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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
20 Results for "
ADME properties
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "ADME properties" in MCE Product Catalog:
Synonyms: Aur0101; Auristatin-0101
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PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
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GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma .
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Polyoxypropylene stearyl ether can be used as an excipient, such as surfactant, softener, lubricating, wetting, plasticizing, solubilizing and dispersing properties. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Cat. No.: HY-175741
CAS No.: 3094992-69-2
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IID432 is a potent, orally active, and covalent inhibitor of Trypanosoma cruzi topoisomerase II. IID432 shows an EC50 of 8 nM against T. cruzi intracellular amastigotes, exhibits excellent oral bioavailability (52% in rats), favorable ADME properties, and no S1P pathway modulation. IID432 achieves relapse-free cure in a chronic T. cruzi infection mouse model, can be used for the study of Chagas disease .
Cat. No.: HY-149767
CAS No.: 2882934-64-5
CMX990 is a SARS-CoV-2 3CL protease inhibitor. The EC90s for inhibiting SARS-CoV-2 were 9.6 nM and 101 nM in human bronchial epithelial cells (HBECs) and HeLa-ACE2 cells, respectively. CMX990 has good ADME and pharmacokinetic properties .
Cat. No.: HY-10486
CAS No.: 361444-66-8
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JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal .
Cat. No.: HY-176287
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ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
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 .
Cat. No.: HY-106016
CAS No.: 119229-64-0
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HP 184 is an acetylcholine release (ChE) stimulator whose ADME properties can be altered by replacing hydrogen with deuterium .
Cat. No.: HY-157041
CAS No.: 3017151-83-3
MAGL-IN-10 is areversible monoacylglycerol lipase (MAGL) inhibitor with very good ADME properties and low in vivo toxicity.MAGL-IN-10 can be used for the research ofcancer, neurological disorders and inflammatory pathologies .
Cat. No.: HY-155103
CAS No.: 2961381-94-0
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Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study .
Cat. No.: HY-147549
CAS No.: 2492436-35-6
Antitrypanosomal agent 6 (compound 18a) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 6 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC50 value of 0.47 μM. Antitrypanosomal agent 6 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA .
Cat. No.: HY-147550
CAS No.: 2492436-38-9
Antitrypanosomal agent 7 (compound 18c) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 7 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC50 value of 0.71 μM. Antitrypanosomal agent 7 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA .
Cat. No.: HY-133031A
CAS No.: 474084-56-5
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CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
Cat. No.: HY-153145
CAS No.: 922128-14-1
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F2276-0104 is a potential PCAF bromodomain (PDB 5FDZ) inhibitor. F2276-0104 is predicted to have good cell permeability and ADME properties. F2276-0104 can be used for cancer-related research .
Cat. No.: HY-181110
Target:
Free Radical Scavengers Monoamine Oxidase Reactive Oxygen Species (ROS) Cholinesterase (ChE) Interleukin Related
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MAO-A-IN-4 is a highly selective and reversible inhibitor of monoamine oxidase A (MAO-A), with an IC50 of 0.06 μM against hMAO-A. MAO-A-IN-4 exhibits anti-inflammatory, antioxidant, neuroprotective, and antidepressant activities. MAO-A-IN-4 possesses favorable ADME properties and is suitable for research related to depression .
Cat. No.: HY-W237439
CAS No.: 958712-85-1
SEN205A is a fragment compound that binds to the hydrophobic pocket of human S100B (Kd=0.5-1.0 mM), which is the key region for the interaction of S100B with TRTK-12 and p53, and SEN205A can be displaced from this site by TRTK-12. SEN205A exhibits excellent in vitro ADME properties, including high metabolic stability, chemical stability, and good solubility under physiological pH conditions. SEN205A can serve as a starting fragment for structure-based optimization to develop inhibitors targeting the S100B-p53 protein-protein interaction and investigate the pathogenesis of malignant melanoma .
Cat. No.: HY-182757
CAS No.: 2812381-74-9
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Y1693 is an orally active RANKL inhibitor with a Kd of 5.03 μM for hRANKL. Y1693 inhibits the activation of the downstream c-fos/NFATc1 signaling pathway by blocking its interaction with RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation and bone resorptive activity, while downregulating the mRNA and protein expressions of TRAP, cathepsin K, c-fos and NFATc1. Y1693 shows no obvious cytotoxicity to bone marrow-derived macrophages and osteoclast precursor cells, and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research related to osteoporosis and periodontal diseases .
Cat. No.: HY-L041
468 compounds
Macrocycles, molecules containing 12-membered or larger rings, are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, showing favorable ADME- and PK-properties. Macrocycles have demonstrated repeated success when addressing targets that have proved to be highly challenging for standard small-molecule drug discovery, especially in modulating macromolecular processes such as protein–protein interactions (PPI). Otherwise, the size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity.
MCE offers a unique collection of 468 macrocyclic compounds which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE Macrocyclic Compound Library is a useful tool for discovering new drugs, especially for “undruggable” targets and protein–protein interactions.
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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
