A 438079

CAS No. 899507-36-9

A 438079( —— )

Catalog No. M26041 CAS No. 899507-36-9

A 438079 is a potent, and selective antagonist of P2X7 receptor (pIC50: 6.9).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 85 In Stock
2MG 39 In Stock
5MG 63 In Stock
10MG 93 In Stock
25MG 180 In Stock
50MG 291 In Stock
100MG 516 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    A 438079
  • Note
    Research use only, not for human use.
  • Brief Description
    A 438079 is a potent, and selective antagonist of P2X7 receptor (pIC50: 6.9).
  • Description
    A 438079 is a potent, and selective antagonist of P2X7 receptor (pIC50: 6.9).(In Vitro):A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM in 1321N1 cells stably expressing rat P2X7 receptors. A 438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM.(In Vivo):In neuropathic rats noxious and innocuous evoked activity of different classes of spinal neurons is reduced by A 438079 (80 μmol/kg, i.v.), and it significantly raises withdrawal thresh-olds in both the SNL and CCI models. A 438079 has superior neuroprotective effects compared with an equal dose of phenobarbital (25 mg/kg). A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A 438079 reduces nociceptive behavior scores in the HC model.
  • In Vitro
    In 1321N1 cells stably expressing rat P2X7?receptors, A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM. A 438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM.
  • In Vivo
    A 438079 (80 μmol/kg, i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats. A 438079 (100 and 300 μmol/kg, i.p.) significantly raises withdrawal thresh-olds in both the SNL and CCI models. Intraperitoneal injection of A 438079 (5 and 15 mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus. A 438079 has superior neuroprotective effects compared with an equally dose of phenobarbital (25 mg/kg).?A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    P2X Receptor
  • Recptor
    TRPM4
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    899507-36-9
  • Formula Weight
    306.15
  • Molecular Formula
    C13H9Cl2N5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (326.64 mM)
  • SMILES
    Clc1cccc(-c2nnnn2Cc2cccnc2)c1Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.9-Phenanthrol inhibits human TRPM4 but not TRPM5 cationic channels[J]. British Journal of Pharmacology, 2010, 153(8):1697-1705.
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