GPVI antagonist 1 (compound 5) is a glycoprotein VI (GPVI) platelet receptor antagonist. GPVI antagonist 1 inhibits collagen-induced platelet aggregation with an IC50 of 25.3 μM[1].
Z-DL-Pro-OH (N-Cbz-DL-proline) is a proline derivative, can be used for the synthesis of drugs or other compounds[1].
PHOME is a fluorogenic substrate for sEH. sEH can hydrolyze the epoxy ring in the PHOME substrate. PHOME can be used for fluorescent epoxide hydrolase assay (extracted from patent CN113402447A)[1].
LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect[1][2].
Calpain inhibitor V (Mu-Val-HPh-FMK) is a cell-permeable and irreversible inhibitor of calpain that has anti-chlamydial activity[1].
Solriamfetol (JZP-110) is a selective dopamine and norepinephrine reuptake inhibitor with robust wake-promoting effects. Solriamfetol binds to dopamine and norepinephrine transporters, so it can inhibit reuptake of dopamine and norepinephrine. Solriamfetol treatment significantly improves the ability to stay awake and subjective symptoms of excessive sleepiness in adults with narcolepsy.
Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.
[DAla2] Dynorphin A (1-9) (porcine) is a dynorphin, which can be used in studies of analgesic, addiction, and depression.
Sitaxsentan (sodium) is an orally active, highly selective antagonist of endothelin A receptors.
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
DMG-PEG 2000 is used for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles[1].
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2].
AR-C66096 (FPL 66096) tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism[1].
mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC50 of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC50 of 119 nM[1].
PYBG-TMR is a dye and has a role as a fluorochrome. PYBG-TMR specifically and efficiently labels the target genetically encoded SNAP-tags in live cells[1].
RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice[1].
Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo[1].
Sodium benzoate can be used as an excipient, such as antimicrobial agent, preservative, lubricant. 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[1].
Tadnersen (BIIB078), an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion[1].
H-Phe-Gly-His-p-nitro-Phe-Phe-Ala-Phe-OMe is a polypeptide that can be hydrolyzed by Rennin (HY-P2810). H-Phe-Gly-His-p-nitro-Phe-Phe-Ala-Phe-OMe is commonly used as a biochemical reaction reagent[1].
Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor[1].
AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.IC50 Value: Target: GABA receptorin vitro: AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1]. in vivo: AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3].
Sulfo-Cy3-Tetrazine is a click chemistry reagent containing an tetrazine group. Sulfo-Cy3-Tetrazine is water soluble cyanine fluorescence dye, which is an inverse electron demand [4+2] cycloaddition that takes place between tetrazine and trans-cyclooctene or other strained olefin.
Gelidoside is a acylsecoiridoid glucoside isolated from the aerial parts of Gentiana gelida[1].
Soladulcoside A is a steroidal glycoside and antineoplastic agent that can be obtained from the whole plant of Solanum nigrum. Soladulcoside A can inhibit A549 cells and has the potential to study cancers such as non-small cell lung cancer (NSCLC)[1].
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM[1].
Cyclo (ARG-ALA-ASP- (D-Tyr) -LYS) (C (Radyk)) is a control peptide for c(RGDyK)[1].
m-PEG10-alcohol (Decaethylene glycol monomethyl ether) is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. m-PEG10-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CHIR-99021 trihydrochloride is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases[1][2].