Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
Methacrolein-2,4-dinitrophenylhydrazone is a small molecule azo and nitro dye[1].
Bermekimab (MABp1) is a human monoclonal antibody that targets interleukin-1alpa (IL-1α). Bermekimab prevents tumour-related inflammation[1].
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) andgreater than 1600-fold selectivity over all other bromodomainstested.target: BRPF1.[1]In vivo: The ip route of administration would be suitable for dosing GSK6853 in potential PK/PD models. [1]
Ginsenoside Rh7 is a minor saponin isolated from the leaves of Panax ginseng[1].
5′-Deoxy-5′-iodothymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
(R)-2-Aminopent-4-enoic acid hydrochloride is a Glycine (HY-Y0966) derivative[1].
Corypalmine is an alkaloid from Corydalis chaerophylla. Corypalmine is an antifungal.
MOTS-c (human) is a biological active peptide. (Recent advances in high-resolution sequencing have led to the discovery of unique peptides derived from mitochondrial genome.1-2 Currently 8 peptides are identified: humanin, mitochondrial open reading frame of the 12S tRNA-c (MOTS-c), and six small humanin-like peptides (SHLP1-6). 1-2 All of these peptides are released into cytosol from mitochondria and associate with increased longevity and cell viability, reduced apoptosis, and other beneficial functions. 1-3 MOTS-c was found to reduce insulin resistance, decrease obesity, and promote homeostasis.)
c-JUN peptide is a cell-permeable c-JUN-JNK interaction inhibitor. c-JUN peptide inhibits serum-induced c-Jun phosphorylation. c-JUN peptide induces apoptosis[1].
Anti-inflammatory agent 46 (compound 7h) is an anti-inflammatory agent with nitric oxide (NO) inhibitory effect. Anti-inflammatory agent 46 binds to iNOS with low energies, inhibits swelling in mice (at dose of 10 mg/kg)[1].
(R)-2-((tert-Butoxycarbonyl)amino)pent-4-ynoic acid is a Glycine (HY-Y0966) derivative[1].
FPS-ZM1 is a high-affinity RAGE inhibitor with a Ki of 25 nM.
Revaprazan (SB 641257) is a reversible proton pump inhibitor with significant anti-inflammatory effects. Revaprazan can be used for chronic gastric inflammation research[1][2].
Labuxtinib is c-kit tyrosine kinase inhibitor[1].
A nonpeptidyl small molecule agonist of GDNF family receptor α1 (GFRα-1); concentration-dependently inhibits [(125)I]GDNF binding in Neuro-2A cells with IC50 of 10.4 uM; induces autophosphorylation of Ret protein, promotes neurite outgrowth in Neuro-2A cells, and induces Ret autophosphorylation in the Neuro-2A cells.
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca2+-release channels/ryanodine receptors (RyRs)? enhances the influx of Ca2+ from the sarcoplasmatic reticulum into the cell[1].
PF-06815345 hydrochloride is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 hydrochloride significantly decreases the PCSK9 level in vivo in mouse[1][2].
NMS-P945 is an ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs). NMS-P945 is suitable for conjugation to mAbs with reproducible Drug Antibody Ratio (DAR) >3.5[1].
Carteolol HCl is a non-selective beta blocker used to treat glaucoma.Target: Beta adrenergic ReceptorCarteolol HCl is a beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. Carteolol hydrochloride at 1 mmol/L (P<0.05) significantly inhibited H2O2-induced cell damage and was able to scavenge O2 (EC50 value: 48 mmol/L). carteolol hydrochloride has a protective action against UVB-induced HCEC damage, and its radical scavenging ability may be an important basis for this effect [1]. The new alginate formulation of long-acting carteolol 1% given once daily is as effective as standard 1% carteolol given twice daily, with no meaningful differences regarding safety. This efficacy wasy was verified at 9 AM (24 hours after the last drop of long-acting carteolol or 12 hours after that of standard carteolol) and at 11 AM (2 hours after the morning drop). The new alginate formulation of long-acting carteolol 1% given once a day is effective and well tolerated by glaucoma patients who require chronic treatment [2].
Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period[1][2].
P-CAB agent 1 (compound B19) is a highly potent potassium-competitive acid blocker agent with an IC50 value of 60.50 nM for H+/K+-ATPase. P-CAB agent 1 has acceptable oral absorption in rats. P-CAB agent 1 can be used for researching acid-related disorders (ARDs)[1].
Trastuzumab beta (ABP 980) is a biosimilar to Trastuzumab (HY-P9907). Trastuzumab beta is a monoclonal antibody (McAb) targeting human epidermal growth factor receptor 2 (HER2). Trastuzumab beta can be used for the research of HER2-positive metastatic breast cancer, early breast cancer (EBC), and metastatic gastric cancer[1].
Multicaulisin, a new Diels-Alder type adduct from Morus multicaulis roots, potently effects against Staphylococcus aureus (MRSA) isolates. Multicaulisin is an antibacterial drug and has the potential for MRSA infections research[1][2].
Ajugol is an iridiod glucoside.
Antifungal agent 31 (compound 12) is a potent and orally active triazole antifungal agents with a pyrrolotriazinone scaffold. Antifungal agent 31 shows antifungal activity against Candida spp. and filamentous fungi. Antifungal agent 31 significantly reduced mortality rates and kidney fungal burden in two murine models of lethal systemic infections[1].
Freneslerbart is an IgG4κ antibody targeting Felcat allergen 1. Felcat allergen 1 is an allergen protein[1].
6-Methylpseudouridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].