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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-proteinbinding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
OSBPL7-IN-1 is an orally active oxysterol bindingprotein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression .
σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasmaproteinbinding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
Felotaxel (SHR110008) is a compound with antitumor activity that has specific pharmacokinetic properties in rats and is rapidly distributed to normal tissues. The kidney is the major excretion organ, and its plasmaproteinbinding capacity is nearly linearly related to concentration.
AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that exerts its inhibitory effect by tightly and reversibly binding to DPPIV. AMG 222 binds to human plasmaproteins in a saturable and concentration-dependent manner, with a binding rate of 80.8% at 1 nM, while the binding rate decreases to 29.4% at concentrations above 100 nM. AMG-222 can be used in research related to diabetes .
Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasmaproteinbinding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor .
Antimycobacterial agent-8 (Compound 49) is an inhibitor for DNA gyrase. Antimycobacterial agent-8 exhibits antibacterial activity against Mycobacterium tuberculosis and M. abscessus with MIC90 of 2.5 μM and 0.63 μM. Antimycobacterial agent-8 exhibits good plasmaproteinbinding ability in mice .
Halofenate, structurally akin to clofibrate, was evaluated in hypertriglyceridemic patients over 6-week periods in a controlled, double-blind crossover trial. It effectively reduced serum triglycerides by 50%, with minimal impact on serum cholesterol levels. Additionally, it lowered serum uric acid by 30% and exhibited uricosuric effects independent of glomerular filtration rate. Halofenate was associated with a significant increase in plasma thyroxine (T4), accompanied by a decrease in protein-bound iodine and T4 by column. In vitro studies confirmed its ability to displace T4 from thyroid-bindingproteins, suggesting a thyroxine-displacing effect, which could influence thyroid function in vivo .
Perforin-IN-2 is a benzosulfonamide perforin inhibitor that alleviates transplant rejection during allogeneic bone marrow/stem cell transplantation. Perforin-IN-2 binds to plasmaproteins with a binding rate of 99.8%. Perforin-IN-2 requires a higher concentration (> 900 μM) to achieve optimal perforin inhibition in vivo. Perforin-in-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and also inhibit the death of K562 leukemia target cells .
5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasmaproteinbinding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .
ML350 (CYM50202) is a highly potent OPRK1 antagonist with selectivity and broad biological applications. With IC50 values of 9-16 nM, ML350 shows high selectivity for OPRK1, with selectivity of 219-382-fold and 20-35-fold relative to OPRD1 and OPRM1, respectively. ML350 exhibited favorable characteristics in in vivo pharmacokinetic analysis, including high passive membrane permeability and moderate human plasmaproteinbinding. Extensive screening of ML350 against multiple ion channels, receptors, and transporters showed that it does not have adverse off-target effects .
(Rac)-Telinavir ((Rac)-SC-52151) is a potent, selective, tight-binding human immunodeficiency virus (HIV) protease inhibitor that exhibits significant anti-HIV activity. (Rac)-Telinavir has a mean 50% effective concentration of 26 ng/ml (43 nM) against various strains of HIV, including HIV-1, HIV-2, and simian immunodeficiency virus. (Rac)-Telinavir, in combination with nucleoside reverse transcriptase inhibitors, demonstrates synergistic effects on inhibiting HIV-1 replication without additive toxicity. (Rac)-Telinavir is highly protein bound in human plasma and exhibits low partitioning into erythrocytes.
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules.
There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery.
MCE provides a unique collection of 4,892 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.
Extracellular vesicles (EVs) are small membrane binding structures that are released from cells into the surrounding environment and play a crucial role in mediating and regulating intercellular communication related to physiological and pathological processes. EVs are lipid membrane vesicles composed of proteins, lipids, and nucleic acids. EVs can be divided into several types based on their source, such as extracellular vesicles, microcapsules, and apoptotic vesicles. The size range of exosomes is 30-150nm, which are endocrine in multi vesicular endosomes (MVEs); microvesicles (50-1000nm) are secreted directly through extracellular interactions, thereby releasing plasma membrane vesicles. In contrast, apoptotic bodies are usually larger, ranging in size from 1 to 5 μ m. This is generated during programmed cell death. EV plays a crucial role in transmitting information between cells and influencing the behavior and function of receptor cells.
MCE designs a unique collection of 415 small molecules related to extracellular vesicles (EVs). It is a good tool to be used for research on metabolize, cancer and other diseases.
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
SPSB2-iNOS inhibitory cyclic peptide-1 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-1(HY-P10383). SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human is the recombinant human-derived RBP4 protein, expressed by E. coli , with tag free. The total length of RBP4 Protein, Human is 183 a.a., with molecular weight of ~20.0 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human (HEK293, hFc) is the recombinant human-derived RBP4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of RBP4 Protein, Human (HEK293, hFc) is 183 a.a., with molecular weight of ~50 kDa.
RBP4 Protein transports retinol in blood plasma, delivering it from the liver to peripheral tissues. It binds to all-trans retinol, transferring it to STRA6 for cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further aids STRA6 in retinol transport. RBP4 Protein, Rat (HEK293, His) is the recombinant rat-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Rat (HEK293, His) is 183 a.a., with molecular weight of ~24 kDa.
RBP4 Protein transports retinol in blood plasma, delivering it from liver stores to peripheral tissues. Binding to all-trans retinol, it transfers it to STRA6 for efficient cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further supports STRA6 in retinol transport. RBP4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Mouse (HEK293, His) is 183 a.a., with molecular weight of ~22.8 kDa.
RBP4 Protein is a member of the lipocalin family and the major transport protein of the hydrophobic molecule retinol, also known as vitamin A, in the circulation. RBP4 Protein, Canine (HEK293, Fc) is the recombinant canine-derived RBP4 protein, expressed by HEK293 , with C-hFc labeled tag.
RBP4 Protein is a member of the lipocalin family and the major transport protein of the hydrophobic molecule retinol, also known as vitamin A, in the circulation. RBP4 Protein, Canine (HEK293, His) is the recombinant canine-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Canine (HEK293, His) is 183 a.a., with molecular weight of ~23 kDa.
RBP4 Protein, a vital retinol transporter in blood plasma, mediates the transfer from liver stores to peripheral tissues. It also enhances retinol transport by interacting with TTR. RBP4 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Cynomolgus (HEK293, His) is 183 a.a., with molecular weight of ~23 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human (HEK293, C-His) is the recombinant human-derived RBP4 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of RBP4 Protein, Human (HEK293, C-His) is 183 a.a., with molecular weight of ~21 kDa.
HABP2 is a protein that cleaves the alpha chain of fibrinogen as well as the beta chain between "Lys-53" and "Lys-54" at multiple sites, preventing direct formation of a fibrin clot. It activates coagulation factor VII and converts prourokinase into its active form. HABP2 Protein, Human (HEK293, His) is the recombinant human-derived HABP2 protein, expressed by HEK293 , with C-6*His labeled tag.
PSP94/MSMB protein forms homodimers and interacts with PI16. PSP94/MSMB Protein, Human (His) is the recombinant human-derived PSP94/MSMB protein, expressed by E. coli , with C-His labeled tag.
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