119149

ZM 241385

A highly potent, selective, non-xanthine adenosine A2A receptor antagonist (K_i = 800 pM for human adenosine A2AR stably expressed in HEK-293 cells).

• Synonym(s): Adenosine A2A Receptor Antagonist I, ZM 241385
• Empirical Formula (Hill Notation): C₁₆H₁₅N₇O₂
• CAS Number: 139180-30-6
• Molecular Weight: 337.34
• MDL number: MFCD00908394
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Product Name: Adenosine A2A Receptor Antagonist I, ZM 241385, A highly potent, selective, non-xanthine adenosine A2A receptor antagonist (K_i = 800 pM for human adenosine A2AR stably expressed in HEK-293 cells).
• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• potency: 800 pM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 15 mg/mL
• application(s): air monitoring
• compatibility: for use with Viable Air Samplers (1.09191); for use with Viable Air Samplers (1.09194); for use with Viable Air Samplers (1.17103); for use with Viable Air Samplers (1.17274); for use with Viable Air Samplers (1.17275)
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [n]21nc(nc2nc(nc1N)NCCc4ccc(cc4)O)c3[o]ccc3
• InChI: 1S/C16H15N7O2/c17-14-20-15(18-8-7-10-3-5-11(24)6-4-10)21-16-19-13(22-23(14)16)12-2-1-9-25-12/h1-6,9,24H,7-8H2,(H3,17,18,19,20,21,22)
• InChI key: PWTBZOIUWZOPFT-UHFFFAOYSA-N

Description

General description

A highly potent, selective, and orally bioavailable non-xanthine adenosine A_2A receptor antagonist (K_i = 800 pM for human adenosine A_2AR stably expressed in HEK-293 cells). Does not exhibit any significant antagonistic activity in A₁, A_2B (K_i = 255 nM and 50 nM, respectively in human adenosine receptors stably expressed in CHO cells) or in A₃R (K_i >10 µM in human A₃R stably expressed in HEK-293 cells). Shown to have a protective effect against beta-amyloid peptide toxicity.

A highly potent, selective, non-xanthine adenosine A2A receptor antagonist (K_i = 800 pM for human adenosine A2AR stably expressed in HEK-293 cells).

Biochem/physiol Actions

Primary Target
A2A

Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Poucher, S. M., et al. 1995. Brit. J. Pharmacol. 115, 1096.
Ongini, E. et al. 1999. Naunyn Schmiedebergs Arch Pharmacol. 359, 7.

Keddie, J. et al. 1996, Eur Journ Pharm. 301, 107.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable