A839977 | CAS#870061-27-1 | P2X7R antagonist

A839977
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531368

CAS#: 870061-27-1

Description: 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

CAS# 870061-27-1

Instruction

Theoretical Analysis

MedKoo Cat#: 531368
Name: A839977
CAS#: 870061-27-1
Chemical Formula: C19H14Cl2N6O
Exact Mass: 412.06
Molecular Weight: 413.262
Elemental Analysis: C, 55.22; H, 3.41; Cl, 17.16; N, 20.34; O, 3.87

Price and Availability

Size	Price	Availability
5mg	USD 230	2 Weeks
10mg	USD 370	2 Weeks
25mg	USD 620	2 Weeks
50mg	USD 890	2 Weeks
100mg	USD 1295	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: A839977

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

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.

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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