Human Sera
Cayman Chemical PAMAM DndrImR G6 0 ScInam 50mg
A negative allosteric modulator of mGluR5 binds to mGluR5 (Ki 35.6 nM) selective for mGluR5 over a panel of 116 additional receptors at 10 UM inhibits quisqualate-induced calcium mobilization and inositol phosphate accumulation in HEK293 cells expressing human mGluR5 (IC50s 7 and 5.9 nM respectively) reduces immobility time in the forced swim test in rats at 10 and 30 mg/kg has anxiolytic-like activity in rats inhibits surgical sciatic nerve constriction-induced cold allodynia in rats at 0.1-10 mg/kg increases the threshold of bladder filling volume to trigger the micturition reflex in anesthetized rats
Cayman Chemical CarbaethopendecInbromIde 100mg
An indole with diverse biological activities selectively inhibits BChE (IC50s 1.97 and 4.97 UM for the human and horse enzymes respectively) over AChE for which it has no activity an inhibitor of 5-HT3A and 5-HT3AB (IC50s 65.35 and 28.44 UM respectively) reduces glutamate-induced increases in cell death in HT22 cells at 50 and 100 UM induces apoptosis in A549 and H1299 NSCLC cells at 40 60 and 80 UM reduces tumor growth and intratumoral levels of phosphorylated GSK3B in an A549 mouse xenograft model at 10 mg/kg also reduces infarct size and cardiac cell apoptosis and prevents cardiac dysfunction in a rat model of ischemia-reperfusion injury at 20 mg/kg
Cayman Chemical EburnamonIn 100mg
An internal standard for the quantification of triptolide by GC- or LC-MS
Cayman Chemical RefametInIb 50mg
A stable cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions CFSE the intracellular cleavage product has ex/em 491/518 nm
Cayman Chemical Esomeprazole MagnsIum 50mg
A selective inhibitor of TGF-B and activin signaling that suppresses SMAD3 phosphorylation (IC50 3 UM) reduces TGF-B1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts
Cayman Chemical TaurolIthocholIc AcIdodIM 50mg
A guanine analog with antineoplastic activity irreversibly inactivates AGT with 40 reduction in alkyltransferase activity achieved at 0.06 UM with recombinant human AGT effective in vivo as well as in vitro
Cayman Chemical SB-271046hydrochlorIde 50mg
PGF2a methyl ester is an analog of PGF2a in which the C-1 carboxyl group has been esterified as the methyl ester. PGF2a methyl ester was one of the first PG esters shown to have ocular hypotensive activity.{8837} This compound continues to be a standard by which other ocular hypotensive PG prodrugs are evaluated. The methyl ester is about 4-5 times more potent than the free acid PGF2a. This difference is attributed to improved corneal penetration and a depot effect of prolonged retention of the ester form of the compound in ocular tissue. A 2.5 Ug dose of PGF2a-OMe applied to the eyes of cats results in a 6-8 mm Hg reduction in IOP.{8837}
Cayman Chemical BuformInhydrochlorIde 100mg
An antibiotic that inhibits DOXP reductoisomerase a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis against both Gram-negative and Gram-positive bacteria and the human malarial parasite P. falciparum (IC50 290-370 nM)
Cayman Chemical D-Mnoheptulose 50mg
An antiemetic and NK1 antagonist (Ki 3 nM IC50 0.09 nM for the human receptor) selective for NK1 over NK3 receptors (Ki 454.1 nM for human NK3) prevents substance P-induced plasma extravasation into the esophagus of guinea pigs at 1 mg/kg reduces NK1-agonist-induced foot tapping in gerbils
Cayman Chemical Galantamine 50mg
An inhibitor of PARPs which can be used in cells or in animals binds and inhibits the PARP TNKS1 (IC50 1 M) inhibits MMP-2 when used at higher concentrations (IC50 56 M)
Cayman Chemical ntalarmInhydrochlorIde 50mg
11b-PGE1 is an epimerized form of PGE1 at the C-11 position. 11b-PGE1 is a less potent isomer of PGE1. It is 13 and 3.6 as potent as PGE1 in contracting the rat uterus and guinea pig ileum respectively.{4158}
Cayman Chemical R S-natbIntartrate 50mg
A thiol-reactive fluorescent probe ex/em 384/513 nm respectively reacts with sulfite to form a fluorescent adduct with similar spectral characteristics and interference from sulfite during thiol determination must be accounted for using secondary methods has been used to monitor oxidative stability in beer
Cayman Chemical MItoxntronhydrochlorIde 50mg
A 77-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (Ki 0.561 nM) shows weaker affinity for EP receptors with Ki values of 100 nM for EP1-3 and 10 nM for EP4
Cayman Chemical MetoprololsuccInate 50mg
A potent selective and orally active inhibitor of human mPGES-1 (IC50 1.3 nM) potently inhibits guinea pig mPGES-1 (IC50 0.9 nM) but not mouse or rat mPGES-1 prevents LPS-induced pyresis hyperalgesia and iodoacetate-induced osteoarthritic pain
Cayman Chemical aPyroldInobutIothIophenon 50mg
A PI3KY inhibitor (IC50 0.025 UM in a binding assay) selective for PI3KY over PI3K PI3Ka and PI3KB (IC50s 7.9 10 and 1.26 UM respectively in binding assays) as well as a panel of 154 lipid and protein kinases inhibits C5a-induced phosphorylation of Akt in RAW 264.7 macrophages (IC50 1.2 UM) inhibits fMLP-induced migration of isolated human granulocytes (IC50 1 UM) decreases disease severity in a mouse model of collagen-induced arthritis at 3 and 10 mg/kg