125 Results for "

poor

" in MedChemExpress (MCE) Product Catalog:
Products (125)

125 Results for "poor" in MCE Product Catalog:

Cat. No.: HY-P991998

Target:  

Fc Receptor (FcR)

Research Areas:  

Inflammation/Immunology Cancer

Anti-Human/Monkey CD16a Antibody (3G8) is a monoclonal antibody targeting CD16a. Anti-Human/Monkey CD16a Antibody (3G8) blocks FcγRIII/CD16a, upregulates the metabolic activity of CD16+ cells, downregulates CD87, a poor prognostic marker, and inhibits the engraftment and growth of leukemia cells in acute myeloid leukemia, and rapidly increases platelet counts in immune thrombocytopenia. Anti-Human/Monkey CD16a Antibody (3G8) is applicable to research related to tumor immunology .
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Cat. No.: HY-W016647R
CAS No.: 4289-98-9
Synonyms: N-Formylmethionine (Standard)
For-Met-OH (Standard) (N-Formylmethionine (Standard)) is the analytical standard of For-Met-OH (HY-W016647). This product is intended for research and analytical applications. For-Met-OH (N-Formylmethionine) can be involved in the translation process of bacteria, chloroplasts, and mitochondria. For-Met-OH plays different roles in different species and organelles, such as promoting the formation of protein complexes in mitochondria and acting as a degradation signal in bacteria and yeast. The level of For-Met-OH is closely related to certain diseases; for example, For-Met-OH is a potential biomarker for metabolic disorders and poor prognosis in critically ill patients.
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Cat. No.: HY-185150
CAS No.: 114088-58-3
Synonyms: 9-(2-Phosphonylmethoxy)ethylguanine
PMEG is a nuclear DNA polymerases α, δ, and ε inhibitor that causes DNA chain termination, inhibits DNA synthesis, induces cytotoxicity in dividing cells. PMEG is an acyclic nucleotide phosphonate that forms an active phosphorylated metabolite, PMEG diphosphate, within cells. PMEG has activity against leukemia and melanoma in rodent models. PMEG has poor cell permeability; its prodrug is Rabacfosadine (GS-9219) (HY-13640). PMEG shows antiviral activity against against various DNA virus infections including murine cytomegalovirus (MCMV) and human cytomegalovirus (HCMV). PMEG can be used for the research of non-hodgkin's lymphoma [1][2].
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Cat. No.: HY-185760
Target:  

Liposome

Research Areas:  

Others

F-L319 is an ionizable lipid and spleen-targeting mRNA delivery vector. F-L319 can be formulated into lipid nanoparticles (LNPs) to drive spleen-restricted reporter protein expression in mice. F-L319 modulates mRNA encapsulation efficiency, cellular uptake efficiency, and delivery efficiency, with effects varying depending on the composition of LNP formulations. When prepared as pure LNPs, F-L319 shows poor mRNA delivery efficiency in cells; in contrast, hybrid LNPs containing F-L319 and L319 significantly enhance mRNA delivery efficiency in cells .
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Cat. No.: HY-176019
Target:  

p38 MAPK c-Myc

Research Areas:  

Cardiovascular Disease Cancer

Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy .
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Cat. No.: HY-W854385
CAS No.: 92448-22-1
Synonyms: SLeA
Research Areas:  

