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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
777 Results for "
Dose-dependent
" in MedChemExpress (MCE) Product Catalog:
Products (777)
777 Results for "Dose-dependent" in MCE Product Catalog:
Cat. No.: HY-116062A
CAS No.: 129540-12-1
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JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
Cat. No.: HY-138232
CAS No.: 141365-20-0
Synonyms: LTNAM
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Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
Cat. No.: HY-144668
CAS No.: 3035088-22-0
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RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
Cat. No.: HY-155297
CAS No.: 55248-23-2
Synonyms: FLA-136
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Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
Cat. No.: HY-16342
CAS No.: 827034-92-4
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NA808 is an Serine Palmitoyltransferase (SPT) inhibitor. NA808 reduces sphingomyelin synthesis, inhibits its activation in hepatic stellate cells, and decreases the expression of α-SMA protein and mRNA, as well as collagen 1A1 mRNA (IC50 0.16, 0.12, and 0.11 μM, respectively). NA808 inhibits HCV replication and reduces NS3 and RdRp protein expression in HCV replicon cells without significant cytotoxicity and exhibits almost no immunosuppressive effect at effective concentrations. NA808 demonstrates broad-spectrum antiviral activity in humanized chimeric liver mice infected with various HCV genotypes, and dose-dependently reduces serum and hepatic HCV RNA levels. NA808 can be used for research on non-alcoholic steatohepatitis and hepatitis C virus infection .
Cat. No.: HY-175204
SHP2 protein degrader-3 is a SHP2 AUTAC degrader. SHP2 protein degrader-3 shows dose-dependent SHP2 degradation ability (DC50 = 3.22 μM) and anti-tumor activity (IC50 = 5.59 μM) in HeLa cells. SHP2 protein degrader-3 induces degradation through the LC3-mediated autophagy pathway, which can be inhibited by lysosome inhibitors. SHP2 protein degrader-3 induces apoptosis in various cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells) (SHP2 Ligand : (HY-100388); LC3 Ligand: (HY-10542); Linker : (HY-128834)) .
Cat. No.: HY-175207
CAS No.: 3109469-27-1
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CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
Cat. No.: HY-181722
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σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain .
Cat. No.: HY-181889
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS G12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS G12C alkylation in KRAS G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .
Cat. No.: HY-182503
CAS No.: 144928-48-3
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GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock .
Cat. No.: HY-19471
CAS No.: 1010440-84-2
(rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET .
Cat. No.: HY-B0661CS
CAS No.: 1189923-88-3
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Antazoline (Phenazoline) is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV .
Cat. No.: HY-B1777S
CAS No.: 93827-50-0
Synonyms: NSC 268508-15N2; Neuridine-15N2
Synonyms: Lysine vasopressin (Standard); [Lys8]-Vasopressin (Standard)
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Cat. No.: HY-P11291A
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Cat. No.: HY-P11909
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Cat. No.: HY-W017141R
CAS No.: 24683-00-9
Cat. No.: HY-W017141S1
CAS No.: 3028868-76-7
Cat. No.: HY-W746556
CAS No.: 52886-39-2
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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
