A-438079 HCl

Catalog No.S7705

For research use only.

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

A-438079 HCl Chemical Structure

CAS No. 899431-18-6

Selleck's A-438079 HCl has been cited by 8 Publications

Purity & Quality Control

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Biological Activity

Description A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
Targets
P2X7 [1]
(in 1321N1 cells)
6.9(pIC50)
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.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells NH;1fpJHfW6ldHnvckBie3OjeR?= NWK0OVR5SW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiC{ZXPvcYJqdmGwdDDQNng4KHKnY3XweI9zKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBj\W68b4nsZoVvgm:rYzDBWHAucW6mdXPl[EBk[WylaYXtJJBzd2S3Y4Tpc44h[nliRlzJVHIh[XO|YYmsJGlEPTB;MD6xNlMxOyEQvF2= Mn7ZNlE2OzZ2M{W=
human 1321N1 cells MnO2SpVv[3Srb36gZZN{[Xl? Mnz0RY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBROlh5IILlZ4VxfG:{IHX4dJJme3OnZDDpckBpfW2jbjCxN|IyVjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk[WylaYXtJIZtfXhiYomgSmxKWFJuIFnDOVA:OC5zMkW4PUDPxE1? MmXHNVY4PTlzMEi=
human THP1 cells NVTX[2x{TnWwY4Tpc44h[XO|YYm= MV3BcpRi\2:waYP0JIFkfGm4aYT5JIF1KFB{WEegdoVk\XC2b4KgbY4hcHWvYX6gWGhROSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGJ7SVSSLXnu[JVk\WRiZYTobYRqfW1idYD0ZYtmNCCLQ{WwQVAvOTJ3OEmg{txO NX:zPFRIOTlzOUG1PFU>
HEK cells MYTGeY5kfGmxbjDhd5NigQ>? MYXBZ5Rqfmm2eTDheEBz[XRiUELYO{Bz\WOncITvdkBmgHC{ZYPz[YQhcW5iSFXLJINmdGy|IHHzd4V{e2WmIHHzJIVn\mWldDDvckBDgkGWUD3pcoR2[2WmIHX0bIllcXWvIIXweIFs\SxiSVO1NF0xNjNzNkKzJO69VQ>? MkLNNVkyQTF3OEW=
In vivo 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).[2] A-438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores.[3] Pretreatment with A-438079 reduces nociceptive behaviour scores in the HC model.[4] 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.[1]

Protocol (from reference)

Animal Research:[3]
  • Animal Models: Sprague-Dawley male rats
  • Dosages: 30 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30mg/mL

Chemical Information

Molecular Weight 342.61
Formula

C13H10Cl3N5

CAS No. 899431-18-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C(=C1)Cl)Cl)C2=NN=NN2CC3=CN=CC=C3.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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