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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
91 Results for "
Plasma Stability
" in MedChemExpress (MCE) Product Catalog:
Products (91)
91 Results for "Plasma Stability" in MCE Product Catalog:
Cat. No.: HY-189203
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MPMS-VA is a highly hydrophilic peptide cleavable linker that can be used for the construction of ADCs. MPMS-VA can be cleaved at the Val-Ala site by lysosomal cathepsin B in tumor cells. MPMS-VA can enhance the hydrophilicity of the antibody-drug conjugate linker-payload system. MPMS-VA improves the plasma stability of relevant ADCs and reduces the systemic release of free payload. MPMS-VA can be applied in research related to solid tumors with co-expression of EGFR/HER2, such as lung cancer, breast cancer, gastric cancer, and urothelial carcinoma .
Cat. No.: HY-159564
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iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
Cat. No.: HY-W099504S2
CAS No.: 38007-42-0
Synonyms: n-Heptyl alcohol-d1
Cat. No.: HY-181086
CAS No.: 2864394-30-7
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FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3 D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies .
Cat. No.: HY-187221
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Anti-SARS-CoV-2 agent prodrug-1 is a double prodrug modified with 5'-ProTide and N 4-propionyl ester, exhibiting anti-SARS-CoV-2 activity (EC50 = 3.22 μM). Anti-SARS-CoV-2 agent prodrug-1 is rapidly converted by esterases into intermediate 4, which has stronger plasma metabolic stability and can be rapidly activated to exert antiviral effects. Anti-SARS-CoV-2 agent prodrug-1 shows anti-SARS-CoV-2 activity in vitro and exhibits low cytotoxicity. Anti-SARS-CoV-2 agent prodrug-1 can be used in studies related to SARS-CoV-2 infection .
Cat. No.: HY-W663179
CAS No.: 681492-17-1
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DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .
Cat. No.: HY-179581
CAS No.: 2962069-39-0
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SLC6A19-IN-4 is an allosteric-competitive and orally active B 0AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B 0AT1 with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B 0AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research .
Cat. No.: HY-181107
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DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC50 values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC50 of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia .
Cat. No.: HY-18778C
CAS No.: 866399-89-5
Synonyms: TA-8995 hemicalcium; DEZ-001 hemicalcium; AMG-899 hemicalcium
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Obicetrapib hemicalcium (TA-8995 hemicalcium) is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib hemicalcium shifts the plasma lipoprotein profile toward more HDL-C particles, reduces circulating PCSK9 levels, increases hepatic LDLR expression and LDLR mRNA levels, and promotes hepatic clearance of VLDL remnants. Obicetrapib hemicalcium increases the number of large HDL particles, reduces the number and area of atherosclerotic lesions and alleviates lesion severity, increases the proportion of unaffected arterial segments, improves lesion stability, and promotes regression of aortic root lesions. Obicetrapib hemicalcium also exerts a synergistic effect with Ezetimibe (HY-17376) to reduce non-HDL-C levels and improve atherosclerosis. Obicetrapib hemicalcium can be used in studies related to atherosclerosis and dyslipidemia .
Cat. No.: HY-183335
Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma .
Cat. No.: HY-184337
CAS No.: 143111-84-6
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Dihydroparadol is a iNOS inhibitor with an IC50 of 7.24 μM, and it is found in ginger. Dihydroparadol partially inhibits the catalytic activity of iNOS, blocks the nuclear translocation of NF-κB p65, reduces NF-κB activity, and attenuates lipopolysaccharide-induced degradation of IκB-α, thereby inhibiting NF-κB-mediated iNOS gene expression and protein production. Dihydroparadol inhibits lipopolysaccharide-induced nitric oxide production in macrophages and exhibits anti-inflammatory activity. Dihydroparadol increases ABCA1 protein abundance by elevating mRNA levels and reducing proteasomal degradation, and also increases ABCG1 protein abundance by enhancing protein stability. Dihydroparadol promotes cholesterol efflux from cholesterol-loaded macrophages via apolipoprotein A1-mediated and plasma-mediated pathways. Dihydroparadol inhibits PDGF-induced vascular smooth muscle cell proliferation, shows no cytotoxicity to vascular smooth muscle cells within the tested concentration range, and does not interfere with endothelial cell proliferation. Dihydroparadol can be used in the research of inflammatory diseases, atherosclerosis and cardiovascular diseases .
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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
