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Pathways Recommended: Antibody-drug Conjugate/ADC Related
Results for "

drug tolerance

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

2

Peptides

2

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1291
    PKI 14-22 amide,myristoylated
    3 Publications Verification

    		 PKA Epigenetic Reader Domain Flavivirus Infection Neurological Disease
    PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
    PKI 14-22 amide,myristoylated
  • HY-164729
    FZ-AD005

    		Antibody-Drug Conjugates (ADCs) Topoisomerase Apoptosis Cancer
    FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
    FZ-AD005
  • HY-N2486
    Desoxyrhaponticin
    1 Publications Verification

    		 Fatty Acid Synthase (FASN) Apoptosis Cancer
    Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects.
    Desoxyrhaponticin
  • HY-12758
    YHO-13351

    		BCRP Cancer
    YHO-13351 is an orally active ABCG2 inhibitor . YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer .
    YHO-13351
  • HY-123297
    TUG-469

    		Free Fatty Acid Receptor Metabolic Disease
    TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes .
    TUG-469
  • HY-W145493
    Glycofurol

    Tetraglycol; Poly(ethylene glycol) tetrahydrofurfuryl ether

    		 Biochemical Assay Reagents Others
    Glycofurol (Tetraglycol) is a hydrophilic, water-miscible cosolvent and absorption enhancer with skin tolerance. Glycofurol can be used as a carrier-based gel for the topical delivery of drugs, including water-insoluble drugs. Glycofurol can form gels with bioadhesiveness, spreadability and suitable viscosity for topical administration .
    Glycofurol
  • HY-P1291A
    PKI 14-22 amide,myristoylated TFA
    3 Publications Verification

    		 PKA Epigenetic Reader Domain Flavivirus Infection Neurological Disease
    PKI 14-22 amide, myristoylated TFA is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated TFA makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated TFA can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated TFA can prevent the development of analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated TFA can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
    PKI 14-22 amide,myristoylated TFA
  • HY-W015399
    4-Methylcinnamic acid

    		Fungal Infection
    4-Methylcinnamic acid is a cinnamic acid derivative with antifungal activity. 4-Methylcinnamic acid can overcome the tolerance of glutathione reductase mutants to 4-Methoxycinnamic acid (HY-N1387). When 4-Methylcinnamic acid is used in combination with traditional antifungal agents, it can reduce their minimum inhibitory concentrations. 4-Methylcinnamic acid can act as an intervention catalyst to enhance the efficacy of traditional antifungal agents and has application potential in targeting fungal cell wall disruption and controlling drug-resistant fungi .
    4-Methylcinnamic acid
  • HY-N2486R
    Desoxyrhaponticin (Standard)

    		Reference Standards Fatty Acid Synthase (FASN) Apoptosis Cancer
    Desoxyrhaponticin (Standard) is the analytical standard of Desoxyrhaponticin. This product is intended for research and analytical applications. Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects .
    Desoxyrhaponticin (Standard)
  • HY-E70599
    Human CES2 Enzyme

    		Carboxylesterase (CES) Metabolic Disease
    Human CES2 Enzyme is a carboxylesterase involved in drug metabolism and lipid homeostasis. Human CES2 Enzyme hydrolyzes triglycerides, cholesteryl esters and retinyl esters to regulate lipid metabolism and energy homeostasis. Human CES2 Enzyme improves glucose tolerance and insulin sensitivity, reduces hepatic lipid accumulation, alleviates white adipose tissue steatitis, decreases plasma cholesterol levels, and reduces body weight and white adipose tissue weight. Human CES2 Enzyme can be used in the research of metabolic syndrome .
    Human CES2 Enzyme
  • HY-164429
    VIP236

    		Integrin Elastase Cancer
    VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
    VIP236
  • HY-117881
    CJ-15208

    		Opioid Receptor Neurological Disease
    CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
    CJ-15208
  • HY-183489
    TAAR1-agonist-4

    		Trace Amine-associated Receptor (TAAR) Neurological Disease Metabolic Disease
    TAAR1-agonist-4 is a TAAR1 agonist and oral hypoglycemic agent with an EC50 of 0.0046 μM for TAAR1. TAAR1-agonist-4 alleviates antipsychotic-related metabolic side effects, improves negative and cognitive symptoms, and reduces drug abuse behaviors. TAAR1-agonist-4 is applicable to research on schizophrenia, acute manic episodes associated with bipolar disorder, and glucose intolerance .
    TAAR1-agonist-4
  • HY-180373
    WR 30090

    		Parasite Infection
    WR 30090 (Compound 37) is a broad-spectrum antimalarial agent that does not rely on the classical antifolate pathway. WR 30090 exhibits strong activity against a variety of chloroquine-sensitive and resistant Plasmodium falciparum strains, especially the highly resistant Vietnamese strain. WR 30090 shows high activity in mouse malaria tests, with a minimum effective dose of 5 mg/kg and a minimum cure dose of 20 mg/kg. WR 30090 can be used for research on acute malaria .
    WR 30090
  • HY-124470
    Amisometradine

    		Others Cardiovascular Disease
    Amisometradine is an orally active aminouracil diuretic with a diuretic potency approximately 40% that of Mersalyl (HY-108868) (when administered intramuscularly). Amisometradine exerts its effects by promoting the excretion of sodium, chloride and a small amount of potassium, exhibits significant therapeutic effects in heart failure models, and has good tolerance with long-term administration. Compared with drugs of the same class, Amisometradine causes fewer gastrointestinal reactions; its minor side effects mainly include nausea, vomiting, diarrhea, tinnitus and deafness, and are usually not accompanied by proteinuria or abnormalities in blood and urine indicators. Amisometradine is an important tool for the study of heart failure and related diuretic mechanisms .
    Amisometradine

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