Histamine has been implicated in a variety of biological functions including thermo- and immunoregulation, food intake, hyperexcitability, pain transmission, arousal, reward, memory, and emotional responses. The histamine H3 receptor is a Gi-coupled presynaptic auto- and hetero-receptor whose activation leads to a decreased release of histamine, glutamate, norepinephrine, and acetylcholine in the brain. H3R antagonists are expected to increase the release of these neurotransmitters, which may contribute therapeutic benefit in diseases characterized by sleep/wake disturbances or cognitive disorders.{21996,21997} JNJ-5207852 is a selective, non-imidazole histamine H3R antagonist with high affinity at the rat (pKi = 8.9) and human (pKi = 9.24) H3 receptors.{21998} In rodents, 1-10 mg/kg JNJ-5207852 administered subcutaneously increases time spent awake and decreases REM sleep and slow-wave sleep.{21998}
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A selective, non-imidazole histamine H3R antagonist with high affinity at the rat (pKi = 8.9) and human (pKi = 9.24) H3 receptors
Formal name: 1-[3-[4-(1-piperidinylmethyl)phenoxy]propyl]-piperidine
Synonyms:
Molecular weight: 316.5
CAS: 398473-34-2
Purity: ≥98%
Formulation: A solution in ethanol
Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms
The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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