ARL 67156 trisodium salt

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ARL 67156 trisodium salt | CAS No. 1021868-83-6 | NTPDase Inhibitors
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Description: NTPDase inhibitor
Alternative Names: FPL 67156

Chemical Name: 6-N,N-Diethyl-D-β,γ-dibromomethyleneATP trisodium salt

Purity: ≥98%

Product Details
Citations (24)
Reviews

Biological Activity

ARL 67156 trisodium salt is a selective NTPDase inhibitor (pIC50 = 4.62 and 5.1 in human blood and rat vas deferens respectively). ARL 67156 prevents vascular calcification and extends longevity in Hutchinson-Gilford progeria syndrome mice. ARL 67156 increases neurogenic contract response to nerve stimulation. ARL 67156 enhances parasympathetic neurotransmission in guinea-pig urinary bladder.

Technical Data

M.Wt:
785.06
Formula:
C15H21Br2N5O12P3.3Na
Solubility:
Soluble to 20 mM in water
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1021868-83-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Autocrine Adenosine regulates tumor polyfunctional CD73+CD4+ effector T cells devoid of immune checkpoints
    N Gourdin, M Bossennec, C Rodriguez, S Vigano, C Machon, C Jandus, D Bauché, J Faget, I Durand, N Chopin, O Tredan, JC Marie, B Dubois, J Guitton, P Romero, C Caux, C Ménétrier-
    Cancer Res., 2018;0(0):.
  2. Hypoxia inducible factor HIF-1 promotes myeloid-derived suppressor cells accumulation through ENTPD2/CD39L1 in hepatocellular carcinoma
    DK Chiu, AP Tse, IM Xu, J Di Cui, RK Lai, LL Li, HY Koh, FH Tsang, LL Wei, CM Wong, IO Ng, CC Wong
    Nat Commun, 2017;8(1):517.
  3. CR1-mediated ATP release by human red blood cells promotes CR1 clustering and modulates the immune transfer process.
    Melhorn M, Brodsky A, Estanislau J, Khoory J, Illigens B, Hamachi I, Kurishita Y, Fraser A, Nicholson-Weller A, Dolmatova E, Duffy H, Ghiran I
    J Biol Chem, 2013;288(43):31139-53.
  4. Targeting Ornithine Decarboxylase by alpha-Difluoromethylornithine Inhibits Tumor Growth by Impairing Myeloid-Derived Suppressor Cells.
    Ye C, Geng Z, Dominguez D, Chen S, Fan J, Qin L, Long A, Zhang Y, Kuzel T, Zhang B
    J Immunol, 2016;196(2):915-23.
  5. Increased CD39 Nucleotidase Activity on Microparticles from Patients with Idiopathic Pulmonary Arterial Hypertension.
    Visovatti SH, Hyman MC, Bouis D
    PLoS ONE, 2012;7(7):e40829.
  6. Differential impact of adenosine nucleotides released by osteocytes on breast cancer growth and bone metastasis.
    Zhou J, Riquelme M, Gao X, Ellies L, Sun L, Jiang J
    Oncogene, 2015;34(14):1831-42.
  7. Pharmacological and biochemical analysis of FPL 67156, a novel, selective inhibitor of ecto-ATPase.
    Crack et al.
    Br.J.Pharmacol., 1995;114:475
  8. Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ecotnucleotidases.
    Levesque et al.
    Br.J.Pharmacol., 2007;152:141
  9. Release of soluble nucleotidases: a novel mechanism for neurotransmitter inactivation?
    Kennedy et al.
    TiPS, 1997;18:263
  10. The ecto-ATPase inhibitor ARL 67156 enhances parasympathetic neurotransmission in the guinea pig urinary bladder.
    Westfall et al.
    Eur.J.Pharmacol., 1997;329:169

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Citations for ARL 67156 trisodium salt

The citations listed below are publications that use Tocris products. Selected citations for ARL 67156 trisodium salt include:

