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oral exposure

" in MedChemExpress (MCE) Product Catalog:

68

阻害剤およびアゴニスト

1

生化学アッセイ試薬

7

天然物

4

同位体標識化合物

製品番号 製品名 Target 研究分野 構造式
  • HY-13687
    IKK 16
    Maximum Cited Publications
    29 Publications Verification

    		 IKK LRRK2 P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    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 .
    IKK 16
  • HY-W088065
    Sodium formate

    		Environmental Pollutants DNA/RNA Synthesis Others
    Sodium formate acts as a key promoter for heterogeneous nucleation of ZIF crystals and thin film synthesis. It is also recognized as a GRAS substance by the FDA, and serves as a cosmetic preservative and food additive. Sodium formate has low acute oral toxicity (acute oral LD50=7410 mg/kg and acute intravenous LD50=807 mg/kg in mice), with no heritable or carcinogenic effects, but exhibits embryonic developmental toxicity and teratogenicity at high concentrations. Sodium formate may cause moderate irritation to rabbit eyes, is relatively safe to the skin, and does not induce tumor formation in rats in vivo. Sodium formate is rapidly absorbed and oxidized to carbon dioxide in vivo, and forms DNA adducts in specific metabolic deficiency models or upon high-dose exposure .
    Sodium formate
  • HY-B1178
    Cotinine
    3 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 .
    Cotinine
  • 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 .
    Irpagratinib
  • 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 .
    Cefuroxime axetil
  • HY-W725179
    VK-2019

    		EBV 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 .
    VK-2019
  • HY-15043
    ELN-441958

    		Bradykinin Receptor Inflammation/Immunology Endocrinology
    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 .
    ELN-441958
  • 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 .
    1-Hydroxypyrene
  • HY-B0487
    Ethisterone

    Pregneninolone; 17α-Ethynyltestosterone

    		 Estrogen Receptor/ERR 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 .
    Ethisterone
  • HY-16100
    BI 99179
    3 Publications Verification

    		 Fatty Acid Synthase (FASN) 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 .
    BI 99179
  • HY-B1073
    Morantel tartrate

    		Parasite 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 .
    Morantel tartrate
  • HY-21197
    Perfluoroenanthic acid

    Perfluoroheptanoic acid; Tridecafluoroheptanoic acid; PFHpA

    		 PPAR Neurological Disease Metabolic Disease Inflammation/Immunology
    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 .
    Perfluoroenanthic acid
  • HY-N5112A
    β,β-Dimethylacrylalkannin
    3 Publications Verification

    Arnebin 1

    		 FGFR Necroptosis Apoptosis CDK JNK Inflammation/Immunology
    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 .
    β,β-Dimethylacrylalkannin
  • HY-Y0496
    1,4-Dichlorobenzene

    		Insecticide Environmental Pollutants Mitosis 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 .
    1,4-Dichlorobenzene
  • HY-13687A
    IKK 16 hydrochloride
    Maximum Cited Publications
    29 Publications Verification

    		 IKK LRRK2 P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    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 .
    IKK 16 hydrochloride
  • HY-116565
    Usmarapride
    1 Publications Verification

    SUVN-D4010

    		 5-HT Receptor 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 .
    Usmarapride
  • 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 .
    1,3-Dicyclohexylurea
  • 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 .
    1-Hydroxypyrene-d9
  • HY-Y1097
    Monomethyl phthalate

    2-(Methoxycarbonyl)benzoic acid

    		 Endogenous Metabolite Reactive Oxygen Species (ROS) Cancer
    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 .
    Monomethyl phthalate
  • HY-156685
    EDI048

    		PI4K Parasite 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 .
    EDI048
  • HY-N2620
    Rutaevin

    		Cytochrome P450 Infection
    Rutaevin is an antifungal toxin and CYP3A4 inactivator. Rutaevin requires NADPH-dependent bioactivation to generate cis-but-2-ene-1,4-dial, which then covalently modifies and mechanism-based inactivates human CYP3A4 (IC50=4.48 μM, Ki=15.98 μM), and interacts with substances such as glutathione. Rutaevin disrupts the cellular structure of Sirococcus conigenus, accumulates linearly in resistant larch after pathogen exposure, and induces liver toxicity in mice via oral administration. Rutaevin can be applied to research in fields related to larch shoot blight and other associated areas .
    Rutaevin
  • HY-W013989R
    1,3-Dicyclohexylurea (Standard)

    		Reference Standards 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 .
    1,3-Dicyclohexylurea (Standard)
  • HY-A0235
    Antrafenine

    Stakane

    		 Drug Derivative Influenza Virus Infection Neurological Disease Metabolic Disease Inflammation/Immunology
    Antrafenine (Stakane) is a derivative of 2-(quinolin-4-ylamino) benzoate, and is an orally active anti-inflammatory and analgesic agent. Antrafenine protects mammalian epithelial cells from cell death upon exposure to influenza A virus A/WSN/33 (H1N1). Antrafenine inhibits carrageenan-induced paw swelling in rats, and reduces exudate volume and total leukocyte infiltration in carrageenan- and calcium pyrophosphate dihydrate crystal-induced pleurisy in rats. Antrafenine can be used in studies related to influenza and pseudogout .
    Antrafenine
  • 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 .
    Sutidiazine
  • 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 .
    SEP-227900
  • 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 .
    cGAS-IN-3
  • 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.
    STING18
  • HY-120253
    Spirotetramat

