An inhibitor of VMAT2 that is selective over VMAT1 (Kis = 97 and >20

Tetrabenazine – 100 mg

Brand:
Cayman
CAS:
58-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

Tetrabenazine is an inhibitor of vesicular monoamine transporter 2 (VMAT2) that is selective over VMAT1 (Kis = 97 and >20,000 nM, respectively, in a serotonin uptake assay).{26973} It dose-dependently reduces levels of the monoamines norepinephrine (Item No. 16673), dopamine (Item No. 21992), and serotonin (5-HT; Item No. 14332) in rat brain and has been used to induce depressive-like behavior in animal models.{47227,47228} Tetrabenazine (5 mg/kg) improves performance in balance beam and rotarod tests and prevents decreases in the number of striatal medium spiny neurons (MSNs) in a YAC128 transgenic mouse model of Huntington’s disease.{47229} Formulations containing tetrabenazine have been used in the treatment of chorea associated with Huntington’s disease.  

 

Available on backorder

Add to quotes
SKU: 20380 - Category:

Description

An inhibitor of VMAT2 that is selective over VMAT1 (Kis = 97 and >20,000 nM, respectively, in a serotonin uptake assay); dose-dependently reduces levels of the monoamines norepinephrine, dopamine, and 5-HT in rat brain; has been used to induce depressive-like behavior in animal models; improves performance in balance beam and rotarod tests and prevents decreases in the number of striatal MSNs in a YAC128 transgenic mouse model of Huntington’s disease at 5 mg/kg

Formal name: rel-1,3R,4,6,7,11bR-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-one

Synonyms:  NSC 169886|NSC 172187|Ro 1-9569|TBZ

Molecular weight: 317.4

CAS: 58-46-8

Purity: ≥98% (mixture of enantiomers)

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease||Research Area|Neuroscience|Neuroprotection

Related products

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

    Anhydrotetracycline (hydrochloride) – 100 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 - 100 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 – 10 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 - 10 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 – 500 µg

    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 - 500 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page