24 Citations: Showing 1 - 10

  1. Blocking Antibodies Targeting the CD39/CD73 Immunosuppressive Pathway Unleash Immune Responses in Combination Cancer Therapies.
    Authors: Perrot Et al.
    Cell Rep  2019;27:2411
  2. ATP-based therapy prevents vascular calcification and extends longevity in a mouse model of Hutchinson-Gilford progeria syndrome.
    Authors: Villa-Bellosta
    Proc.Natl.Acad.Sci.U.S.A.  2019;116:23698
  3. Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
    Authors: Ng
    Cell Signal  2018;51:59
  4. Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
    Authors: Kleiner Et al.
    Mol Vis  2018;24:647
  5. Imaging extracellular ATP with a genetically-encoded, ratiometric fluorescent sensor.
    Authors: Conley
    PLoS One  2017;12(11):e0187481
  6. Expression of CD39 on activated T cells impairs their survival in older individuals.
    Authors: Fang Et al.
    Cell Rep.  2016;14:1218
  7. Endothelial cation channel PIEZO1 controls blood pressure by mediating flow-induced ATP release.
    Authors: Wang Et al.
    J Clin Invest  2016;126:4527
  8. A molecular signature in the pannexin1 intracellular loop confers channel activation by the α1 adrenoreceptor in smooth muscle cells.
    Authors: Billaud Et al.
    J Neuroimmune Pharmacol  2015;8:ra17
  9. Stimulation of Glia Reveals Modulation of Mammalian Spinal Motor Networks by Adenosine.
    Authors: Acton and Miles
    Sci Signal  2015;10:e0134488
  10. Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats.
    Authors: Ziemlinska Et al.
    PLoS One  2014;9:e88833
  11. Release of monocyte migration signals by breast cancer cell lines after ablative and fractionated γ-irradiation.
    Authors: Hennel Et al.
    Proc Natl Acad Sci U S A  2014;9:85
  12. Ligand-gated purinergic receptors regulate HIV-1 Tat and mor. related neurotoxicity in primary mouse striatal neuron-glia co-cultures.
    Authors: Sorrell and Hauser
    Radiat Oncol  2014;9:233
  13. Purines released from astrocytes inhibit excitatory synaptic transmission in the ventral horn of the spinal cord.
    Authors: Carlsen and Perrier
    Front Neural Circuits  2014;8:60
  14. Chemotherapeutic drugs induce ATP release via caspase-gated pannexin-1 channels and a caspase/pannexin-1-independent mechanism.
    Authors: Boyd-Tressler Et al.
    J Biol Chem  2014;289:27246
  15. Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium.
    Authors: Carneiro Et al.
    Br J Pharmacol  2014;171:3404
  16. P2Y6 receptor inhibition perturbs CCL2-evoked signalling in human monocytic and peripheral blood mononuclear cells.
    Authors: Campwala Et al.
    J Cell Sci  2014;127:4964
  17. Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
    Authors: Shabir Et al.
    PLoS One  2013;305:F396
  18. Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP.
    Authors: Ashpole Et al.
    J Biol Chem  2013;288:14599
  19. ABCC6 prevents ectopic mineralization seen in pseudoxanthoma elasticum by inducing cellular nucleotide release.
    Authors: Jansen Et al.
    Sci Rep  2013;110:20206
  20. Metabolism of circulating ADP in the bloodstream is mediated via integrated actions of soluble adenylate kinase-1 and NTPDase1/CD39 activities.
    Authors: Yegutkin Et al.
    FASEB J  2012;26:3875
  21. Glial-derived adenosine modulates spinal motor networks in mice.
    Authors: Witts Et al.
    J.Neurophysiol.  2012;107:1925
  22. Th1/Th17 cell induction and corresponding reduction in ATP consumption following vaccination with the novel Mycobacterium tuberculosis vaccine MVA85A.
    Authors: Griffiths Et al.
    PLoS One  2011;6:e23463
  23. ATP-dependent infra-slow (0.1 Hz) oscillations in thalamic networks.
    Authors: Lörincz Et al.
    PLoS One  2009;4:e4447
  24. Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder.
    Authors: Kennedy Et al.
    J Neurosci  2007;27:845

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