A histamine H3 receptor antagonist (Kis = 1.17 and 7.08 nM for human and rat receptors

JNJ-10181457 (hydrochloride) – 500 µg

Brand:
Cayman
CAS:
544707-20-2
Storage:
-20
UN-No:
Non-Hazardous - /

JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}  

 

Available on backorder

Add to quotes
SKU: 11997 - 500 µg Category:

Description

A histamine H3 receptor antagonist (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively); increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats at 10 mg/kg; reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans at 1.25-10 mg/kg; decreases the time spent in the open areas of the elevated zero maze in mice at 10 mg/kg, as well as increases locomotor activity in an open field test; inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.

Formal name: 4-[[3-[4-(1-piperidinyl)-1-butyn-1-yl]phenyl]methyl]-morpholine, dihydrochloride

Synonyms:  RWJ 662733

Molecular weight: 385.4

CAS: 544707-20-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

Related products

  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    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}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 µg

    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.  

     

    Brand:
    Cayman
    SKU:10009531 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page