Cat. No. | Product Name | Field of Application | Chemical Structure |
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DC33259 | AH13205 |
AH13205 is an EP2 prostanoid receptor agonist.
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DC33258 | AGN193109 |
AGN193109 is a retinoic acid receptor (RAR) antagonist.
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DC33257 | AFDX384 |
AFDX384 is potent M2/M4 selective antagonist.
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DC33256 | ACT-462206 |
ACT-462206 is an orally active, potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.
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DC33255 | p38 MAP Kinase Inhibitor IV |
p38 MAP Kinase Inhibitor IV is an ATP-competitive inhibitor of p38α/β MAPK with IC50 values of 130 nM for p38α and 550 nM for p38β. It is much less active with ≤23% inhibition at 1 μM against p38γ/σ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203580 in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM inhibitor). A recent study showed that p38 MAP Kinase Inhibitor IV could consistently and significantly enhance reprogramming and iPS cell generation from somatic cells.
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DC33254 | AC-90179 |
AC-90179 is a high selective 5-hydroxytryptamine2A receptor inverse agonist. It is an atypical antipsychotic pharmaceutical. It has been shown to alleviate hallucinogen-induced vasocontriction and possible other harmful physical symptoms.
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DC33253 | Panepoxydone |
Panepoxydone is a fungal metabolite that inhibits NF-κB transcription factor by preventing IκB phosphorylation, thus inhibiting the release of NF-κB from the IκB : NF-κB complex and its translocation into the nucleus. Panepoxydone also has antimalarial, cytotoxic activities and anti-parasitic activity against Trypanosoma cruzi.
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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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