Cayman Chemical

A positively charged sulfhydryl-specific reagent that reacts with substituted-cysteines; used to provide functional information about relative positions of amino acids within a protein and to probe binding site electrostatic interactions.

A selective TRPV1 antagonist widely used in pain research; inhibits capsaicin-evoked Ca2+ influx with an IC50 value of 0.7 μM in cultured trigeminal ganglion neurons; reduces capsaisin-induced nociceptive responses in a model of pain and suppresses tolerance to the analgesic effects of chronic...

A BH3 mimetic that selectively inhibits Bcl-2 (Ki 3-fold less avidly to the related family proteins, Bcl-xL and Bcl-W (Kis = 48 and 245 nM, respectively); inhibits the growth of Bcl-2-dependent cell lines and in vivo tumor xenografts and demonstrates antileukemic activity in patients with refractory...

An indoleacetamide that acts as a high affinity TSPO agonist (Ki = 5 nM); enhances steroidogenesis of neuroactive steroids, thus potentiating GABAA receptor signaling to produce anticonvulsant, anxiolytic, and sedative activity in both animal and clinical models.

A unique LT with weak contractile activity on both guinea pig ileum and pulmonary parenchyma compared to 5-LO-derived LTs; increases vascular permeability of human endothelial cell monolayers with similar potency to that of 5-LO-derived LTs.

A cell- and brain-permeable inhibitor of SIRT2 (IC₅₀ = 15.5 μM); dimishes neuronal cell death induced by mutant huntingtin fragment in culture; down-regulates cholesterol biosynthetic gene expression and reduces total cholesterol levels in neurons in vivo.

U-46619 is a TP receptor agonist that exhibits properties similar to TXA2, inducing platelet aggregation and vascular smooth muscle contraction. 5-trans U-46619 is a minor impurity (2-5%) which is variably present in most commercial preparations of U-46619. The biological activity of 5-trans U-46619...

A hydrolyzable tannin with phytotoxic activity.

A selective GABA_B receptor antagonist.

IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor that demonstrates IC₅₀ values of 59 and 12 nM for human IDO enzymatic activity and HeLa cell assays, respectively. It is inactive against tryptophan 2,3-dioxygenase (TOD; IC₅₀ > 10 µM).

A reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells.

L-NIO is a non-selective inhibitor of all NOS isoforms. The Ki values for nNOS (rat), eNOS (bovine), and iNOS (mouse) are 1.7, 3.9, and 3.9 µM, respectively.

Intended to be used as a building block in drug discovery chemistry.

A potent, selective antagonist of the serotonin (5-HT) receptor 5-HT3 (pKi = 10.4 in rat cortex); orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs; remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life.

An internal standard for the quantification of LTB4 by GC- or LC-MS.

An antagonist of the CCR5 receptor, inhibiting binding of the ligand RANTES with an IC₅₀ value of 1.4 nM; inhibits HIV-1 replication in CCR5-expressing cells (IC₅₀ = 2.8 nM).

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

An antiemetic compound that selectively antagonizes the human NK1 receptor (Kis = 3 and 454.1 nM for hNK1 and hNK3, respectively; IC₅₀ = 0.09 nM for hNK1).

Cloprostenol (sodium salt) is a more water solute, crystalline form of cloprostenol than the free acid.

A natural demethoxy derivative of curcumin; suppresses proliferation in cancer cells at 50-100 μM; down-regulates p300 and inhibits LPS-induced iNOS expression.

A degradation product of tryptophan upon exposure to visible light that activates the AhR (Kd = 70 pM) and is a substrate for CYP1A1, CYP1A2, and CYP1B1 (Kis = 15.4, 3.9, and 13.3 µM, respectively); used to study the immunomodulatory and host defense mechanisms of AhR signaling pathways.

A 33 amino acid hypothalamic neuropeptide with a role in appetite regulation, wakefulness, locomotor activity, sympathetic and HPA activity, and pain thresholds; binds the orexin-1 and -2 receptors with equal affinity.

An enantiomer of the short-lived oral anti-coagulant acenocoumarol with a longer plasma elimination half-life (6.6 hours) and slower plasma clearance (1.9 L/hour), compared to the (S)-enantiomer (1.8 hours, 28.5 L/hour); rapidly absorbed from the gastrointestinal tract with essentially complete oral...