12 products were found matching "Cay11990"!

Prostaglandin B3 (PGB3) is a non-enzymatic dehydration product resulting from the treatment of Prostaglandin E3 (PGE3) with strong base. In a structure-activity binding study to determine the affinity of various prostaglandins to human PPARgamma, PGB3 exhibited a Ki value greater than 1 mM. In contrast, PGB1 and...

Thromboxane B3 (TXB3) is the stable hydrolysis product of TXA3 synthesized from eicosapentaenoic acid (EPA, Cay-90110) by COX and thromboxane synthase. It is biosynthesized in various tissues such as seminal vesicles, lung, PMNL, and ocular tissues.Formal Name: 9alpha,11,15S-trihydroxy-thromba-5Z,13E,17Z-trien-1-oic...

A-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172. A-769662 specifically activates beta1 subunit-containing AMPK heterotrimers, and its effects are independent...

WZB117 is an irreversible inhibitor of glucose transporter 1 (Glut1) that blocks glucose transport in diverse cancer cells (IC50 = ~0.6 µM), reducing extracellular lactate and intracellular ATP levels. It inhibits cancer cell proliferation (IC50s = 5-10 µM), resulting in cell cycle arrest, senescence, and necrosis...

Endoplasmic reticulum (ER) stress, caused by accumulation of misfolded proteins and a disruption of calcium homeostasis, has been linked to several neuronal diseases including, Parkinson's, Alzheimer's, and prion diseases. A screen for protective activity against ER stress-dependent cell death identified...

Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced...

Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 µM). It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 µM. Ro 67-7476 increases the...

Olopatadine is a histamine H1 receptor antagonist (Ki =41 nM). It is 1,059- and 4,177-fold selective for histamine H1 over H2 and H3 receptors, respectively. Olopatadine inhibits histamine-induced phosphoinositide turnover in isolated human conjunctival epithelial cells, isolated human corneal fibroblasts, and human...

TCN 238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4, EC50 = 1 µM). It has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells. It has no activity at the adenosine A2A, serotonin 5-HT1A, or...

Glutamate, the major excitatory neurotransmitter in the central nervous system, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors (mGlus) discovered thus far, development of inhibitors to mGlu5 has been given significant attention in preclinical...

Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16). While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8,...

Histamine has been implicated in a variety of biological functions including thermo- and immunoregulation, food intake, hyperexcitability, pain transmission, arousal, reward, memory, and emotional responses. The histamine H3 receptor is a Gi-coupled presynaptic auto- and hetero-receptor whose activation leads to a...