Cancer

Sialyl Lewis A (SLeA) is a tumor-associated carbohydrate antigen, also known as carbohydrate antigen 19-9 (CA19-9), that binds to E-selectin (ELAM-1) and selectins to mediate cell-endothelium adhesion. Sialyl Lewis A promotes cancer cell-vascular endothelium adhesion, and its surface presence correlates with increased tumorigenicity and invasiveness in cancer cells. Sialyl Lewis A shows elevated expression in human adenocarcinomas of the colon, pancreas, and stomach, with expression levels linked to tumor progression and poor prognosis in colorectal and gastric carcinomas. Sialyl Lewis A can be used for the research of cancers, such as colon, pancreas, stomach, and squamous lung cancer .
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Cat. No.: HY-116578S
CAS No.: 1215315-86-8
Synonyms: EXP999-d6; RP9965-d6
Metopimazine-d6 (EXP999-d6; RP9965-d6) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
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Cat. No.: HY-N7833
CAS No.: 24257-10-1
Heneicosapentaenoic Acid (HPA) is a 21:5 omega-3 fatty acid found in trace amounts in the green alga B. pennata and in fish oils. Its chemical composition is similar to eicosapentaenoic acid (EPA), except that a carbon is extended at the carboxy terminus, placing the first double bond at the δ6 position. HPA can be used to study the importance of double bond position in omega-3 fatty acids. It incorporates phospholipids and triacylglycerols in vivo with the same efficiency as EPA and docosahexaenoic acid, and exhibits a strong inhibitory effect on the synthesis of arachidonic acid from linoleic acid. HPA is a poor substrate for prostaglandin H synthase (PGHS) (cyclooxygenase) and 5-lipoxygenase, but retains the ability to rapidly inactivate PGHS.
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Cat. No.: HY-N17304
CAS No.: 314744-17-7
10S,13aR-Antofine N-oxide is a phenanthroindolizidine N-oxide alkaloid and cytotoxic agent found in Cynanchum vincetoxicum. 10S,13aR-Antofine N-oxide exerts cytotoxic effects in drug-sensitive (KB-3-1, IC50 = 0.11 μM) and multi-drug-resistant (KB-V1, IC50 = 0.16 μM) carcinoma cells. 10S, 13aR-Antofine N-oxide acts as a poor substrate for the P-glycoprotein (P-170) efflux pump. 10S,13aR-Antofine N-oxide can be used for the research of cancers .
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Cat. No.: HY-L061
5,513 compounds

Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.

MCE offers a unique collection of 5,513 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.

Cat. No.: HY-103249
CAS No.: 303957-69-9
Purity:  98.08%
Synonyms: Reutericycline
Reutericyclin (Reutericycline) is an orally active antibacterial and anti-obesity agent that selectively inhibits Gram-positive bacteria. By selectively dissipating transmembrane potential, Reutericyclin exerts non-lytic bactericidal or bacteriostatic activity against pathogens such as Clostridium difficile and Staphylococcus aureus, and rapidly kills vegetative cells and spores of Clostridium difficile. Reutericyclin possesses favorable properties including resistance to enzymatic hydrolysis, iron-chelating function, and poor absorption by colonic epithelium. Reutericyclin not only eradicates staphylococcal biofilms and inhibits drug-resistant strains, but also counteracts Risperidone (HY-11018)-induced weight gain by inducing changes in gut microbiota composition and restoring energy utilization efficiency. Reutericyclin can be used in research related to Clostridium difficile infection, Risperidone-induced weight gain, and staphylococcal superficial skin infections .
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Cat. No.: HY-187618
CAS No.: 1508276-29-6
Target:  

TRP Channel

Research Areas:  

Metabolic Disease

GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx .GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity .GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses .GRC-17536 exhibits antitussive activity .GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study .GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough .
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Cat. No.: HY-N15721
CAS No.: 1630745-39-9
Synonyms: Trp-CA
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .
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Cat. No.: HY-L033
370 compounds

Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide: e.g. stability against proteolysis (duration of activity) and poor bioavailability. Certain other properties, such as receptor selectivity or potency, often can be substantially improved. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. Hence mimics have great potential in drug discovery.

MCE Peptidomimetic Library contains 370 compounds including peptoid, α-helix mimetics, β-turn/sheets mimetics, etc. This library is an indispensable tool of structure-activity relationships in drug discovery.

Cat. No.: HY-W010713
CAS No.: 2669-65-0
Synonyms: Fimaporfin free base
Target:  

Photosensitizer

Research Areas:  

Cancer

Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
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Cat. No.: HY-L945
74 compounds

Sulfonyl fluoride (-SO₂F) overcomes the poor target selectivity of traditional covalent warheads that rely heavily on cysteine. With high stability and tunable electrophilicity under physiological conditions, it targets multiple nucleophilic residues including Lys, Tyr, Ser and His, offering expanded druggable space, lower off-target risks and prolonged efficacy. It is widely used in covalent inhibitors, molecular glues, PROTACs and chemical probes.

