Oxazinanes
Cayman Chemical SB242084 hydrochloride
An antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors; brain penetrant with significant anxiolytic activity; used extensively in animal research
Cayman Chemical Fingolimod hydrochloride
An immune modulator and a prodrug form of FTY720 phosphate; decreases the number of circulating lymphocytes in mice at 1 mg/kg; increases skin allograft survival in rats from 0.3-3 mg/kg; prevents disease development in a rat model of EAE; inhibits S1P lyase from 0.3-30 µM
Cayman Chemical PIK75 hydrochloride
A selective inhibitor of p110α with an IC50 value of 5.8 nM; inhibits p110γ and p110β with IC50 values of 0.076 µM and 1.3 µM, respectively
Cayman Chemical Trimidox hydrochloride
A specific ribonucleotide reductase inhibitor; inhibits growth of human promyelocytic leukemia HL-60 cells (IC50 = 35 µM)
Cayman Chemical MethylLNIO hydrochloride
A competitive NOS inhibitor; more potent inhibitor of nNOS (Ki = 3.0 µM) than eNOS (Ki = 10.0 µM) or iNOS (Ki = 9.5 µM)
Cayman Chemical H89 hydrochloride
A potent, non-selective inhibitor of PKA with an IC50 value of 0.14 µM (Ki = 48 nM) that is widely used to disrupt PKA signaling; inhibits S6K1, MSK1, ROCK2, PKBa, and MAPKAP-K1b with IC50 values of 0.08, 0.12, 0.27, 2.6, and 2.8 µM, respectively
Cayman Chemical MethylLNIO hydrochloride
A competitive NOS inhibitor; more potent inhibitor of nNOS (Ki = 3.0 µM) than eNOS (Ki = 10.0 µM) or iNOS (Ki = 9.5 µM)
Cayman Chemical Fingolimod hydrochloride
An immune modulator and a prodrug form of FTY720 phosphate; decreases the number of circulating lymphocytes in mice at 1 mg/kg; increases skin allograft survival in rats from 0.3-3 mg/kg; prevents disease development in a rat model of EAE; inhibits S1P lyase from 0.3-30 µM
Cayman Chemical PropenylLNIO hydrochloride
A potent, selective iNOS inhibitor (Kis = 17, 10.3 and 58.2 µM for iNOS, nNOS, and eNOS, respectively, for initial rate binding kinetics); demonstrates reversible tight binding inhibition that is selective for iNOS over nNOS (Kis = 0.56 and 6 µM, respectively)
Cayman Chemical SRT 1720 hydrochloride
A selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol; improves insulin sensitivity, lowers plasma, glucose and increases mitochondrial capacity in diet-induced obese and diabetic leptin-deficient ob/ob mice after one week of treatment with an oral dose of 100 mg/kg once daily.
Cayman Chemical Dimebolin hydrochloride
A neuroprotective agent; binds to histamine H1 and H2 receptors (IC50s = 3.8 and 287 nM, respectively), as well as α1A-, α1B-, α1D-, and α2A-ARs, imidazoline I2 receptors, and 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors (Kis = 8-313 nM); inhibits NMDA-evoked currents and voltage-gated calcium channels in mouse primary striatal neurons (IC50s = 10 and 50 μM, respectively); inhibits glutamate-induced apoptosis in primary striatal neurons derived from the YAC128 transgenic mouse model of Huntington’s disease at 50 μM; inhibits cell death induced by amyloid-β (25-35) in cerebellar granule cells at 25 μM; inhibits decreases TWAA acquisition in a rat model of AF64A-induced Alzheimer’s disease at 1 mg/kg
Cayman Chemical GW 3965 hydrochloride
An orally-active agonist of LXRα and LXRβ, activating the human isoforms with EC50 values of 190 and 30 nM, respectively; alters LXR-regulated gene expression in mice and rats, affecting pathways related to glucose and lipid metabolism
Cayman Chemical FR122047 hydrochloride
A selective COX-1 inhibitor (IC50 = 0.028 µM for the human enzyme); selective for COX-1 over COX-2 (IC50 = 65 µM); inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation in human platelet-rich plasma (IC50 = 180-200 nM); unlike aspirin, it does not induce gastric damage at 100 mg/kg, p.o.; has an anti-inflammatory effect in a rat models of collagen-induced arthritis
Cayman Chemical DLthreoPDMP hydrochloride
An inhibitor of sphingolipid biosynthesis; inhibits glucosylceramide synthase by 33 and 48% in MDCK cell homogenates at 5 and 10 µM; reduces the synthesis of glucosylceramide increases cellular ceramide, and induces cell cycle arrest; increases Aβ42 and Aβ39 production independent of ceramide metabolism via modulation of γ-secretase activity
Cayman Chemical PIK75 hydrochloride
A selective inhibitor of p110α with an IC50 value of 5.8 nM; inhibits p110γ and p110β with IC50 values of 0.076 µM and 1.3 µM, respectively