Midaglizole hydrochloride

SKU: orb1709888

Description

Midaglizole hydrochloride (DG5128) is a selective α2-adrenoceptor antagonist with a 7.4-fold higher affinity for α2- versus α1-adrenoceptors (pKi = 6.28). It is utilized in pharmacological research to study adrenergic signaling in both in vitro binding assays and in vivo models of cardiovascular and sympathetic nervous system function.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 79689-25-1
• MW: 324.25
• Purity: >99.99% (May vary between batches)
• Formula: C₁₆H₁₉Cl₂N₃
• SMILES: C1(C(CC2=NCCN2)C3=CC=CC=C3)=NC=CC=C1.Cl.Cl
• Target: Adrenergic Receptor
• Solubility: DMSO:45 mg/mL (138.78 mM)

Bioactivity

• Target IC50:
  α2-adrenoceptor:6.28(pKi )
• In Vivo:
  Midaglizole (3 and 30 mg/kg, i.v.) elevates blood pressure in pithed rats.
• In Vitro:
  The inhibitory effect of midazolam (DG-5128) at a concentration of up to 10 μM in the cerebral cerebral membrane of [3H] clonidine is more effective than that of [3H] prazosin. The suppression method is uniform and conforms to the simple law of mass action. The EC50 values of midazolazole-induced insulin release in rat pancreatic islets and MIN6β cell lines were 200 nM and 24 μM, respectively. The IC50 values of midazolam for Kir6.2 and Kir6.2/SUR1 induced KATP current were 3.8 μM and 4.4 uM, respectively.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DG5128 hydrochloride, DG-5128 Hydrochloride, DG 5128 Hydrochloride, (±)-DG5128 hydrochloride, Adrenergic Receptor, AdrenergicReceptor, Midaglizole Hydrochloride, α2-adrenoceptor

Compound Identifiers

PubChem CID

157562