DMT-2'-O-Methylguanosine phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
MC-EVCit-PAB-MMAE (Linker-Payload 11) is a drug-linker conjugates for ADC. MC-EVCit-PAB-MMAE contains the ADCs linker (MC-EVCit-PAB) and a potent tubulin polymerization inhibitor MMAE (HY-15162)[1].
GSK467 is a selective KDM5 (JARID1) inhibitor with a Ki of 10 nM for KDM5B, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members[1].
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively[1][2].
Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
Thiamine monochloride (Vitamin B1) is an essential vitamin that plays an important role in cellular production of energy from ingested food and enhances normal neuronal actives.
Biotinyl tyramide is a biotin derivative used for tyramide signal amplification, as a reagent to amplify both immunohistochemical signals and in situ hybridization protocols[1][2][3][4].
5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 free base has antipsychotic drug-like activity. 5-HT2C agonist-3 free base blocks Amphetamine-induced hyperactivity[1].
Eperisone-d10 ((±)-Eperisone-d10) hydrochloride is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect[1][2 [3].
Sodium 2-oxobutanoate-13C,d4 is the deuterium and 13C labeled Sodium 2-oxobutanoate[1].
Noraucuparin is a biphenyl-type phytoalexin. Noraucuparin has antifungal effect. Noraucuparin can be isolated from the leaves of Sorbus pohuashanensis[1].
Arbaclofen placarbil is a novel transported prodrug of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist
Dasycarpol (compound 2) is a product of microbial transformation of fraxinellone by Aspergillus niger (AS 3.421). Dasycarpol shows moderate cytotoxicity against A549 cells ,with the IC50 of 20 ug/mL[1].
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells, suppressing the phosphorylation of Dvl2/3 and LRP6 in HeLa cells. IWP-O1 functions by preventing the secretion of Wnt proteins[1].
Swainsonine is an alkaloid isolated from Astragalus, acts as an inhibitor of α-mannosidase, with anti-tumor activity[1].
N-(Azido-PEG3)-N-Boc-PEG3-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Br-PEG3-CH2COOH (compound 28) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Voleneol is a sesquiterpene, that can be isolated from the seeds of Guarea guidonia (MELIACEAE)[1].
m-PEG4-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Clonostachydiol is an anthelmintic macrodiolide from the fungus Clonostachys cylindrospora (strain FH-A 6607)[1].
Bi-linderone is isolated as racemate from the traditional Chinese medicinal plant Lindera aggregata. Bi-linderone has activity against glucosamine-induced insulin resistance in HepG2 cells at a concentration of 1 μg/mL[1].
ENMD-1068 hydrobromide is a potent PAR2 antagonist. ENMD-1068 hydrobromide attenuates joint inflammation in a dose-dependent manner. ENMD-1068 hydrobromide can be used in research of joint inflammation[1].
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2.
AChE/BChE-IN-2 (Compound 13b) is a potent inhibitor of AChE/BChE (AChE IC50 = 0.96 ± 0.14 µM, BChE IC50 = 1.23 ± 0.23 µM). AChE/BChE-IN-2 has the potential for the research of AD diseases[1].
Hederagenic acid (compound 2) is a kind of triterpenoid saponin. Hederagenic acid can be isolated from the roots of Kalopanax septemlobus (Thunb.) Koidz[1].
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects[1][2].
Diammonium Glycyrrhizinate, isolated from the licorice root, is a widely used anti-inflammatory agent[1].
Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca2+ levels. Angiotensin II also acts at the Na+/H+ exchanger in the proximal tubules of the kidney[1][2].
Xylazine Hydrochloride is α2 class of adrenergic receptor agonist.Target: Adrenergic ReceptorXylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. An analogue of clonidine, it is an agonist at the α2 class of adrenergic receptor. Xylazine has recently emerged as a recreational drug, especially in Puerto Rico [1]. Administration of xylazine (0.17 mg/kg of body weight, diluted to a 10-ml volume, using 0.9% NaCl) induced approximately 2.5 hours of local analgesia without apparent side effects. Higher doses of xylazine caused mild hind limb ataxia. Administration of lidocaine induced a similar duration of analgesia, with severe hind limb ataxia (100% incidence). We concluded that xylazine given by epidural injection results in safe, effective perineal analgesia in horses [2].
L-Leucine-2-13C is the 13C-labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway[1].