UN2811, 5 g, Cayman Chemical
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5-Fluorouracil
Cayman ChemicalA pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.
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6-Thioguanine
Cayman ChemicalA thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.
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Ketoconazole
Cayman ChemicalAn orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC50 = 63.5 nM), as well as a variety of other CYP isoforms.
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Amlodipine
Cayman ChemicalA dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC50 = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and…
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Nicardipine (hydrochloride)
Cayman ChemicalA dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…
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Carprofen
Cayman ChemicalAn NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC50s = 22.3 and 3.9 µM, respectively) and also FAAH (IC50 = 74 µM).
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Doxepin (hydrochloride)
Cayman ChemicalA tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.
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Bupivacaine
Cayman ChemicalAn amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.
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Vitamin D2
Cayman ChemicalProduced in fungi, including yeast, and invertebrates from ergosterol in response to ultraviolet radiation; metabolized first to 25-hydroxyvitamin D2 and subsequently to the active 1,25-dihydroxyvitamin D2.
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Xylazine
Cayman ChemicalAn agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.
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Quinacrine (hydrochloride hydrate)
Cayman ChemicalAn anti-protozoal agent; prevents misfolding of prion protein (EC50 = 0.3 μM), blocks voltage-dependent sodium channels (IC50 = 3.3 μM), inhibits aldehyde oxidase (IC50 = 3.3 μM), antagonizes the riboflavin-binding protein (Ki = 6.7 μM), inhibits…
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Tenoxicam
Cayman ChemicalAn NSAID that acts as a COX-2 inhibitor (IC50s = 20 and 322 nM for COX-1 and COX-2, respectively).
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Primaquine (phosphate)
Cayman ChemicalAn antimalarial drug used in the treatment of persistent liver forms of P. vivax or P. ovale infection for its ability to kill late-stage gametocytes and hypnozoites.
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Chlorpromazine (hydrochloride)
Cayman ChemicalA phenothiazine classified as an antipsychotic compound; antagonizes dopamine and serotonin receptors (Kis = 0.66, 0.84, 1.2, and 1.8 nM for D2, D3, D4, and 5-HT2A, respectively); also antagonizes histamine, α1- and α2-adrenergic, and muscarinic acetylcholine receptors.
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Clonidine (hydrochloride)
Cayman ChemicalA centrally acting α2-adrenergic receptor agonist that decreases peripheral vascular resistance by centrally inhibiting sympathetic nerve activity; also acts as an agonist of the imidazoline (I1) receptor (Ki = 4-8 nM).
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Benzbromarone
Cayman ChemicalAn inhibitor of URAT1 (IC50 = 0.3 µM for hURAT1) that prevents renal urate resorption; also potently inhibits CYP2C9 (Ki = 20 nM) and has been used to study adverse drug-drug interactions.
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(±)-Baclofen
Cayman ChemicalA selective agonist of GABAB (IC50 = 200 nM); causes skeletal muscle relaxation and blocks spasticity.
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Benztropine (mesylate)
Cayman ChemicalA centrally acting M1 muscarinic acetylcholine receptor antagonist (Ki = 0.59 nM in rat) that also inhibits dopamine uptake through the dopamine transporter (Ki = 160 nM); used in the management of Parkinson’s disease symptoms to address involuntary tremor and dystonia.
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(-)-Epinephrine
Cayman ChemicalA natural neurotransmitter that is activates adrenoceptors (Kis = 15, 735, and 3,970 nM for α1A-, β2-, and β1-adrenergic receptors, respectively); may induce either contraction or relaxation of vascular smooth muscle, depending on adrenoceptor subtype expression.
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5-Chlororesorcinol dimethyl ether
Cayman Chemical5-Chloroesorcinol dimethyl ether is a synthetic intermediate useful for pharmaceutical synthesis.
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Verapamil (hydrochloride)
Cayman ChemicalThe prototypical blocker of L-type calcium channels that produces excitation-contraction uncoupling in cardiac muscle by preventing the slow-inward current of Ca2+ (IC50 = 0.38 μM in guinea pig aortic strip).
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Carbamoylcholine (chloride)
Cayman ChemicalAn agonist of both nAChR and mAChR receptors, with reported Ki values ranging from 10 to 10,000 nM for different receptors and different preparations; used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.
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Colistin (sulfate)
Cayman ChemicalA polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.
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Vitamin D3
Cayman ChemicalAn intermediate form of vitamin D which is obtained from dietary sources, such as fish, or through the conversion of 7-dehydrocholesterol by ultraviolet light; metabolized to the active form 1,25-dihydroxyvitamin D3 by CYP450 isoforms in the liver.
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3-Nitropropionic Acid
Cayman ChemicalAn irreversible inhibitor of mitochondrial Complex II succinate dehydrogenase, resulting in energy depletion through disruption of the electron transport chain; used in animal models of Huntington’s disease and epilepsy.