    BY-108330

    		 Environmental Pollutants Insecticide SOD Glutathione Peroxidase Carboxylesterase (CES) Infection Metabolic Disease
    Spirotetramat (BY-108330) is an orally active Insecticide and lipid biosynthesis inhibitor. Spirotetramat regulates the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), with short-term exposure increasing their activities and long-term exposure altering their activities. Spirotetramat induces the activity and mRNA expression of carboxylesterase (CarE). Spirotetramat induces oxidative stress and lipid peroxidation in tadpoles. Spirotetramat is toxic to amphibian tadpoles and exhibits sublethal/non-lethal toxicity to amphibians. Spirotetramat causes death in immature psyllids, aphids, scale insects, mealybugs, whiteflies and thrips, and shows a high lethal rate against Cacopsylla pyri nymphs. Spirotetramat reduces the fecundity of Aphis gossypii. Spirotetramat induces tolerance in the offspring of exposed Aphis gossypii, and acts on Myzus persicae, Bemisia tabaci and Tetranychus urticae .
    Spirotetramat
  • HY-B2058
    Triticonazole

    		Fungal Androgen Receptor Infection
    Triticonazole is an orally active triazole fungicide and androgen receptor antagonist. Triticonazole inhibits testosterone-induced androgen receptor activation and reduces basal testosterone secretion. Prenatal exposure to Triticonazole causes shortened anogenital distance in male rat fetuses and induces organ-specific histopathological changes in pigs. Triticonazole can be used for detoxification of seeds contaminated with fungal pathogens, but there is a risk of animal poisoning if the treated seeds are used as animal feed .
    Triticonazole
  • HY-120496
    Clofutriben

    ASP3662

    		 11β-HSD Neurological Disease Metabolic Disease
    Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain .
    Clofutriben
  • HY-142644
    ATX inhibitor 7

    		Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.
    ATX inhibitor 7
  • HY-116565A
    Usmarapride free base
    1 Publications Verification

    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 .
    Usmarapride free base
  • HY-Y0496S
    1,4-Dichlorobenzene-d4

    		Isotope-Labeled Compounds Insecticide Others
    1,4-Dichlorobenzene-d4 is the deuterium labeled 1,4-Dichlorobenzene. 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. 1,4-Dichlorobenzene increases the levels of white blood cell count, serum alanine aminotransferase and blood urea nitrogen in occupationally exposed populations. 1,4-Dichlorobenzene is metabolized to 2,5-dichlorophenol and excreted in urine, and this metabolite can serve as a biomarker for 1,4-Dichlorobenzene exposure. Due to its specific hepatotoxic characteristics, 1,4-Dichlorobenzene is applicable to liver cancer-related research .
    1,4-Dichlorobenzene-d4
  • HY-13687R
    IKK 16 (Standard)

    		IKK LRRK2 Reference Standards P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related Inflammation/Immunology
    IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. 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.
    IKK 16 (Standard)
  • 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 .
    Aβ42-IN-1 free base
  • 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.
    Aβ42-IN-1
  • 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 .
    BAY-405
  • HY-W014075R
    1-Hydroxypyrene (Standard)

    		Reference Standards 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.
    1-Hydroxypyrene (Standard)
  • 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 Cmax and oral exposure. LX-039 has anti-tumor activity .
    LX-039
  • 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 .
    ROCK-IN-9
  • 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 .
    ERK5-IN-3
  • 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 .
    Antidepressant agent 9
  • 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 .
    FGFR-IN-7
  • 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 .
    Human enteropeptidase-IN-1
  • 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 .
    SCH 39304
  • HY-Y1097R
    Monomethyl phthalate (Standard)

    2-(Methoxycarbonyl)benzoic acid (Standard)

    		 Reference Standards Endogenous Metabolite Cancer
    Monomethyl phthalate (Standard) is the analytical standard of Monomethyl phthalate. This product is intended for research and analytical applications. 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.
    Monomethyl phthalate (Standard)
  • 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 .
    MerTK/Axl-IN-1
  • HY-B0487R
    Ethisterone (Standard)

    Pregneninolone (Standard); 17α-Ethynyltestosterone (Standard)

    		 Reference Standards Estrogen Receptor/ERR Metabolic Disease
    Ethisterone (Pregneninolone; 17α-Ethynyltestosterone) (Standard) is the analytical standard of Ethisterone (HY-B0487). This product is intended for research and analytical applications. Ethisterone 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 .
    Ethisterone (Standard)
  • HY-155992
    WLB-89462

    		Sigma Receptor Neurological Disease
    WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 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) .
    WLB-89462
  • 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 .
    BChE-IN-8

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