DPTN dihydrochloride

SKU: orb1819121

Description

DPTN dihydrochloride is a potent and selective A3 adenosine receptor (A3AR) antagonist, exhibiting high affinity with Ki values of 1.65 nM (human), 9.61 nM (mouse), and 8.53 nM (rat). This compound is a valuable research tool for investigating the role of A3AR in various in vitro and in vivo models of inflammation, cancer, and ischemia-reperfusion injury.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 325767-87-1
• MW: 459.39
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₂₀Cl₂N₄OS
• SMILES: O=C(C1=CC=CN=C1)NC2=NC(C3=CC(C)=CC(C)=C3)=C(C4=CC=NC=C4)S2.Cl.Cl
• Target: Adenosine Receptor
• Solubility: DMSO:2.3 mg/mL (5.01 mM)

Bioactivity

• Target IC50:
  A3 (human):1.65 nM (Ki)
• In Vitro:
  DPTN dihydrochloride is a potent antagonist of human, mouse, and rat A3AR. However, compared with human A3AR, DPTN dihydrochloride has a weaker effect and reduced selectivity in mice and rats (approximately 20 times that of A2BAR). The binding affinity test of DNPT (10 μM) on the cell membrane of transfected HEK293 cells showed that its Ki values for hA1, hA2A, hA2B and hA3 were 162±49, 121±42, 230±40 and 1.65±0.57 nM respectively[ 1]. The Ki values of DPTN dihydrochloride at A1, A2A, A2B and A3 receptors are 411, 830, 189 and 9.61 nM (mouse); 333, 1147, 163 and 8.53 nM (rat) 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

A3A, AdenosineReceptor, Adenosine Receptor, DPTN, DPTN Dihydrochloride, DPTNdihydrochloride

Compound Identifiers

PubChem CID

168301117