75 Results for "

oral exposure

" in MedChemExpress (MCE) Product Catalog:
Products (75)

75 Results for "oral exposure" in MCE Product Catalog:

31
31 Publications Verification
Cat. No.: HY-13687
CAS No.: 873225-46-8
Purity:  99.88%
IKK 16 is an orally active IKK inhibitor. IKK 16 shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway .
loading...
    loading...
31
31 Publications Verification
Cat. No.: HY-13687A
CAS No.: 1186195-62-9
Purity:  99.95%
IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-B1178
CAS No.: 486-56-6
Synonyms: (-)-Cotinine; (S)-Cotinine; NIH-10498
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 .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-16100
CAS No.: 1291779-76-4
Research Areas:  

Metabolic Disease Cancer

BI 99179, a chemical probe, 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 .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-N5112A
CAS No.: 34539-65-6
Synonyms: Arnebin 1
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-B0487
CAS No.: 434-03-7
Synonyms: Pregneninolone; 17α-Ethynyltestosterone
Target:  

Estrogen Receptor/ERR

Research Areas:  

Metabolic Disease

Ethisterone (Pregneninolone; 17α-Ethynyltestosterone) is a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone has almost no effect on the phagocytic activity of the reticuloendothelial system in male guinea pigs, while in utero exposure can induce abnormalities in the urogenital system of offspring .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-116565
CAS No.: 1428862-33-2
Purity:  ≥98.0%
Synonyms: SUVN-D4010
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease

Usmarapride (SUVN-D4010) (Example 3)is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=27.5 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-156685
CAS No.: 2767264-57-1
Purity:  99.86%
Target:  

PI4K Parasite

Research Areas:  

Infection Metabolic Disease Cancer

EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-116565A
CAS No.: 1428862-32-1
Purity:  99.91%
Synonyms: SUVN-D4010 free base
Target:  

5-HT Receptor

Research Areas:  

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 .
loading...
    loading...
Cat. No.: HY-156618
CAS No.: 2230974-62-4
Purity:  99.63%
Synonyms: ABSK011
Target:  

FGFR

Research Areas:  

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 .
loading...
    loading...
Cat. No.: HY-B1325
CAS No.: 64544-07-6
Target:  

Bacterial Antibiotic

Research Areas:  

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 .
loading...
    loading...
Cat. No.: HY-W725179
CAS No.: 2044520-06-9
Target:  

EBV

Research Areas:  

Cancer

VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
loading...
    loading...
Cat. No.: HY-15043
CAS No.: 913064-47-8
Purity:  99.51%
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
loading...
    loading...
Cat. No.: HY-W014075
CAS No.: 5315-79-7
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 .
loading...
    loading...
Cat. No.: HY-B1073
CAS No.: 26155-31-7
Target:  

Parasite

Research Areas:  

Infection

Morantel tartrate is an anthelmintic agent. Sustained-release three-layer composite tablets of Morantel tartrate are administered orally and release after exposure to rumen fluid. Morantel tartrate reduces the fecal egg output and worm burden of gastrointestinal nematodes in Hereford calves. Morantel tartrate is used in research related to gastrointestinal nematode infections .
loading...
    loading...
Cat. No.: HY-21197
CAS No.: 375-85-9
Synonyms: Perfluoroheptanoic acid; Tridecafluoroheptanoic acid; PFHpA
Perfluoroenanthic acid (Perfluoroheptanoic acid) is a kind of perfluoroalkyl carboxylic acid organic pollutant. Perfluoroenanthic acid has environmental persistence and bioaccumulation, and exposure can occur via oral, dermal and other routes. Perfluoroenanthic acid exhibits reproductive toxicity, neurotoxicity, hepatotoxicity, immunotoxicity and endocrine-disrupting effects. Perfluoroenanthic acid exerts definite adverse effects on development, spermatogenesis, neuronal activity and liver tissue .
loading...
    loading...
Cat. No.: HY-Y0496
CAS No.: 106-46-7
Research Areas:  

Cancer

1,4-Dichlorobenzene is a non-genotoxic, orally active mitogenic/tumor-promoting carcinogen that is also widely used as a dye, resin intermediate, and deodorant, moth repellent/insecticide. 1,4-Dichlorobenzene induces liver tumors in mice and promotes the growth of spontaneous precancerous lesions, but shows no liver tumor-inducing activity in F344 rats. Exposure to 1,4-dichlorobenzene leads to elevated leukocyte counts, serum alanine aminotransferase, and blood urea nitrogen levels. Due to the hepatotoxic characteristics, 1,4-Dichlorobenzene is applicable to liver cancer-related research .
loading...
    loading...
Cat. No.: HY-W013989
CAS No.: 2387-23-7
Target:  

Epoxide Hydrolase

Research Areas:  

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 .
loading...
    loading...
Cat. No.: HY-W014075S
CAS No.: 132603-37-3
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 .
loading...
    loading...
Cat. No.: HY-Y1097
CAS No.: 4376-18-5
Synonyms: 2-(Methoxycarbonyl)benzoic acid
Monomethyl phthalate is an orally active metabolite of phthalic acid. Monomethyl phthalate, as a urine biomarker after exposure to phthalate, can be used as a detection indicator for thyroid cancer and benign nodules. Monomethyl phthalate reduces the survival rate of young frogs. Monomethyl phthalate induces oxidative damage to red blood cells in rats .
loading...
    loading...