A 967079
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MedKoo CAT#: 558773

CAS#: 1170613-55-4

Description: A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. It has shown impressive efficacy, high selectivity, high potency, and oral bioavailability in attenuation of the noxious effects from TIH exposure. Systemic injection of A-967079 (30 micromol/kg, i.v.) decreased the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation of the ipsilateral hind paw in uninjured and CFA-inflamed rats, and reduced the responses of WDR neurons to high-intensity mechanical stimulation (300 g von Frey hair) of the knee joint in both OA and OA-sham rats.

Chemical Structure

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A 967079
CAS# 1170613-55-4
Instruction

Theoretical Analysis

MedKoo Cat#: 558773
Name: A 967079
CAS#: 1170613-55-4
Chemical Formula: C12H14FNO
Exact Mass: 207.11
Molecular Weight: 207.250
Elemental Analysis: C, 69.55; H, 6.81; F, 9.17; N, 6.76; O, 7.72

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
50mg USD 1350 2 Weeks
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Synonym: A967079, A-967079, (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-penten-3-one oxime

IUPAC/Chemical Name: (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime

InChi Key: HKROEBDHHKMNBZ-CHBKHGQFSA-N

InChi Code: 1S/C12H14FNO/c1-3-12(14-15)9(2)8-10-4-6-11(13)7-5-10/h4-8,15H,3H2,1-2H3/b9-8+,14-12+

SMILES Code: CCC(=N/O)\C(C)=C\C1=CC=C(F)C=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: >3 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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 207.25 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Gyamfi OA, Bortey-Sam N, Donkor AB, White CW, Logue BA. Analysis of TRPA1 antagonist, A-967079, in plasma using high-performance liquid chromatography tandem mass-spectrometry. J Pharm Anal. 2020 Apr;10(2):157-163. doi: 10.1016/j.jpha.2019.12.005. Epub 2019 Dec 13. PMID: 32373387; PMCID: PMC7192962.


2: Zhao J, Lin King JV, Paulsen CE, Cheng Y, Julius D. Irritant-evoked activation and calcium modulation of the TRPA1 receptor. Nature. 2020 Sep;585(7823):141-145. doi: 10.1038/s41586-020-2480-9. Epub 2020 Jul 8. PMID: 32641835; PMCID: PMC7483980.


3: Heber S, Gold-Binder M, Ciotu CI, Witek M, Ninidze N, Kress HG, Fischer MJM. A Human TRPA1-Specific Pain Model. J Neurosci. 2019 May 15;39(20):3845-3855. doi: 10.1523/JNEUROSCI.3048-18.2019. Epub 2019 Mar 12. PMID: 30862667; PMCID: PMC6520506.


4: Koivisto A, Chapman H, Jalava N, Korjamo T, Saarnilehto M, Lindstedt K, Pertovaara A. TRPA1: a transducer and amplifier of pain and inflammation. Basic Clin Pharmacol Toxicol. 2014 Jan;114(1):50-5. doi: 10.1111/bcpt.12138. Epub 2013 Oct 7. PMID: 24102997.


5: Heber S, Ciotu CI, Hartner G, Gold-Binder M, Ninidze N, Gleiss A, Kress HG, Fischer MJM. TRPV1 antagonist BCTC inhibits pH 6.0-induced pain in human skin. Pain. 2020 Jul;161(7):1532-1541. doi: 10.1097/j.pain.0000000000001848. PMID: 32107360.


6: He H, Zhao R, Hu K, Qiu L, Ding W, Li Y. A novel negative thermotaxis behavior in rice planthoppers is regulated by TRPA1 channel. Pest Manag Sci. 2020 Sep;76(9):3003-3011. doi: 10.1002/ps.5846. Epub 2020 Apr 27. PMID: 32248592.


7: Ton HT, Phan TX, Abramyan AM, Shi L, Ahern GP. Identification of a putative binding site critical for general anesthetic activation of TRPA1. Proc Natl Acad Sci U S A. 2017 Apr 4;114(14):3762-3767. doi: 10.1073/pnas.1618144114. Epub 2017 Mar 20. PMID: 28320952; PMCID: PMC5389314.


8: Zhu J, Zhang S, Geng Y, Song Y. Transient receptor potential ankyrin 1 protects against sepsis-induced kidney injury by modulating mitochondrial biogenesis and mitophagy. Am J Transl Res. 2018 Dec 15;10(12):4163-4172. PMID: 30662659; PMCID: PMC6325509.


9: Martínez-Rojas VA, García G, Noriega-Navarro R, Guzmán-Priego CG, Torres- López JE, Granados-Soto V, Murbartián J. Peripheral and spinal TRPA1 channels contribute to formalin-induced long-lasting mechanical hypersensitivity. J Pain Res. 2017 Dec 27;11:51-60. doi: 10.2147/JPR.S153671. PMID: 29343980; PMCID: PMC5749559.


