2-Cl-IB-MECA

SKU: orb1226018

Description

2-Cl-IB-MECA (Chloro-IB-MECA, CF-102, Namodenoson) is a potent, selective A3 adenosine receptor agonist with Ki of 0.33 nM, 2500- and 1400-fold selectivity over A1 and A2a receptors; also displays 46,000-fold selectivity versus the Na(+)-independent adenosine transporter; inhibits adenylate cyclase via rat A3 receptors in CHO cells (IC50=67 nM); induces apoptosis in HL-60 cells at concentrations of <30 uM, significantly induced Ca(2+) release from intracellular Ca(2+) pools followed by Ca(2+) influx; increases plasma histamine concentrations in conscious rats.Liver Cancer Phase 2 Clinical(In Vitro):In human ADF cells of astroglial lineage, 100 nM Namodenoson (2-Cl-IB-MECA) caused a marked reorganization of the cytoskeleton, with appearance of stress fibres and numerous cell protrusions. High concentrations of Namodenoson (2-Cl-IB-MECA) directly cause influx of Ca2+.(In Vivo):Intravenous administration of 200 μg/kg Namodenoson (2-Cl-IB-MECA) resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations. Administration of a second dose of Namodenoson (2-Cl-IB-MECA) did not elicit any hemodynamic effects.

Key Properties

• CAS Number: 163042-96-4
• MW: 544.7308
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₈ClIN₆O₄
• SMILES: O[C@H]1[C@H](N2C=NC3=C(NCC4=CC=CC(I)=C4)N=C(Cl)N=C23)O[C@H](C(NC)=O)[C@H]1O
• Target: Adenosine Receptor
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• In Vivo:
  Intravenous administration of 200 μg/kg Namodenoson (2-Cl-IB-MECA) resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations. Administration of a second dose of Namodenoson (2-Cl-IB-MECA) did not elicit any hemodynamic effects.
• In Vitro:
  In human ADF cells of astroglial lineage, 100 nM Namodenoson (2-Cl-IB-MECA) caused a marked reorganization of the cytoskeleton, with appearance of stress fibres and numerous cell protrusions. High concentrations of Namodenoson (2-Cl-IB-MECA) directly cause influx of Ca2+.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cl-IB-MECA | CF-102 | Namodenoson

Quick Database Links

Gene Symbol

Adenosine Receptor