptor partial agonist (EC₅₀=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .

HY-158615

STING18 Stimulator of interferon genes 18	Others	Others
STING18 (Stimulator of interferon genes 18) is a compound that inhibits STING protein by utilizing a small molecule active site dimer, with good oral exposure, slow binding kinetics, and functional inhibitory activity on STING-mediated cytokine release.

HY-12769S2

Mebeverine acid-d3 Mebeverine metabolite Mebeverine acid-d₃	Isotope-Labeled Compounds	Neurological Disease
Mebeverine acid-d₃ (Mebeverine metabolite Mebeverine acid-d₃) is deuterium labeled Mebeverine acid. Mebeverine acid (Mebeverine metabolite Mebeverine acid) is a secondary metabolite of Mebeverine. Mebeverine is an antispasmodic agent. Mebeverine acid is a valuable marker of oral exposure to Mebeverine .

HY-W013989R

1,3-Dicyclohexylurea (Standard)	Epoxide Hydrolase	Cardiovascular Disease
1,3-Dicyclohexylurea (Standard) is the analytical standard of 1,3-Dicyclohexylurea. This product is intended for research and analytical applications. 1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats .

HY-143439

LX-039	Estrogen Receptor/ERR	Cancer
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC₅₀ value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high C_max and oral exposure. LX-039 has anti-tumor activity .

HY-W027382

SEP-227900	Endogenous Metabolite	Cancer
SEP-227900 is an orally active and potent DAAO (DAO) inhibitor with potential inhibitory applications. The biological activity of SEP-227900 may show benefits in diseases associated with vitamin D or sunlight exposure. SEP-227900 is expected to play an important role in improving cancer prognosis .

HY-156593

ROCK-IN-9	ROCK	Cancer
ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC₅₀ of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .

HY-16100

BI 99179 1 Publications Verification	Fatty Acid Synthase (FASN)	Metabolic Disease Cancer
BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC₅₀ of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats .

HY-162459

cGAS-IN-3	Cyclic GMP-AMP Synthase	Inflammation/Immunology
cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats .

HY-170945

Antidepressant agent 9	iGluR Serotonin Transporter	Neurological Disease
Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable NMDAR and SERT inhibitor with IC₅₀ values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test .

HY-147684

FGFR-IN-7	FGFR	Neurological Disease
FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research .

HY-156618

Irpagratinib ABSK011	FGFR	Cancer
Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC₅₀<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .

HY-147927

Human enteropeptidase-IN-1	Enteropeptidase	Metabolic Disease
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research .

HY-105110

SCH 39304 SM-8668	Fungal	Infection
SM-8668 is an effective orally active antifungal agent, with median effective doses (ED₅₀) of 0.18, 3.7, and 5.9 mg/kg for systemic candidiasis, aspergillosis, and cryptococcosis in mice, respectively. Pharmacokinetic studies in mice and rats indicate that SM-8668 has a long half-life and a high total exposure. SM-8668 can be used in anti-infective research .

HY-162940

MerTK/Axl-IN-1	TAM Receptor	Inflammation/Immunology Cancer
MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC₅₀s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .

HY-150605

ERK5-IN-3	ERK	Cancer
ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC₅₀ of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC₅₀ of 31 nM .

HY-155992

WLB-89462	Sigma Receptor	Neurological Disease
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (K_i: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .

HY-147859

BChE-IN-8	Amyloid-β	Neurological Disease
BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC₅₀ values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research .

HY-147927A

(S)-Human enteropeptidase-IN-1	Enteropeptidase	Metabolic Disease
(S)-Human enteropeptidase-IN-1 (Compound 6c) is an orally active enteropeptidase inhibitor with low systemic exposure (IC₅₀ (initial): 26 nM; IC₅₀ (app): 1.8 nM). (S)-Human enteropeptidase-IN-1 promotes increased fecal protein output and effectively reduces body weight in a diet-induced obese (DIO) rat model. (S)-Human enteropeptidase-IN-1 inhibits enteropeptidase via a reversible covalent mechanism and prolongs the enzyme inactivation time. (S)-Human enteropeptidase-IN-1 can be used in anti-obesity research .

HY-112142A

(Rac)-AB-423 DVR-23	HBV	Inflammation/Immunology
(Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .

HY-B1325

Cefuroxime axetil	Bacterial Antibiotic	Infection Inflammation/Immunology
Cefuroxime axetil is an orally effective broad-spectrum β-lactam antibiotic that targets bacterial penicillin-binding proteins (PBPs, such as PBP3 and PBP1). Cefuroxime axetil inhibits cell wall synthesis, leading to bacterial lysis and death, with a minimum inhibitory concentration (MIC) of 0.12-4 mg/L for non-typeable Haemophilus influenzae (NTHi). Cefuroxime axetil is hydrolyzed by esterase to the active ingredient Cefuroxime (HY-B1256A) after oral absorption. Topical administration of Cefuroxime via bioadhesive nanoparticles (BNPs) can prolong the drug's retention time in the middle ear (≥7 days). Cefuroxime axetil can be used in the study of otitis media (especially NTHi infection). Cefuroxime axetil can achieve precise antibacterial effects through oral or topical nano-delivery systems, reducing systemic exposure and the risk of antibiotic resistance .

HY-B1178

Cotinine 1 Publications Verification (-)-Cotinine; (S)-Cotinine; NIH-10498	Endogenous Metabolite nAChR	Cardiovascular Disease Inflammation/Immunology
Cotinine ((-)-Cotinine) is an orally active alkaloid found in tobacco and is the primary metabolite of nicotine. Cotinine is metabolized by CYP2A13 into trans-3'-hydroxycotinine. Cotinine is used as a biomarker to measure exposure to tobacco smoke components. Cotinine has vasodepressor activity. The mixture of cotinine and nicotine (Nicotine) has antiproliferative activity against pterygium. (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, leading to the release of dopamine (Dopamine, HY-B0451). Cotinine ((-)-Cotinine) is used in research related to cardiovascular and inflammatory diseases .

HY-169308

EGFR-IN-132	EGFR	Cancer
EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC₅₀ of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure .

HY-15042

MK 0686	Bradykinin Receptor	Metabolic Disease
MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .

HY-169309

EGFR-IN-133	EGFR	Cancer
EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC₅₀ of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure .

HY-168650

ROCK/HDAC-IN-1	ROCK HDAC	Inflammation/Immunology Cancer
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC₅₀: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC₅₀: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC₅₀: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .

HY-159905

HPK1-IN-54	MAP4K	Inflammation/Immunology
HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC₅₀ value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy .

Cat. No.	Product Name	Category	Target	Chemical Structure