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Submit ReviewARL 67156 trisodium salt
Description: NTPDase inhibitor
Alternative Names: FPL 67156
Chemical Name: 6-N,N-Diethyl-D-β,γ-dibromomethyleneATP trisodium salt
Purity: ≥98% (HPLC)
Biological Activity for ARL 67156 trisodium salt
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 for ARL 67156 trisodium salt
| M. Wt | 785.06 |
| Formula | C15H21Br2N5O12P3.3Na |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1021868-83-6 |
| PubChem ID | 52948496 |
| InChI Key | KJYSFRKUFDOOSQ-ZANJJFDZSA-K |
| Smiles | O[C@H]3[C@H](O)[C@@H](O[C@@H]3COP(OP(C(Br)(Br)P(O)(O[Na])=O)(O[Na])=O)(O[Na])=O)N1C=NC2=C1N=CN=C2N(CC)CC |
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.
Solubility Data for ARL 67156 trisodium salt
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 15.78 | 20 |
Preparing Stock Solutions for ARL 67156 trisodium salt
The following data is based on the product molecular weight 785.06. 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 |
|---|---|---|---|
| 0.2 mM | 6.37 mL | 31.84 mL | 63.69 mL |
| 1 mM | 1.27 mL | 6.37 mL | 12.74 mL |
| 2 mM | 0.64 mL | 3.18 mL | 6.37 mL |
| 10 mM | 0.13 mL | 0.64 mL | 1.27 mL |
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Product Datasheets for ARL 67156 trisodium salt
References for ARL 67156 trisodium salt
References are publications that support the biological activity of the product.
Crack et al (1995) Pharmacological and biochemical analysis of FPL 67156, a novel, selective inhibitor of ecto-ATPase. Br.J.Pharmacol. 114 475 PMID: 7533620
Kennedy et al (1997) Release of soluble nucleotidases: a novel mechanism for neurotransmitter inactivation? TiPS 18 263 PMID: 9277128
Levesque et al (2007) Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ecotnucleotidases. Br.J.Pharmacol. 152 141 PMID: 17603550
Westfall et al (1997) The ecto-ATPase inhibitor ARL 67156 enhances parasympathetic neurotransmission in the guinea pig urinary bladder. Eur.J.Pharmacol. 329 169 PMID: 9226410
Villa-Bellosta (2019) ATP-based therapy prevents vascular calcification and extends longevity in a mouse model of Hutchinson-Gilford progeria syndrome. Proc.Natl.Acad.Sci.U.S.A. 116 23698 PMID: 31690656
If you know of a relevant reference for ARL 67156 trisodium salt, please let us know.
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Keywords: ARL 67156 trisodium salt, ARL 67156 trisodium salt supplier, Ecto-ATPase, inhibitors, inhibits, ARL67156, trisodium, salt, FPL67156, NTPDase, neurotransmission, progeria, FPL, 67156, 1283, Tocris Bioscience
24 Citations for ARL 67156 trisodium salt
Citations are publications that use Tocris products. Selected citations for ARL 67156 trisodium salt include:
Conley (2017) Imaging extracellular ATP with a genetically-encoded, ratiometric fluorescent sensor. PLoS One 12 e0187481 PMID: 29121644
Acton and Miles (2015) Stimulation of Glia Reveals Modulation of Mammalian Spinal Motor Networks by Adenosine. Sci Signal 10 e0134488 PMID: 26252389
Hennel et al (2014) Release of monocyte migration signals by breast cancer cell lines after ablative and fractionated γ-irradiation. Proc Natl Acad Sci U S A 9 85 PMID: 24666643
Ashpole et al (2013) Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP. J Biol Chem 288 14599 PMID: 23543737
Lörincz et al (2009) ATP-dependent infra-slow (0.1 Hz) oscillations in thalamic networks. PLoS One 4 e4447 PMID: 19212445
Perrot et al (2019) Blocking Antibodies Targeting the CD39/CD73 Immunosuppressive Pathway Unleash Immune Responses in Combination Cancer Therapies. Cell Rep 27 2411 PMID: 31116985
Wang et al (2016) Endothelial cation channel PIEZO1 controls blood pressure by mediating flow-induced ATP release. J Clin Invest 126 4527 PMID: 27797339
Witts et al (2012) Glial-derived adenosine modulates spinal motor networks in mice. J.Neurophysiol. 107 1925 PMID: 22205649
Villa-Bellosta (2019) ATP-based therapy prevents vascular calcification and extends longevity in a mouse model of Hutchinson-Gilford progeria syndrome. Proc.Natl.Acad.Sci.U.S.A. 116 23698 PMID: 31690656
Carneiro et al (2014) Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium. Br J Pharmacol 171 3404 PMID: 24697602
Yegutkin et al (2012) Metabolism of circulating ADP in the bloodstream is mediated via integrated actions of soluble adenylate kinase-1 and NTPDase1/CD39 activities. FASEB J 26 3875 PMID: 22637533
Ng (2018) Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells. Cell Signal 51 59 PMID: 30076967
Billaud et al (2015) A molecular signature in the pannexin1 intracellular loop confers channel activation by the α1 adrenoreceptor in smooth muscle cells. J Neuroimmune Pharmacol 8 ra17 PMID: 25690012
Sorrell and Hauser (2014) Ligand-gated purinergic receptors regulate HIV-1 Tat and mor. related neurotoxicity in primary mouse striatal neuron-glia co-cultures. Radiat Oncol 9 233 PMID: 24158495
Kleiner et al (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis 24 647 PMID: 30310263
Fang et al (2016) Expression of CD39 on activated T cells impairs their survival in older individuals. Cell Rep. 14 1218 PMID: 26832412
Ziemlinska et al (2014) Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats. PLoS One 9 e88833 PMID: 24551172
Carlsen and Perrier (2014) Purines released from astrocytes inhibit excitatory synaptic transmission in the ventral horn of the spinal cord. Front Neural Circuits 8 60 PMID: 24926236
Boyd-Tressler et al (2014) Chemotherapeutic drugs induce ATP release via caspase-gated pannexin-1 channels and a caspase/pannexin-1-independent mechanism. J Biol Chem 289 27246 PMID: 25112874
Campwala et al (2014) P2Y6 receptor inhibition perturbs CCL2-evoked signalling in human monocytic and peripheral blood mononuclear cells. J Cell Sci 127 4964 PMID: 25271060
Jansen et al (2013) ABCC6 prevents ectopic mineralization seen in pseudoxanthoma elasticum by inducing cellular nucleotide release. Sci Rep 110 20206 PMID: 24277820
Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. PLoS One 305 F396 PMID: 23720349
Griffiths et al (2011) Th1/Th17 cell induction and corresponding reduction in ATP consumption following vaccination with the novel Mycobacterium tuberculosis vaccine MVA85A. PLoS One 6 e23463 PMID: 21887254
Kennedy et al (2007) Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. J Neurosci 27 845 PMID: 17251425
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Prevents degradation of ATP released from cultured cells.
By
Anonymous on 01/10/2018
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Primary Astrocytes
Used in ATP release assay from cultured cells to inhibit ectonucleotidase function
Working concentration of 100 uM
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P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.