10 products were found matching "Cay14659-25"!

The Src kinases constitute a family of non-receptor tyrosine kinases, which includes Src and Lck. Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes. It less effectively blocks the receptor tyrosine kinases VEGFR2 and C-fms (IC50 =...

Tegaserod (maleate) is a potent agonist of the serotonin 4 receptor (5-HT4, Ki = 3.9-31 nM). As 5-HT4 receptors are associated with cholinergic nerves lining the colon, tegaserod (maleate) stimulates colonic motility and transit in vivo, in both healthy and diseased gastrointestinal tracts. However, it lacks...

Citicoline is an endogenous intermediate in the synthesis of phosphatidylcholine, the major phospholipid in eukaryotic cells. It also serves as a choline donor in the biosynthesis of the neurotransmitter acetylcholine. Citicholine demonstrates protective effects in cerebral ischemia, traumatic brain injury, and...

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 µM, respectively). It less effectively blocks the activity of myosin light chain kinase (IC50 = 240 µM).Formal Name:...

Clorgyline is a potent monoamine oxidase (MAO) inhibitor that preferentially targets MAO-A over MAO-B (Kis = 0.054 and 58 µM, respectively). This inhibition is irreversible. Clorgyline is without effect on serotonin (Cay-14332) receptors, but it does inhibit the sigma receptor sigma1 on Jurkat human T lymphocyte...

JWH 081 (Cay-10579) is a cannabimimetic aminoalkylindole that shows a high-affinity for the central cannabinoid (CB1) receptor with a Ki value of 1.2 nM and ten-fold reduced affinity for the peripheral cannabinoid (CB2) receptor (Ki = 12.4 nM). JWH 081-N-(cyclohexylmethyl) analog (Cay-14655) is a synthetic CB where...

Physical exertion and exercise are the primary defenses against obesity, insulin resistance, and diabetes. The transcriptional co-activator peroxisome proliferator-activated receptor C coactivator 1alpha (PGC-1alpha), regulates mitochondrial biogenesis and function. Expression of the membrane protein fibronectin...

Loratadine is a non-sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H1 receptors (Ki = 35 nM). It has been shown to inhibit the release of leukotriene C4 (IC50 = 8 µM) and histamine (IC50 = 11 µM) from rodent mast cells and to inhibit allergic bronchospasm in guinea pigs with...

Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue. It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets. Oleic...

JNK inhibitor VIII is an inhibitor of JNK1, JNK2, and JNK3 (Kis= 2, 4, and 52 nM, respectively). It is selective for JNK1, JNK2, and JNK3 over a panel of 74 kinases (Kis = >720 nM for all). It inhibits the phosphorylation of c-Jun in HepG2 cells (EC50 = 920 nM). JNK inhibitor VIII (10 µM) inhibits NGF-induced...