A dopamine D1-like receptor antagonist (Kis = 1.9 and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors

LE300 – 1 mg

Brand:
Cayman
CAS:
274694-98-3
Storage:
-20
UN-No:
Non-Hazardous - /

LE300 is a dopamine D1-like receptor antagonist (Kis = 1.9 and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively) and antagonist of the serotonin (5-HT) receptor subtype 5-HT2A (pA2 = 8.32 in a rat tail artery assay).{45983,45984} It is selective for dopamine D1 and D5 over D2L and D4.4 receptors (Kis = 44.7 and 109 nM, respectively).{45983} LE300 inhibits the conditioned avoidance response in the pole-jump test in rats (ED50 = 0.94 mg/kg), which is predictive for antipsychotic-like activity.{45985} It also reduces locomotor activity in the open field test in rats (ED50 = 0.74 mg/kg).  

 

Available on backorder

Add to quotes
SKU: 29856 - 1 mg Category:

Description

A dopamine D1-like receptor antagonist (Kis = 1.9 and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively) and 5-HT2A receptor antagonist (pA2 = 8.32 in a rat tail artery assay); selective for dopamine D1 and D5 over D2L and D4.4 receptors (Kis = 44.7 and 109 nM, respectively); inhibits the conditioned avoidance response in the pole jump test in rats (ED50 = 0.94 mg/kg), which is predictive for antipsychotic-like activity; reduces locomotor activity in the open field test in rats (ED50 = 0.74 mg/kg)

Formal name: 6,7,8,9,14,15-hexahydro-7-methyl-5H-indolo[3,2-f][3]benzazecine

Synonyms: 

Molecular weight: 290.4

CAS: 274694-98-3

Purity: ≥98%

Formulation: A solid

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 500 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 500 mg

    Available on backorder

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

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 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 - 25 µg

    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