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Chemical Structure| 899431-18-6 Chemical Structure| 899431-18-6

Structure of A 438079 HCl
CAS No.: 899431-18-6

Chemical Structure| 899431-18-6

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A 438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).

Synonyms: A-438079 (hydrochloride); A 438079 hydrochloride

4.5 *For Research Use Only !

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Product Details of A 438079 HCl

CAS No. :899431-18-6
Formula : C13H10Cl3N5
M.W : 342.61
SMILES Code : ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1.[H]Cl
Synonyms :
A-438079 (hydrochloride); A 438079 hydrochloride
MDL No. :MFCD09971142
InChI Key :MBTJFFMIPPMRGR-UHFFFAOYSA-N
Pubchem ID :11688742

Safety of A 438079 HCl

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H228-H315-H319
Precautionary Statements:P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
Class:4.1
UN#:1325
Packing Group:

Isoform Comparison

Biological Activity

Target
  • P2X receptor

    P2X7, pIC50:6.9

In Vitro:

Cell Line
Concentration Treated Time Description References
ESdM cells 10 μM 1 hour To evaluate the effect of A 438079 on METH-induced microglial migration, results showed that A 438079 significantly reversed the METH-induced increase in migration. PMC4847215
Bone marrow-derived dendritic cells (BMDC) 1 μg/ml LPS 4 hours To investigate P2RX7-independent IL-1β release mechanisms. Results showed that BMDC produced significant IL-1β when stimulated with LPS, independent of P2RX7. PMC9322550

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Status epilepticus model Intracerebroventricular infusion 10 μM 2 weeks A-438079 infusion increased SE-induced neuronal death in the CA3 region PMC3123566
Rats Single Prolonged Stress (SPS) model Intracerebroventricular (ICV) infusion 3 μg/kg Once daily for 7 days Blocking P2X7Rs prevented the SPS-induced impaired fear extinction and extinction of cue-induced center avoidance in male and female rats PMC10106407
Lewis rats Collagen-induced arthritis (CIA) model Intrathecal administration 50 μg/day Once daily for 8 days To investigate the effects of A-438079 on mechanical hypersensitivity, spinal microgliosis, and IL-1β levels in CSF in CIA model rats. Results showed that A-438079 significantly attenuated mechanical allodynia, reduced spinal microgliosis, and prevented the increase of IL-1β. PMC4851814
Rats Transient global cerebral ischemia/reperfusion injury model induced by the four-vessel occlusion (4-VO) method Intracerebroventricular injection 3 μg Single injection, observed for 7 days after reperfusion To investigate the protective effects of A-438079 on transient global cerebral ischemia/reperfusion injury in rats. Results showed that A-438079 significantly increased survival rates, reduced neuronal death and DNA cleavage, and improved behavioral deficits. PMC3418181
Mice Cyclophosphamide-induced hemorrhagic cystitis model Intraperitoneal injection 50, 100, 200 mM/kg Two doses, first 30 min before cyclophosphamide, second 4 h after cyclophosphamide To evaluate the analgesic and anti-inflammatory effects of A 438079 on cyclophosphamide-induced hemorrhagic cystitis. Results showed that A 438079 significantly reduced nociceptive behavior scores, edema and hemorrhage indices induced by cyclophosphamide, and decreased c-Fos expression in the lumbar spinal cord and brain cortical areas, as well as reduced myeloperoxidase activity and macrophage migration in bladder tissue, and lowered tissue levels of IL-1β and TNF-α. PMC3252976
BALB/cJ mice Bone cancer pain model Subcutaneous injection 300 μmol/kg Single dose, 30 and 60 minutes duration Acute A-438079 treatment failed to alleviate bone cancer pain-related behaviours PMC6463294
rats nephrotoxic nephritis (NTN) model intraperitoneal injection 275 μmol/kg twice daily for 7 days To investigate the protective effects of A-438079 in the NTN model. Results showed that A-438079 significantly reduced proteinuria and haematuria in both WKY WT and P2RX7 KO rats, indicating its effects are mediated through non-P2RX7-dependent mechanisms. PMC9322550

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.92mL

0.58mL

0.29mL

14.59mL

2.92mL

1.46mL

29.19mL

5.84mL

2.92mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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