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Cat. No. Product Name Field of Application Chemical Structure
DC33252 PBOX-6
PBOX-6 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-drug resistance (IC50 = 2.28 μM/HL60-MDR1, 2.86 μM/HL60-BCG2, 1.91 μM/HL60; IC50 = 4.71 μM/A2780-ADR, 4.10 μM/A2780). PBOX-6 inhibits the assembly of purified tubulin in cell-free assays and causes microtubule depolymerization in MCF-7 cells by binding a tubulin site distinct from those targeted by vinblastine and colchicine. When administered via intratumoral injection (7.5 mg/kg/day) in vivo, PBOX-6 is reported to significantly inhibit tumour growth in a murine model of neuroblastoma and a CML model of the imatinib-resistant T315I mutants.
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DC33251 PD-85639
PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).
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DC33250 AC-186
AC-186 is reported as a selective nonsteroidal estrogen receptor agonist.
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DC33248 PF-04279405
PF-04279405 is a potent and selective glucokinase activator.
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DC33247 PF-04445597
PF-04445597 is a potent, orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP).
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DC33246 PF-04671536
PF-04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A). In primary human pancreatic islets, PF-04671536 increases insulin secretion in a glucose-dependent manner.
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DC33245 PF-04753299
PF-04753299 is a potent and selective inhibitor of LpxC (UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase) that is effective in a murine of gram-negative bacteria infection model.
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DC33244 PF-05236216 hydrochloride
PF-05236216 hydrochloride is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta/epsilon (CK1δ/ε) that modulates circadian rhythms in mice.
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DC33243 PF-06284674
PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.
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DC33242 PF-06422913
PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
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DC33241 PF-06456384 trihydrochloride
PF-06456384 trihydrochloride is a highly potent and selective inhibitor against voltage-gated sodium channel NaV1.7 (SCN9A; IC50 = 0.01, <0.1, 75 nM against human, mouse, rat Nav1.7, respectively, by conventional patch clamp; human Nav1.7 IC50 = 0.58 nM by PatchExpress electrophysiology) with >300-fold selectivity over other human NaVs (IC50 = 3 nM/NaV1.2, 5.8 nM/NaV1.6, 75 nM/NaV1.7, 314 nM/NaV1.1, 1.45 μM/NaV1.4, 2.59 μM/NaV1.5, 6.44 μM/NaV1.3, 26 μM/NaV1.8).
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DC33240 PF-06463922 acetate
PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
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DC33239 PF-06663195
PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1).
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DC33237 PF-06745268
PF-06745268 is an orally available, brain penetrant, potent and selective γ-secretase modulator. PF-06745268 induces robust and sustained reduction of brain amyloid-β42 (Aβ42) in rats.
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DC33236 PF-06748962
PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.
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DC33235 PF-3774076
PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.
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DC33234 PF-4800567 hydrochloride
PF-4800567 hydrochloride is a casein kinase 1e (CK1e) selective inhibitor (IC50 = 32 nM) that is 20 fold selective for the CK1e isoform over CK1d. PF-4800567 blockes CK1e-mediated PER3 nuclear translocation, but does not effect the circadian clock in animal studies.
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DC33233 PF-5081090
PF-5081090 is a potent inhibitor of LpxC, a metalloenzyme required for the synthesis of lipid A, an essential component of the outer membrane of Gram-negative bacteria. The IC50 for enzyme inhibition is 1.1 nM and the minimal inhibitory concentration (MIC) for inhibiting growth of Pseudomonas aeruginosa growth is 0.008 mg/mL.
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DC33232 PF-514273
PF-514273 is a highly selective CB1 antagonist. The Ki for binding to CB1 and CB2 receptors is 1 nM and 10 mM, respectively. PF-514273 inhibits food intake and weight gain in rodents.
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DC33230 PHA 767491 hydrochloride
PHA 767491 hydrochloride is a potent and selective ATP-competitive dual inhibitor cdc7/cdk9. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites.
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DC33229 Phenazepam
Phenazepam is the benzodiazepine that exhibit anticonvulsive, anxiolytic, sedative and hypnotic effects in humans and experimental animals. Phenazepam is an agonist of the γ-Aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.
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DC33228 Nitrophenide
Nitrophenide is a bioactive chemical.
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DC33224 Aklomide
Aklomide is a Coccidiostat (for Poultry).
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DC33223 Tramiprosate
Tramiprosate, also known as homotaurine, is a gamma-Aminobutyric acid (GABA) receptor agonist and a glycosaminoglycan mimetic used in the treatment of Alzheimer's disease.
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DC33220 Pramoxine
Pramoxine, also known as Pramocaine, is a topical anesthetic. Pramoxine decreases the permeability of the neuronal membrane to sodium ions by reversibly binding to and inhibiting voltage-gated sodium channels. This results in stabilization of the membrane and, thereby inhibiting the ionic fluxes required for membrane depolarization, hence resulting in the failure to initiate a propagated action potential and subsequent conduction blockade.
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DC33219 Phthalylsulfathiazole
Phthalylsulfathiazole is a broad spectrum antimicrobial agent. Phthalylsulfathiazole is used in the treatment of dysentery, colitis, and gastroenteritis.
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DC33218 Phenoxybenzamine hydrochloride
Phenoxybenzamine hydrochloride is an α-1 adrenergic receptor antagonist used to treat hypertension and as a peripheral vasodilator. Phenoxybenzamine reduced neuronal death in rat hippocampal slice cultures following exposure to oxygen glucose deprivation. Phenoxybenzamine treated TBI (traumatic brain injury) animals also showed a significant improvement in both learning and memory compared to saline treated controls. At 32 h post-TBI phenoxybenzamine treated animals had significantly lower expression of pro-inflammatory signaling proteins CCL2, IL1β, and MyD88, suggesting that phenoxybenzamine may exert a neuroprotective effect by reducing neuroinflammation after TBI.
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DC33217 Paromomycin Sulfate
Paromomycin sulfate is an aminoglycoside antimicrobial agent derived from Streptomyces sp. AG-P 1441. Paromomycin likely induced resistance as confirmed by the expression of pathogenesis-related genes: PR-1, β-1,3-glucanase, chitinase, PR-4, peroxidase, and PR-10, which enhanced plant defense against P. capsici in chili pepper.
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DC33216 Isoxsuprine
Isoxsuprine is a beta 2-adrenergic agonist and NR2B subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonist used for the treatment of pre-term labor and dysmenorrhea. Isoxsuprine affects the vascular smooth muscle and results in peripheral vascular dilation. Isoxsuprine also relaxes the uterine smooth muscles. Isoxsuprine elevated the blood flow volume in the umbilical arteries. Veterinary treatment of cows with isoxsuprine may temporarily lead to low levels of isoxsuprine in the hair of their newborn calves, which promotes growth.
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DC33215 Iodoquinol
Iodoquinol is one of the halogenated 8-quinolinols that's widely used as an intestinal antiseptic, especially as an antiamebic agent. Iodoquinol is also used topically in other infections and may cause central nervous system and eye damage.
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