EIDD-1931-d2 is the deuterium labeled 3,6-Dichloro-2-methoxybenzoic acid[1].
Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R[1].
Inarigivir soproxil is an agonist of innate immunity and shows potent antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.
Azido-PEG3-CH2CO2Me is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Fmoc-β-cyclopropyl-L-Alanine is an alanine derivative[1].
NBD-Arg-Pro-Lys-Pro-Leu-Ala-Nva-Trp-Lys-(DMC)-NH2 is an substrate for hydrolysis of the matrix metalloproteinase stromelysin (MMP-3) and can be easily detected at Abs/Em=350/465 nm[1].
Spirendolol is a β adrenergic receptor antagonist.
Lenperone (AHR 2277 free?base) has antipsychotic effect. Lenperone improves depressive symptoms[1].
E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway[1].
Cinnamycin is tetracyclic lantibiotic produced from S. cinnamoneus that contains four unusual amino acids: erythro-β-hydroxyaspartic acid, mesolanthionine, threo-β-methyllanthionine, and lysinoalanine.1 Cinnamycin has demonstrated antiviral activity against herpes simplex virus type 1 KOS strain infection in Vero cells via a cytopathic effect reduction assay. Cinnamycin recognizes the structure of phosphatidylethanolamine and forms an equimolar complex with the phospholipid on biological membranes. This peptide has been used as a probe for analyzing the transbilayer movement of phosphatidylethanolamine.
Coumarinic acid is a brain-penetrating inhibitor of AChE and β-amyloid. Coumarinic acid can be used in study anti-Alzheimer drug[1].
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats[3][4][5].
Iopanoic acid is an inhibitor of 5'-Deiodinase and also an iodinated contrast medium.
(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader[1].
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease[1][2][3][4].
PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.
Ethyl (4-(trifluoromethoxy)phenyl)glycinate is a Glycine (HY-Y0966) derivative[1].
Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacterium tuberculosis (M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml)[1].
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 106 μg/mL. Cefroxadine can be used for the research of infection[1].
Ganoderenic acid C is a triterpenoid isolated from Ganoderma lingzhi. Ganoderenic acid C is abundant in fruit bodies at an early growth stage[1].
Tetrakis (4-carboxyphenyl) porphyrin (TCPP) plays the role of a metal remover[1].
Schisandrol B is one of its major active constituents of traditional hepato-protective Chinese medicine, Schisandra sphenanthera.IC50 value:Target:in vitro: SolB pretreatment significantly attenuated the increases in alanine aminotransferase and aspartate aminotransferase activity, and prevented elevated hepatic malondialdehyde formation and the depletion of mitochondrial glutathione (GSH) in a dose-dependent manner. SolB also dramatically altered APAP metabolic activation by inhibiting the activities of CYP2E1 and CYP3A11, which was evidenced by significant inhibition of the formation of the oxidized APAP metabolite NAPQI-GSH [1]. SolB abrogated APAP-induced activation of p53 and p21, and increased expression of liver regeneration and antiapoptotic-related proteins such as cyclin D1 (CCND1), PCNA, and BCL-2.
Alpha-cyperone is associated with the down-regulation of COX-2,IL-6,Nck-2,Cdc42 and Rac1, resulting in reduction of inflammation. which would be highly beneficial for treatment of inflammatory diseases such as AD.In vitro: The anti-inflammatory activity of alpha-cyperone is associated with the down-regulation of COX-2 and IL-6 via the negative regulation of the NFκB pathway in LPS-stimulated RAW 264.7 cells.[1]Alpha-Cyperone binds and interacts with tubulin and is capable of distinctly destabilizing microtubule polymerization. The effect of this interaction could result in reduction of inflammation which would be highly beneficial for treatment of inflammatory diseases such as AD. One microliter of alpha-Cyperone was dissolved in DMSO (1:1 v/v) and it was further diluted in double distilled water (ddH2O) to a final volume of 20 microliter. [2]
H-Glu-OtBu is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). H-Glu-OtBu is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2
(((9H-Fluoren-9-yl)methoxy)carbonyl)-L-cysteine is a cysteine derivative[1].
Relatlimab (BMS-986016) is a human monoclonal antibody anti-LAG-3 antibody generated by immunization of transgenic mice bearing human immunoglobulin miniloci with recombinant LAG-3 protein. Relatlimab blocks LAG-3/MHC II interaction with an IC50 value of 0.67 nM and LAG-3/FGL1 interaction with an IC50 value of 0.019 nM. Relatlimab can be used in research of cancer[1].
H-Glu(OtBu)-OtBu is a glutamic acid derivative[1].
L-DOPA is a natural form of DOPA used in the treatment of Parkinson's disease. L-DOPA is the precursor of dopamine and product of tyrosine hydroxylase.Target: Dopamine ReceptorL-DOPA (L-3,4-dihydroxyphenylalanine) is a chemical that is made and used as part of the normal biology of humans, some animals and plants. Some animals and humans make it via biosynthesis from the amino acid L-tyrosine. L-DOPA is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine collectively known as catecholamines. L-DOPA can be manufactured and in its pure form is sold as apsychoactive drug with the INN levodopa; trade names include Sinemet, Parcopa, Atamet, Stalevo, Madopar, Prolopa, etc. As a drug it is used in the clinical treatment of Parkinson's disease and dopamine-responsive dystonia.L-DOPA crosses the protective blood-brain barrier, whereas dopamine itself cannot. Thus, L-DOPA is used to increase dopamine concentrations in the treatment of Parkinson's disease and dopamine-responsive dystonia. This treatment was made practical and proven clinically by George Cotzias and his coworkers, for which they won the 1969 Lasker Prize. In addition, L-DOPA, co-administered with a peripheral DDCI, has been investigated as a potential treatment for restless leg syndrome. However, studieshave demonstrated "no clear picture of reduced symptoms".
DBCO-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
MC-4R Agonist 2 hydrochloride (Example 1) is a MC4R agonist. MC-4R Agonist 2 hydrochloride can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction[1].