Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity[1][2][3].
LGLLLRHLRHHSNLLANI (B18) is an 18 amino acid peptide. LGLLLRHLRHHSNLLANI derives from the membrane-associated protein binding. LGLLLRHLRHHSNLLANI shows a high affinity for Cu(2+) ions[1].
Di-N-desethyl Amiodarone hydrochloride is a metabolite of Amiodarone (HY-14187). Di-N-desethyl Amiodarone hydrochloride is a strong inhibitor of the respiratory chain[1].
4,4'-Dihydroxybiphenyl-d8 is the deuterium labeled 4,4'-Dihydroxybiphenyl[1].
2-Piperidone is an endogenous metabolite.
PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC50 of 0.01 μM.
Aristola-1(10),8-dien-2-one is a sesquiterpene compound that can be isolated from rhizome of Nardostachys chinensis of Valerianaceae[1].
TCO-GK-PEG4-NHS ester is an ADC Linker, and can be used for synthesis of [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d. [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d binds with high affinity and immunoreactivity to HER2[1].
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect[1][2][3].
Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418[1].
Sancycline (Bonomycin; 6-Demethyl-6-deoxytetracycline) hydrochloride is a semi-synthetic tetracycline antibiotic[1].
Isoguaiacin is a natural product[1].
SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells[1].
Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].
κM-Conotoxin RIIIK is a potassium channel antagonist. κM-Conotoxin RIIIKcan block voltage-activated potassium ion channels [1].
Talnetant Hcl(SB 223412 Hcl) is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.IC50 Value: 1.4 nM (hNK-3-CHO binding Ki) [1]Target: NK3 receptorin vitro: In vitro studies demonstrated that 53 is a potent functional antagonist of the hNK-3 receptor (reversal of senktide-induced contractions in rabbit isolated iris sphincter muscles and reversal of NKB-induced Ca2+ mobilization in CHO cells stably expressing the hNK-3 receptor), while in vivo this compound showed oral and intravenous activity in NK-3 receptor-driven models (senktide-induced behavioral responses in mice and senktide-induced miosis in rabbits) [1]. Talnetant has high affinity for recombinant human NK3 receptors (pKi 8.7) and demonstrates selectivity over other neurokinin receptors (pKi NK2 = 6.6 and NK1<4). In native tissue-binding studies, talnetant displayed high affinity for the guinea pig NK3 receptor (pKi 8.5) [3].in vivo: Rectal barostat tests were performed on 102 healthy volunteers, randomized to receive either oral talnetant 25 or 100 mg or placebo over 14-17 days [2]. Talnetant (3-30 mg/kg i.p.) significantly attenuated senktide-induced 'wet dog shake' behaviors in the guinea pig in a dose-dependent manner. Microdialysis studies demonstrated that acute administration of talnetant (30 mg/kg i.p.) produced significant increases in extracellular dopamine and norepinephrine in the medial prefrontal cortex and attenuated haloperidol-induced increases in nucleus accumbens dopamine levels in the freely moving guinea pigs [3].Toxicity: Talnetant had no effect on rectal compliance, sensory thresholds or intensity ratings compared with placebo [2].Clinical trial: Study Of Talnetant Versus Placebo And Risperidone In Schizophrenia. Phase 2
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability[1].
THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease[1].
Miroestrol is a highly active phytoestrogen. Miroestrol can produce mammogenic effect. Miroestrol exhibits bone loss prevention and neuroprotective in ovariectomized mice. Miroestrol also can reduce cancer risk[1][2][3][4].
Methyl O-Acetylricinoleate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
3-O-Benzoyl-1,2: 5,6-bis(di-O-isopropylidene)-alpha-D-galactofuranose 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].
Anti-MRSA agent 1 (Compound 13d) is a wonderful MRSA (MIC = 0.5 μg/mL) inhibitor. Anti-MRSA agent 1 (Compound 13d) could effectually relieve the development of MRSA resistance[1].
NIOCH 14 is a antiviral agent and a pro-drug. NIOCH 14 has antiviral activity against orthopoxviruses. NIOCH 14 can significantly lower proportions of infected mice, and virus production levels in the lungs. NIOCH 14 can be used for researching anti-smallpox[1][2].
HBV-IN-7 is a potent HBV inhibitor with an EC50 of 7 nM (WO2021213445A1, compound 5)[1].
2-(2,4-Dichlorobenzyl)thioadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
ATP dipotassium (Adenosine 5'-triphosphate dipotassium) is a central component of energy storage and metabolism in vivo, provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP dipotassium is an important endogenous signaling molecule in immunity and inflammation[1][2].
Furobufen, an anti-inflammatory agent, produces antiarthritic, antipyretic effects. Furobufen has an analgesic effect in inflamed tissue[1].