12 products were found matching "Cay16150"!

1-(1-Naphthyl)piperazine (1-NP) is a ligand for serotonin (5-hydroxytryptamine, 5-HT) receptors. It acts as an antagonist for 5-HT at 5-HT1 and 5-HT2 in rat cortical membranes with IC50 values of 6 and 1 nM, respectively. 1-NP also blocks contraction in the rat fundus induced by either 5-HT or tryptamine (IC50 = 1...

5-Methylcytidine is a modified nucleoside derived from 5-methylcytosine and is a minor constituent of RNA as well as DNA for certain organisms. Roughly one to two residues of 5-methylcytidine occur in every 1,000 RNA residues. It has been used in epigenetics research, especially in studies involving DNA methylation...

Sinomenine is a natural plant alkaloid commonly used to alleviate inflammation associated with rheumatoid arthritis. It activates histamine release, reduces joint stiffness and pain, and alters cytokine generation without producing gastrointestinal adverse events. Sinomenine also impairs signaling through NF-kappaB,...

Rapamycin (Cay-13346) is a natural macrolide immunosuppressant that activates mTORC1. Seco rapamycin (sodium salt) is a nonenzyme-dependent degradation product of rapamycin (Cay-13346) resulting from ester hydration followed by dehydration. It has less than 4% of the potency of rapamycin in a thymocyte proliferation...

Phentolamine is a reversible antagonist of alpha-adrenergic receptors, non-specifically binding all alpha1- and alpha2-adrenoceptors with nanomolar affinities. Formulations containing phentolamine have been used in the treatment of hypertensive emergencies, as well as chronic and emergent pain.Formal Name:...

trans-Clovamide is a naturally occurring caffeoyl conjugate identified in the antioxidant polyphenolic fraction of cocoa (T. cacao L.). It has antioxidant and antiradical properties and has shown neuroprotective effects (EC50s = 0.9-3.7 µM) in several in vitro models of neuronal death.Formal Name:...

5-Methyltetrahydrofolic acid is a biologically active form of folic acid that functions, in conjunction with vitamin B12, as a methyl-group donor involved in the conversion of homocysteine to methionine. The availability of methyl groups is essential for a variety of methylation reactions including the synthesis of...

Bisphosphonates bind strongly to bone and reduce bone resorption through effects on both osteoclasts and osteoblasts. Clodronate is a non-nitrogenous bisphosphonate that has been used in the treatment of osteoporosis and other metabolic bone diseases. It binds to hydroxyapatite crystals with an affinity constant of...

Estradiol 3-(beta-D-glucuronide) (E23G) is a non-cholestatic regioisomer of the estrogen metabolite, estradiol 17-(beta-D-glucuronide) (E217G, Cay-16156). It acts as a substrate for multidrug resistance protein 2 (MRP2, Km = 122 µM), competing with E217G for MRP2-mediated transport (IC50 = 14.2 µM). E23G has been...

Estradiol 17-(beta-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile. It acts as a substrate of the multidrug resistance protein 2 (MRP2, Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow. In addition to...

PluriSln 1 is an N-acyl phenylhydrazine derivative that inhibits stearoyl-CoA desaturase, a key enzyme for lipid metabolism that is expressed in human pluripotent stem cells (hPSCs). PluriSln 1 can selectively induce ER stress, attenuate protein synthesis, and induce apoptosis in hPSCs (EC50 = 2 µM) while sparing...

Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO. By acting at SMO, GSA 10 has been shown to promote the differentiation of...