Search results for 'pri 724'
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24R-Calcipotriol(PRI 2202) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
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Arrhythmias-Targeting Compound 1 is used in the research of arrhythmias, extracted from patent WO 2001028992 A2.
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marine xenobiotic metabolite
Imidacloprid-urea with a role as a marine xenobiotic metabolite, is the primary imidacloprid soil metabolite, whereas imidacloprid-olefin is the main plant-relevant metabolite and is more toxic to insects than imidacloprid.
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Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities
Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica. Triphala inhibits NF-κB activation. Triphala exerts antifungal action. Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
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mucosal protective agent and an anti-ulcer drug
Cetraxate (DV-1006) Hydrochloride (HCl) is a mucosal protective agent and an anti-ulcer drug candidate. Cetraxate raises levels of calcitonin gene-related peptide and substance P in human plasma.
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BTK inhibitor
BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.
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Merafloxacin, also known as CI 934, is a fluoroquinolone antibacterial, which was also identified as a ?1 PRF inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on ?1 PRF of other beta coronaviruses. Importantly, frameshift inhibition by merafloxacin substantially impedes SARS-CoV-2 replication in Vero E6 cells, thereby providing the proof of principle of targeting ?1 PRF as an effective antiviral strategy for SARS-CoV-2.
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neurotrophic agent
Leteprinim, also known as AIT-082 and SPI-205, is a neurotrophic agent potentially for the treatment of Alzheimer's disease, and spinal cord injury.
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Class III antiarrhythmic agent
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion.
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Oleanolic acid derivative 1 is an oleanolic acid derivative, which is a novel triterpenoid-steroid hybrid molecule.
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D2R antagonist
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist.
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beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
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antibody drug conjugates (ADCs) toxin
Duocarmycin MA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-drug resistant cell lines.
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Dual MDM2/TSPO Inhibitor
PK 11195 is a 2?Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitor, and is potentially useful for the Treatment of Gliomas.
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dopamine D2 receptor antagonist
Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.
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fluorescent derivatization reagent
5-FAM (5-Carboxyfluorescein) contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid. Fluorescein is the most common fluorescent derivatization reagent for labeling biomolecules.
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PrPSc-IN-1 is a fluorescent probe, binds to the misfolded protein PrPSc, inhibits its accumulation, with an IC50 of 1.6 μM. Anti-prion activity.
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UAE (UBA1) inhibitor
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination.
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Dihydrofolate inhibitor
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
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Trimethoprim 3-oxide (Trimethoprim 3-N-oxide) is the primary metabolite of trimethoprim.
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ACE inhibitor
Rentiapril is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity.
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ACE inhibitor
Utibapril is an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activities.
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RAR degrader
PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader.
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KDM2A/7A inhibitor
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16?μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
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Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.
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ERα degrader
PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader.
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AR degrader
PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader.
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KIT and PDGFRA inhibitor
Avapritinib (BLU-285) is a highly potent, selective, and orally bioavailable KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively.
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ACE inhibitor
NCX899 is a NO-releasing derivative of enalapril, and shows inhibitory activity against angiotensin-converting enzyme (ACE) activity.
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dopamine D2/D3 receptor antagonist
Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively.
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Eprinomectin(MK-397) is an avermectin selected for development as a topical endectocide; has anthelmintic, insecticidal and miticidal activity.
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d-Atabrine dihydrochloride is an active enantiomer of quinacrine which displays antiprion activity.
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Luminol(Diogenes reagent) is a versatile chemical that exhibits chemiluminescence, with a striking blue glow, when mixed with an appropriate oxidizing agent.
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progesterone receptor modulator
Ulipristal (acetate) is a novel selective progesterone receptor modulator (SPRM) for the treatment of benign gynecological conditions such as uterine myoma.
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CYP3A4/5 inhibitor and substrate
Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
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Top1 inhibitor
Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively.
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dopamine D2/D3 receptor antagonist
Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
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PDE3 inhibitor
Olprinone(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor.
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HCV NS5B polymerase inhibitor
NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC50 of NM107 in the wild-type replicon cells is 1.85 μM.
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T-type Ca2+ channel antagonist
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
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l-Atabrine dihydrochloride is a less active enantiomer of quinacrine which displays antiprion activity.
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metalloproteinase inhibitor
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively.
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N-Desmethyl Clomipramine D3 hydrochloride is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine'.
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hERG potassium channel inhibitor
Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
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amine-reactive green fluorescent dye
5(6)-FAM SE is an amine-reactive green fluorescent dye widely used for labeling proteins or other molecules that contain a primary or secondary aliphatic amine.
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ERbeta agonist
Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.
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P2X7 receptor antagonist
CE-224535 is a selective P2X7 receptor antagonist.
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5(6)-Carboxyfluorescein contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid; cell-impermeant 5,6-FAM can also be used as a nonfixable polar tracer to investigate fusion, lysis and gap-junctional communication and to detect changes in cell or liposome volume.
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Valifenalate(IR5885; Valiphenal), which is approved for application on high-value crops such as grapes, tomatoes and other vegetables, is effective against various types of mildew and is currently marketed primarily under the Valis moniker; insecticide agent.
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5(6)-TAMRA contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid; bright, orange-fluorescent dye produces conjugates with absorption/emission maxima of ~555/580 nm.
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