MCE has built a highly diverse sulfonyl fluoride fragment library with 1,162 structurally diverse, drug-like fragments. Designed for balanced reactivity, stability and compatibility, these molecules feature tunable electrophilicity, simple scaffolds and high derivatization potential. Combined with SuFEx click chemistry, the library enables efficient modular modification and rapid structure optimization.

Ideal for targeting non-cysteine residues, this library improves covalent screening and probe development efficiency, serving as a precise tool for early-stage covalent drug discovery and chemical biology research.

Cat. No.: HY-N0394R
CAS No.: 56-89-3
L-Cystine (Standard) is the analytical standard of L-Cystine. This product is intended for research and analytical applications. L-Cystine, the extracellular form of L-Cysteine (HY-Y0337), is a nutritionally dispensable semiessential sulfur-containing amino acid, occurring in proteins of plants and animals. L-Cystine induces Nrf2 protein elevation in a Keap1 (HY-P75897)-dependent manner and activates Nrf2 transcription factor. L-cystine can elicit cytoprotection by reducing ROS generation and protecting against oxidant- or doxorubicin-induced apoptosis. The reduced reabsorption of L-Cystine in renal tubules and its poor solubility in urine are the important causes of cystine precipitation and cystine crystal formation eventually leading to kidney stones. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and cystinosis
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Cat. No.: HY-L188
2,134 compounds

Although brain cancer only accounts for 2% of all tumors, it has a poor prognosis, high mortality and high recurrence rate. Brain cancer can be divided into primary brain cancer and secondary brain cancer. According to the location of the cancer, brain cancer can also be divided into: brain glioma, pituitary adenoma, schwannoma, craniopharyngioma, meningioma and so on. Glioma is the most common primary brain tumor, accounting for about 1/3 of all brain tumors. At present, brain cancer lacks precision targeted therapeutic drugs, and there is still a great clinical demand that has not been met. With the continuous development of high-throughput screening technology, it may be able to help develop effective anti-brain cancer drugs by screening compounds targeting PKC, PD-1, c-Met, PARP, etc targets.

MCE designs a unique collection of 2,134 small molecules with definite or potential anti-brain cancer activity, which is an important tool for studying the pathological mechanism of brain cancer and developing drugs for brain cancer.

Cat. No.: HY-L173
2,967 compounds

Ovarian cancer is the most common cause of death in female genital malignancies, with the highest mortality rate in female genital malignancies. It is characterized by difficulty in detection in the early stage of the disease, high recurrence rate and poor prognosis. In fact, ovarian cancer includes many pathologic types. It is usually divided into epithelial ovarian cancer, malignant germ cell tumors and sex cord stromal tumors, of which epithelial ovarian cancer is the most dominant form. Clinical treatment of ovarian cancer prioritizes surgery combined with paclitaxel chemotherapy. However, due to the spread and drug resistance of tumor cells, the recurrence of ovarian cancer is high. In this case, combined with traditional methods, the development of new therapeutic agents can help to improve the treatment effect of ovarian cancer.

MCE designs a unique collection of 2,967 compounds with definite or potential anti-ovarian cancer activity, which mainly targeting the main targets of ovarian cancer such as PARP, ATM/ATR, VEGFR and HIF/HIF Prolyl-Hydroxylase, etc. It is an essential tool for development and research of anti-ovarian compounds.

Cat. No.: HY-L941
4,236 compounds

Orthosteric sites are highly conserved, leading to poor subtype selectivity, off-target toxicity and drug resistance in traditional drugs. By contrast, allosteric sites show low conservation, high hydrophobicity, weak polarity, confined geometry and dynamic cryptic properties, granting modulators high selectivity, functional tunability and safety. Thus, allosteric therapy has become a major focus in drug discovery.

MCE curated nearly 1,000 clinical-stage allosteric modulators, analyzed PDB complex structures to identify key pharmacophores and privileged scaffolds, then designed and filtered compounds using rational “scaffold derivation + physicochemical screening” with strict property criteria. The resulting compounds show high rigidity and shape complementarity to shallow, dynamic, hydrophobic allosteric pockets.

This library comprises 4,315 diverse, lead-like compounds ideal for allosteric drug discovery and target screening, covering kinases, GPCRs and more. All are analogs of clinical-stage molecules with similarity > 0.6, combining high druggability and allosteric binding potential to support efficient early-stage R&D.