10: Wang S, Zhai C, Zhang Y, Yu Y, Zhang Y, Ma L, Li S, Qiao Y. Cardamonin, a Novel Antagonist of hTRPA1 Cation Channel, Reveals Therapeutic Mechanism of Pathological Pain. Molecules. 2016 Aug 29;21(9):1145. doi: 10.3390/molecules21091145. PMID: 27589700; PMCID: PMC6274095.


11: Martínez-Rojas VA, Salinas-Abarca AB, Gómez-Víquez NL, Granados-Soto V, Mercado F, Murbartián J. Interaction of NHE1 and TRPA1 Activity in DRG Neurons Isolated from Adult Rats and its Role in Inflammatory Nociception. Neuroscience. 2021 Jun 15;465:154-165. doi: 10.1016/j.neuroscience.2021.04.025. Epub 2021 May 3. PMID: 33957206.


12: McGaraughty S, Chu KL, Perner RJ, Didomenico S, Kort ME, Kym PR. TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats. Mol Pain. 2010 Mar 5;6:14. doi: 10.1186/1744-8069-6-14. PMID: 20205719; PMCID: PMC2841076.


13: Dalenogare DP, Ritter C, Bellinaso FRA, Kudsi SQ, Pereira GC, Fialho MFP, Lückemeyer DD, Antoniazzi CTD, Landini L, Ferreira J, Bochi GV, Oliveira SM, De Logu F, Nassini R, Geppetti P, Trevisan G. Periorbital Nociception in a Progressive Multiple Sclerosis Mouse Model Is Dependent on TRPA1 Channel Activation. Pharmaceuticals (Basel). 2021 Aug 23;14(8):831. doi: 10.3390/ph14080831. PMID: 34451927; PMCID: PMC8400939.


14: Ritter C, Dalenogare DP, de Almeida AS, Pereira VL, Pereira GC, Fialho MFP, Lückemeyer DD, Antoniazzi CT, Kudsi SQ, Ferreira J, Oliveira SM, Trevisan G. Nociception in a Progressive Multiple Sclerosis Model in Mice Is Dependent on Spinal TRPA1 Channel Activation. Mol Neurobiol. 2020 May;57(5):2420-2435. doi: 10.1007/s12035-020-01891-9. Epub 2020 Feb 24. PMID: 32095993.


15: Zhai C, Liu Q, Zhang Y, Wang S, Zhang Y, Li S, Qiao Y. Identification of natural compound carnosol as a novel TRPA1 receptor agonist. Molecules. 2014 Nov 14;19(11):18733-46. doi: 10.3390/molecules191118733. PMID: 25405290; PMCID: PMC6271858.


16: Chen Z, Du S, Kong C, Zhang Z, Mokhtar AD. Intrathecal administration of TRPA1 antagonists attenuate cyclophosphamide-induced cystitis in rats with hyper-reflexia micturition. BMC Urol. 2016 Jun 17;16(1):33. doi: 10.1186/s12894-016-0150-x. PMID: 27315798; PMCID: PMC4912737.


17: Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, Segreti JA, Han P, Zhang XF, Niforatos W, Bianchi BR, Baker SJ, Zhong C, Simler GH, McDonald HA, Schmidt RG, McGaraughty SP, Chu KL, Faltynek CR, Kort ME, Reilly RM, Kym PR. Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation. Pain. 2011 May;152(5):1165-1172. doi: 10.1016/j.pain.2011.01.049. Epub 2011 Mar 12. PMID: 21402443.


18: Saarnilehto M, Chapman H, Savinko T, Lindstedt K, Lauerma AI, Koivisto A. Contact sensitizer 2,4-dinitrochlorobenzene is a highly potent human TRPA1 agonist. Allergy. 2014 Oct;69(10):1424-7. doi: 10.1111/all.12488. Epub 2014 Aug 22. PMID: 25041656.


19: Schwarz MG, Namer B, Reeh PW, Fischer MJM. TRPA1 and TRPV1 Antagonists Do Not Inhibit Human Acidosis-Induced Pain. J Pain. 2017 May;18(5):526-534. doi: 10.1016/j.jpain.2016.12.011. Epub 2017 Jan 3. PMID: 28062311.


20: Dalenogare DP, Theisen MC, Peres DS, Fialho MFP, Lückemeyer DD, Antoniazzi CTD, Kudsi SQ, Ferreira MA, Ritter CDS, Ferreira J, Oliveira SM, Trevisan G. TRPA1 activation mediates nociception behaviors in a mouse model of relapsing- remitting experimental autoimmune encephalomyelitis. Exp Neurol. 2020 Jun;328:113241. doi: 10.1016/j.expneurol.2020.113241. Epub 2020 Feb 8. PMID: 32045597.