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Clobenpropit dihydrobromide

VUF 9153

A Potent and Selective Antagonist of Histamine H3 Receptors and an Antagonist of NMDA Receptors

Cat #: C-345
Alternative Name VUF 9153
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 470.65
    Purity: >99%
    Effective concentration 10 nM – 10 µM.
    Structure
    Chemical name 3-(1H-imidazol-5-yl)propyl N'-[(4-chlorophenyl)methyl]carbamimidothioate;dihydrobromide.
    Molecular formula C14H19Br2ClN4S.
    CAS No.: 145231-35-2
    PubChem CID 11213569
    Activity Clobenpropit dihydrobromide is a potent and selective antagonist/inverse agonist of the histamine H3 receptors (pA2 = 9.93), with partial agonist activity at histamine H4 receptors1. It is also an antagonist of the NMDA receptors (IC50 1 µM - 14 µM)2.
    References-Activity
    1. van der Goot, H. et al. (1992) Eur. J. Med. Chem. 27, 511.
    2. Hansen, K.B. et al. (2010) J. Pharmacol. Exp. Ther. 333, 650.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at +4°C.
    Solubility Up to 100 mM in water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to prepare solutions afresh on the day of use, or aliquot stock solutions stored at -20°C to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs Clobenpropit dihydrobromide inhibits NMDA receptor channels expressed in Xenopus oocytes.
      Alomone Labs Clobenpropit dihydrobromide inhibits NMDA receptor channels expressed in Xenopus oocytes.
      A. Representative time course of NR1/NR2A currents, elicited by transient stimulations with 100 µM glutamate + 100 µM glycine every 50 sec, while membrane potential was held at -80 mV, and reversibly inhibited by 5 µM Clobenpropit dihydrobromide (#C-345). B. Superimposed current traces from the recording shown in A, after application of control and 5 µM Clobenpropit dihydrobromide, as indicated. Transient stimulation is indicated by the arrow.
    References - Scientific background
    1. van der Goot, H. et al. (1992) Eur. J. Med. Chem. 27, 511.
    2. Black, S.A. et al. (2014) Front. Cell Dev. Biol. 2, 45.
    3. Hansen, K.B. et al. (2010) J. Pharmacol. Exp. Ther. 333, 650.
    Scientific background

    Clobenpropit dihydrobromide (VUF 9153) is a synthetic compound that acts as a potent, selective and competitive antagonist of the histamine H3 receptor and shows partial agonist activity towards the histamine H4 receptor. In addition, the compound acts as an antagonist of N-Methyl-d-aspartate (NMDA) receptors1 and displays IC50 values of 1 µM-14 µM2.

    NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. They play an important role in a variety of cellular processes and brain functions such as, synaptic plasticity, addiction and stroke, and mediate physiological functions such as learning and memory formation and participates in glutamate excitotoxicity2

    Histamine H3 receptors are presynaptic G-protein coupled receptors that are expressed in the central nervous system. They regulate the release of several neurotransmitters, including biogenic amines, acetylcholine, GABA and glutamate3.

    Target Histamine H3, Histamine H4, NMDA receptors
    Last update: 02/01/2022

    Clobenpropit dihydrobromide (#C-345) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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