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MedKoo Cat#: 531368 | Name: A839977
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

A839977 is a P2X7R antagonist in cancer-bearing animals where it attenuated dorsal horn neuronal responses in a modality and intensity-specific way. Spinal application of 0.4-mg/kg and 1.2-mg/kg A839977 significantly reduced the evoked responses to high-intensity mechanical and thermal stimulation, whereas no effect was seen in response to low-intensity or electrical stimulation. In awake animals, 40-mg/kg A839977 (i.p.) significantly reduced both early- and late-stage pain behavior.

Chemical Structure

A839977
A839977
CAS#870061-27-1

Theoretical Analysis

MedKoo Cat#: 531368

Name: A839977

CAS#: 870061-27-1

Chemical Formula: C19H14Cl2N6O

Exact Mass: 412.0606

Molecular Weight: 413.26

Elemental Analysis: C, 55.22; H, 3.41; Cl, 17.16; N, 20.34; O, 3.87

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
A839977; A-839977; A 839977;
IUPAC/Chemical Name
1-(2,3-dichlorophenyl)-N-{[2-(pyridin-2-yloxy)phenyl]methyl}-1H-1,2,3,4-tetrazol-5-amine
InChi Key
GMVNBKZQJFRFAR-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H14Cl2N6O/c20-14-7-5-8-15(18(14)21)27-19(24-25-26-27)23-12-13-6-1-2-9-16(13)28-17-10-3-4-11-22-17/h1-11H,12H2,(H,23,24,26)
SMILES Code
ClC1=C(Cl)C(N2N=NN=C2NCC3=CC=CC=C3OC4=NC=CC=C4)=CC=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 413.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Xu H, Wang M, Li Y, Shi M, Wang Z, Cao C, Hong Y, Hu B, Zhu H, Zhao Z, Chu X, Zhu F, Deng X, Wu J, Zhao F, Guo J, Wang Y, Pei G, Zhu F, Wang X, Yang J, Yao Y, Zeng R. Blocking connexin 43 and its promotion of ATP release from renal tubular epithelial cells ameliorates renal fibrosis. Cell Death Dis. 2022 May 31;13(5):511. doi: 10.1038/s41419-022-04910-w. PMID: 35641484; PMCID: PMC9156700. 2: Falk S, Schwab SD, Frøsig-Jørgensen M, Clausen RP, Dickenson AH, Heegaard AM. P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience. 2015 Apr 16;291:93-105. doi: 10.1016/j.neuroscience.2015.02.011. Epub 2015 Feb 14. PMID: 25686524. 3: Shao X, Guha S, Lu W, Campagno KE, Beckel JM, Mills JA, Yang W, Mitchell CH. Polarized Cytokine Release Triggered by P2X7 Receptor from Retinal Pigmented Epithelial Cells Dependent on Calcium Influx. Cells. 2020 Nov 24;9(12):2537. doi: 10.3390/cells9122537. PMID: 33255431; PMCID: PMC7760537. 4: Albalawi F, Lu W, Beckel JM, Lim JC, McCaughey SA, Mitchell CH. The P2X7 Receptor Primes IL-1β and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain. Front Cell Neurosci. 2017 Aug 8;11:227. doi: 10.3389/fncel.2017.00227. PMID: 28848393; PMCID: PMC5550720. 5: Liu JP, Liu SC, Hu SQ, Lu JF, Wu CL, Hu DX, Zhang WJ. ATP ion channel P2X purinergic receptors in inflammation response. Biomed Pharmacother. 2023 Feb;158:114205. doi: 10.1016/j.biopha.2022.114205. Epub 2023 Jan 4. PMID: 36916431. 6: Nurkhametova D, Siniavin A, Streltsova M, Kudryavtsev D, Kudryavtsev I, Giniatullina R, Tsetlin V, Malm T, Giniatullin R. Does Cholinergic Stimulation Affect the P2X7 Receptor-Mediated Dye Uptake in Mast Cells and Macrophages? Front Cell Neurosci. 2020 Oct 28;14:548376. doi: 10.3389/fncel.2020.548376. PMID: 33328886; PMCID: PMC7673375. 7: Gangadharan V, Nohe A, Caplan J, Czymmek K, Duncan RL. Caveolin-1 regulates P2X7 receptor signaling in osteoblasts. Am J Physiol Cell Physiol. 2015 Jan 1;308(1):C41-50. doi: 10.1152/ajpcell.00037.2014. Epub 2014 Oct 15. PMID: 25318104; PMCID: PMC4281673. 8: Nurkhametova D, Kudryavtsev I, Guselnikova V, Serebryakova M, Giniatullina RR, Wojciechowski S, Tore F, Rizvanov A, Koistinaho J, Malm T, Giniatullin R. Activation of P2X7 Receptors in Peritoneal and Meningeal Mast Cells Detected by Uptake of Organic Dyes: Possible Purinergic Triggers of Neuroinflammation in Meninges. Front Cell Neurosci. 2019 Feb 13;13:45. doi: 10.3389/fncel.2019.00045. PMID: 30814932; PMCID: PMC6381076. 9: Lu W, Albalawi F, Beckel JM, Lim JC, Laties AM, Mitchell CH. The P2X7 receptor links mechanical strain to cytokine IL-6 up-regulation and release in neurons and astrocytes. J Neurochem. 2017 May;141(3):436-448. doi: 10.1111/jnc.13998. PMID: 28244110; PMCID: PMC5408351. 10: Campagno KE, Lu W, Jassim AH, Albalawi F, Cenaj A, Tso HY, Clark SP, Sripinun P, Gómez NM, Mitchell CH. Rapid morphologic changes to microglial cells and upregulation of mixed microglial activation state markers induced by P2X7 receptor stimulation and increased intraocular pressure. J Neuroinflammation. 2021 Sep 20;18(1):217. doi: 10.1186/s12974-021-02251-7. PMID: 34544431; PMCID: PMC8454080. 11: Honore P, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81. doi: 10.1016/j.bbr.2009.05.018. Epub 2009 May 21. PMID: 19464323.