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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
28 Results for "
systemic exposure
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "systemic exposure" in MCE Product Catalog:
2
2 Cited Publications
Cat. No.: HY-B1444
CAS No.: 24168-96-5
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Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, exhibiting a rapid rate of absorption and low systemic exposure potential .
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1 Cited Publications
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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 .
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Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment .
Cat. No.: HY-B1325
CAS No.: 64544-07-6
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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 .
Synonyms: INS-1009
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Treprostinil palmitil is a long-acting inhaled pulmonary vasodilator prodrug of Treprostinil (HY-100441), formulated in a lipid nanoparticle (LNP). Treprostinil palmitil can inhibit pulmonary vascular remodeling induced by Su/Hx challenge in rats. Treprostinil palmitil can induce cough. Treprostinil palmitil demonstrates a sustained presence in the lungs with reduced systemic exposure and prolonged inhibition of hypoxia-induced pulmonary vasoconstriction in vivo. Treprostinil palmitil can be studied in research for pulmonary arterial hypertension and interstitial lung disease .
Cat. No.: HY-W725179
CAS No.: 2044520-06-9
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 .
Cat. No.: HY-157763
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Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding BTK bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces BTK degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo BTK degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)) .
Cat. No.: HY-15234S
Cat. No.: HY-15234R
CAS No.: 397864-44-7
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Fluticasone furoate (Standard) is the analytical standard of Fluticasone furoate. This product is intended for research and analytical applications. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment .
Cat. No.: HY-174383
CAS No.: 2857007-03-3
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PDE3/4-IN-2 is a dual PDE3A and PDE4B1 inhibitor, with an IC50 of 0.13 nM against PDE3A and 50 nM against PDE4B1. PDE3/4-IN-2 exhibits higher systemic exposure and longer retention time in lung tissues in ICR mice. PDE3/4-IN-2 can be used in research on respiratory diseases such as asthma and chronic obstructive pulmonary disease, as well as autoimmune inflammation-related studies .
Cat. No.: HY-B1444R
CAS No.: 24168-96-5
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Isoconazole (nitrate) (Standard) is the analytical standard of Isoconazole (nitrate). This product is intended for research and analytical applications. Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, exhibiting a rapid rate of absorption and low systemic exposure potential .
Cat. No.: HY-W762012
CAS No.: 3268-87-9
Synonyms: OCDD
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Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant but is not acutely toxic. In rats, Octachlorodibenzo-p-dioxin (50 μg/kg i.v. or 50-5000 μg/kg p.o.) has a systemic elimination half-life of 3-5 months and accumulates and concentrates in the liver and adipose tissue after low-dose, repeated exposure. Repeated administration of octachlorodibenzo-p-dioxin causes increases in 7-ethoxyresorufin-O-deethylase (7-EROD) activity and total cytochrome P-450 levels .
Cat. No.: HY-170448
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PROTAC AR Degrader-9 is a topically applicable androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-9 recruits Cereblon (CRBN) E3 ubiquitin ligase to induce AR ubiquitination and proteasomal degradation in human dermal papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 possesses excellent skin retention, modulates androgenetic alopecia (AGA)-related downstream paracrine factors including TGF-β1 and β-catenin, promotes hair regeneration in mice. and exhibits favorable skin pharmacokinetics profiles with minimal systemic exposure. PROTAC AR Degrader-9 can be used for the study of androgenetic alopecia (AGA) .
Cat. No.: HY-147927
CAS No.: 1802891-20-8
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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 .
Cat. No.: HY-163672
CAS No.: 2688785-13-7
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Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC50=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases .
Cat. No.: HY-105110
CAS No.: 120924-80-3
Synonyms: SM-8668
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 .
Cat. No.: HY-112142A
CAS No.: 422547-55-5
Synonyms: DVR-23
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(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 .
Cat. No.: HY-147927A
CAS No.: 1802891-23-1
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(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 .
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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 .
Cat. No.: HY-185398
Synonyms: Amikacin disulfate liposome; Liposomal amikacin
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Amikacin liposome is a liposome-encapsulated form of Amikacin disulfate (HY-B0509B), an aminoglycoside antibiotic with antibactericidal avtivity. Amikacin liposome prolongs the release of amikacin in the lungs and reduces systemic exposure, thereby lowering systemic toxicity.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
