Tanimilast (CHF-6001) is a novel highly potent and selective phosphodiesterase 4 inhibitor(IC50=0.026 ± 0.006 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration.Tanimilast is used for the research of obstructive lung diseases[1].
Coenzyme A (trilithium), a ubiquitous essential cofactor, is an acyl group carrier and carbonyl-activating group for the citric acid cycle and fatty acid metabolism. Coenzyme A (trilithium) plays a central role in the metabolism of carboxylic acids, including short- and long-chain fatty acids[1].
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors[1][2].
(S)-4-(tert-Butoxy)-3-((tert-butoxycarbonyl)amino)-4-oxobutanoic acid is an aspartic acid derivative[1].
Ginsenoside Ra3, isolated from Panax ginseng, possesses anti-cancer activity[1].
KCC2 blocker 1 is an orally active and selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate and has antiepileptic effect[1].
Seliforant (SENS-111, SENS111) is a novel potent, selective histamine H4 receptor antagonist.
HEP-1 (Human ezrin peptide (324-337)) is an orally active peptide with anti-HIV activity. HEP-1 enhances antibody titers generated by hepatitis B vaccination. HEP-1 has the potential to be studied against viral infections[1].
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
JT002 is an orally active inhibitor of the NLRP3 inflammasome. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice[1].
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2).
Daphnicyclidin F is a Daphniphyllum alkaloid isolated from the stem of Daphniphyllum humile[1].
Propargyl-PEG17-methane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Wallichoside is a sesquiterpene that can be isolated from Pteris wallichiana[1].
1-Methyl-2-[(Z)-6-undecenyl]-4(1H)-quinolone, as a colorless oil, is a quinolone alkaloid isolated from the fruit of Evodia rutaecarpa BENTHAM (Rutaceae)[1].
Z-Asp(OMe)-OH is an aspartic acid derivative[1].
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM)[1].
Novel highly potent, selective, and irreversible GSTP1 inhibitor
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease[1][2].
Morpholine-d8 (hydrochloride) is the deuterium labeled Morpholine hydrochloride[1].
Fmoc-N-amido-PEG7-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
L-Alpha glycerylphosphorylcholine (alpha-GPC, choline alfoscerate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have potential for the treatment of Alzheimer's disease and dementia.IC50 value:Target: Anti-ADAlpha-GPC rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer’s disease. An Italian multicentre clinical trial on 2,044 patients suffering from recent stroke were supplied alpha-GPC in doses of 1,000 mg/day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].
STING modulator-5 (compound 38) is a STING modulator with a pIC50 value of 9.5. STING modulator-5 antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. STING modulator-5 is a antagonist of THP-1 cells, it can be used for immunological disease research[1].
L,L-Dityrosine is a constituent of acid hydrolysates of a number of biological materials, including the insect cuticular resilin[1].
Nauclefine is an indole alkaloid isolated from Nauclea officinalis. Nauclefine acts as a PDE3A modulator to induce cancer cell apoptosis through a PDE3A-SLFN12-dependent death pathway[1].
Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities.
Hexasodium phytate (Phytic acid hexasodium) is a phosphorus storage compound of seeds and cereal grains. Hexasodium phytate has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Hexasodium phytate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
2’-Chloro-N6-benzyl adenosine 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].
4′-Bromoflavone, a cancer chemopreventive agent, is a potent phase II detoxification enzymes inducer[1].
Alogliptin(SYR-322) is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.IC50 value: <10 nMTarget: DPP4Alogliptin is an orally administered, anti-diabetic drug in the DPP-4 inhibitor class. A randomized clinical trial reporting in 2011 aimed to determine the efficacy and safety of alogliptin versus placebo and voglibose among newly diagnosed Type 2 diabetes patients in Japan. The main outcome indicated that alogliptin was statistically superior to both comparitors. A randomized clinical trial reporting in 2012 aimed to demonstrate that alogliptin was "non-inferior" to a "very low fat/calorie traditional Japanese diet" among newly diagnosed Type 2 diabetes patients in Japan. The outcome indicated that both the drug and dietary treatments comparably impacted indicators of the diabetic condition, such as HbA1c levels and glycemic efficacy. The drug treatment had its impact without changing body mass index (BMI), but the dietary treatment was accompanied by a significant reduction in the BMI…