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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
67 Results for "
clinical development
" in MedChemExpress (MCE) Product Catalog:
Products (67)
67 Results for "clinical development" in MCE Product Catalog:
Cat. No.: HY-119340
CAS No.: 87626-55-9
Synonyms: Flavoneacetic acid
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Mitoflaxone (flavoneacetic acid) is a synthetic flavonoid compound with vascular targeting properties. Mitoflaxone exerts anti-proliferative effects on endothelial cells through a superoxide-dependent mechanism, this effect leads to changes in the permeability of tumor blood vessels, thereby exerting anti-tumor effects [1] [2] .
Cat. No.: HY-19500
CAS No.: 215122-74-0
SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.
Cat. No.: HY-16622A
CAS No.: 1005407-76-0
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GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
Hedonal is a compound with anesthetic activity. In related research in Russia, it has a certain development history in experimental and clinical applications, and is of great significance to the development of anesthesiology.
Cat. No.: HY-12629
CAS No.: 1539296-45-1
Synonyms: PF-06297470
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.
Cat. No.: HY-120285
CAS No.: 285559-03-7
Synonyms: RWJ-351647 hydrochloride; SPD-556 hydrochloride
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M-0002 hydrochloride (RWJ-351647 hydrochloride) is a biologically active compound that acts as an antagonist of the vasopressin V2 receptor. M-0002 hydrochloride is potentially useful for inhibiting ascites. M-0002 hydrochloride shows excellent properties that are favorable for clinical development .
Cat. No.: HY-117742
CAS No.: 380382-38-7
DA-7867 is an antibacterial compound with activity against a wide range of bacteria, including drug-resistant bacteria. DA-7867 shows promising antibacterial activity against some clinically important pathogens, including drug-resistant bacteria. It is an amide analog of Tedizolid (HY-14855), reflecting the potential use of tetrazoles in the development of new antibacterial agents .
Cat. No.: HY-119467
CAS No.: 1366240-73-4
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MDK0734 is a selective inhibitor that inhibits feline hepsin B endopeptidase and exopeptidase activities. MDK0734 demonstrated efficacy in a cell-based in vitro tumor invasion model, significantly attenuating the invasive ability of MCF-10A neoT cells. MDK0734 provides new potential inhibitors for the development of clinically useful compounds targeting the deleterious effects of feline hepsin B in cancer progression .
Cat. No.: HY-118326
CAS No.: 1190379-37-3
MRT 68601 is a potent TBK1 inhibitor with the activity of inhibiting autophagosome formation in lung cancer cells. MRT 68601 may have potential effects against targets associated with host-dependent factors identified in SARS-CoV-2 infection. The drug targets involved in MRT 68601 are related to existing FDA-approved drugs and compounds in clinical trials, which can provide support for the development of broad-spectrum antiviral therapies .
Cat. No.: HY-167950
CAS No.: 849150-59-0
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PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC50 of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy .
Cat. No.: HY-16769
CAS No.: 1356033-60-7
Synonyms: P7170; AK151761
Panulisib (P7170; AK151761) is an orally active inhibitor of PI3K (IC50 = 2.2 nM) and mTOR (IC50 = 4.4 nM). Panulisib inhibits ALK1 and DNA-PK, two enzymes that respectively participate in angiogenesis and DNA repair, with IC50 values of 47 nM and 1.5 nM respectively. Panulisib inhibits cell proliferation and apoptosis. Panulisib can be used for research on breast cancer and non-small cell lung cancer .
Cat. No.: HY-161461
CAS No.: 1341007-95-1
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E234G HYPE-IN-1 (Compound I2.10) is an inhibitor of AMPylation directed by the Huntingtin-interacting protein E (HYPE), possessing low micromolar bioactivity, low cytotoxicity, and blood-brain barrier permeability. E234G HYPE-IN-1 can inhibit the AMPylation of B-cell immunoglobulin-binding protein (BiP), the primary substrate of HYPE. E234G HYPE-IN-1 is suitable for development as a HYPE-specific therapeutic agent for clinical conditions such as neurodegenerative diseases and diabetes .
Cat. No.: HY-16469
CAS No.: 637774-61-9
SR13668 is a potent indole analog derived from indole-3-carbinol (I3C), known for its natural anticancer properties but limited by poor metabolic characteristics. Developed to enhance I3C's anticancer efficacy, SR13668 effectively inhibits growth factor-stimulated Akt activation. It demonstrates strong oral anticancer activity across different cancer types in preclinical studies, showing promise in clinical development due to its favorable safety profile and potent therapeutic effects .
Cat. No.: HY-150260
CAS No.: 155641-16-0
SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance .
Cat. No.: HY-12193
CAS No.: 556835-30-4
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A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
Cat. No.: HY-121708
CAS No.: 930089-25-1
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
Cat. No.: HY-L026
2,539 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication, such as lower risk and less investment. Clinical drugs have confirmed bioactivities, clear mechanisms and high safety that are suitable for drug repurposing.
MCE owns a unique collection of 2,539 clinical compounds that refer to various research areas including anti-cancer, anti-infection, anti-inflammation, nervous disease. Those compounds are of detailed information on clinical development status, research area, targets, etc.
Cat. No.: HY-L053
1,536 compounds
From target identification to clinical research, traditional drug discovery and development is a time-consuming and costly process, which also bears high risk. Compared with traditional drug discovery, drug repositioning or repurposing, also known as old drugs for new uses can greatly shorten the development cycle and reduce development cost, which has become a new trend of drug development. After undergoing clinical trials, approved drugs have identified bioactivities, good pharmacokinetic characteristics and safety, which can greatly improve the success rate of drug discovery. A number of successes have been achieved, such as metformin for type 2 diabetes and thalidomide for leprosy and multiple myeloma, etc.
MCE provides a unique collection of 1,536 China NMPA (National Medical Products Administration) approved compounds, which have undergone extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties. MCE NMPA-Approved Drug Library is a good tool for drug repurposing which could dramatically accelerate drug development.
Cat. No.: HY-L026P
3,262 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication, such as lower risk and less investment. Clinical drugs have confirmed bioactivities, clear mechanisms and high safety that are suitable for drug repurposing.
MCE owns a unique collection of 3,262 clinical compounds that refer to various research areas including anti-cancer, anti-infection, anti-inflammation, nervous disease. Those compounds are of detailed information on clinical development status, research area, targets, etc. Clinical Compound Library Plus, with powerful screening capability, further complements Clinical Compound Library (HY-L026) by adding some compounds with low solubility or solution stability (Part B) to this library. All those supplementary are supplied in powder form.
Cat. No.: HY-L035
5,127 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved and clinical drugs, especially after phase I drugs, have identified bioactivities, good pharmacokinetic characteristics and safety which are suitable for drug repurposing.
MCE Drug Repurposing Compound Library contains 5,127 approved drugs and passed phase Ⅰclinical drugs, which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties.
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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
