TCTDSTNCYKAT is an engineered-variant peptide of antifreeze protein (AFP)[1].
Timiperone has a strong affinity for cerebral dopamine D2 receptor. Timiperone has antipsychotic activity, and inhibits stereotyped behaviour. Timiperone can be used for research of schizophrenia[1][2][3].
RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM[1].
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d9 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
5,6-Dihydroxyindole, a melanin precursor, has a broad-spectrum antibacterial, antifungal, antiviral, antiparasitic activity. 5,6-Dihydroxyindole has cytotoxic effects and is strongly toxic against various pathogens[1].
Urolithin A is an intestinal metabolite of ellagic acid with antioxidant and antiproliferative effects; inhibits T24 and Caco-2 cell growth with IC50 values of 43.9 and 49 μM, respectively.
Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi)Target: 5-HT4 receptorPrucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Receptor binding data have demonstrated prucalopride's high affinity to both investigated 5-HT(4) receptor isoforms, with mean pK(i) estimates of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively. From the 50 other binding assays investigated in this study only the human D(4) receptor (pK(i) 5.63), the mouse 5-HT(3) receptor (pK(i) 5.41) and the human sigma(1) (pK(i) 5.43) have shown measurable affinity, resulting in at least 290-fold selectivity for the 5-HT(4) receptor [1].
Bumetanide D5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na+-K+-Cl- (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1].
Zingiberen Newsaponin is extracted from isolated from Dioscorea zingiberensis. Zingiberen Newsaponin exhibits induction effect on platelet aggregation[1].
PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs[1].
Lvguidingan is a potent anticonvulsant agent. Lvguidingan also has sedative-hypnotic, tranquilizing, and muscle-relaxing actions. Lvguidingan can be used as antiepileptic agent[1][2].
Metham sodium (Carbathion) is a broad-spectrum soil microbial suppressant. Metham sodium controls soil-borne pests and weeds. Metham sodium inhibits weed seeds, plant-parasitic nematodes, plant pathogenic fungi and soil insects[1].
Obtucarbamate B is a carbamate derivative, that can be isolated from the South China Sea gorgonian coral Melitodes squamata Nutting[1].
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].
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM.GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools[1].
EILDV (human, bovine, rat) is an analogue of the active pentapeptide. EILDV (human, bovine, rat) has active tripeptide amino acid sequence LDV that is conserved in human, bovine, rat. EILDV (human, bovine, rat) can be used for the research of cell adhesion[1].
AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential[1].
1-Deoxy-L-threo-sphinganine-d3 is deuterium labeled 1-Deoxy-L-threo-sphinganine.
PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity[1]. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL)[2].
Glycitin is a natural isoflavone isolated from legumes; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.
Amyloid β-Protein (3-42) is the precursor of Pyr peptide. Pyroglutamate-modified Aβ (pEAβ) (3-42) is the core of the amyloid template block in Alzheimer's disease. pEAβ(3-42) accelerated the aggregation of Aβ(1-42), while Aβ(1-42) significantly slowed the primary and secondary nucleation of pEAβ(3-42)[1].
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist with an IC50 of 12 nM.
SCH54292 is a potent Ras-GEF interaction inhibitor with IC50 of 0.7 μM[1].
JNc-440 is a small molecule that significantly and specifically strengthens the TRPV4-KCa2.3 interaction in mouse endothelial cells, but does not systemically activate TRPV4 and KCa2.3; shows affinity for both TRPV4 and KCa2.3, enhances vasodilation and exerts antihypertensive effects in mice.
Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) [1].
L-Pyrrolysine lithium is the 22nd genetically encoded amino acid. L-Pyrrolysine lithium is an α-amino acid[1][2].
ER-819762 is a novel potent, selective, orally active EP4 receptor antagonist with IC50 of 59 nM in cAMP-dependent reporter assay; inhibits EP4-stimulated Th1 differentiation, Th17 cell expansion, and IL-23 secretion by activated dendritic cells; exhibits no agonism or antagonism for the related PGE2 EP1, EP2 and EP3 receptors; suppresses Th1 and Th17 cytokine production, suppresses disease in collagen- and GPI-induced arthritis in mice, and suppresses CFA-induced inflammatory pain in rats.
(R)-Azasetron besylate (SENS-401) is an orally active calcineurin inhibitor. (R)-Azasetron besylate reduces Cisplatin (HY-17394)-induced hearing loss and cochlear damage[1][2].
exo-Polygalacturonase is an extracellular pectinolytic enzyme. exo-Polygalacturonase acts from the non-reducing side, hydrolyzes pectic acids, and releases mono-galacturonate[1].
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[1][2].