product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
1391/10
catalog :
1391/10
quantity :
10 mg (also 50 mg)
price :
294 USD
more info or order :
citations: 25
Reference
Su L, Bryan N, Battista S, Freitas J, Garabedian A, D Alessio F, et al. Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays. Sci Rep. 2020;10:18850 pubmed publisher
Johansson K, Ståhl A, Arvidsson I, Loos S, Tontanahal A, Rebetz J, et al. Shiga toxin signals via ATP and its effect is blocked by purinergic receptor antagonism. Sci Rep. 2019;9:14362 pubmed publisher
Chandra N, Frängsmyr L, Arnberg N. Decoy Receptor Interactions as Novel Drug Targets against EKC-Causing Human Adenovirus. Viruses. 2019;11: pubmed publisher
Palygin O, Ilatovskaya D, Levchenko V, Klemens C, Dissanayake L, Williams A, et al. Characterization of purinergic receptor expression in ARPKD cystic epithelia. Purinergic Signal. 2018;14:485-497 pubmed publisher
Gao J, Xin W, Huang J, Ji B, Gao S, Chen L, et al. Research articleHemolysis in human erythrocytes by Clostridium perfringens epsilon toxin requires activation of P2 receptors. Virulence. 2018;9:1601-1614 pubmed publisher
Zhang D, Sun Y, Ma M, Wang Y, Lin H, Li R, et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility. elife. 2018;7: pubmed publisher
Li X, Chen W, Li P, Wei J, Cheng Y, Liu P, et al. Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression. Theranostics. 2017;7:4671-4688 pubmed publisher
Koessler J, Schwarz M, Weber K, Etzel J, Koessler A, Böeck M, et al. The role of adenosine diphosphate mediated platelet responsiveness for the stability of platelet integrity in citrated whole blood under ex vivo conditions. PLoS ONE. 2017;12:e0188193 pubmed publisher
Li T, Wu H, Wang Y, Li X, Wang Y. Molecular signaling underlying bulleyaconitine A (BAA)-induced microglial expression of prodynorphin. Sci Rep. 2017;7:45056 pubmed publisher
Koessler J, Hermann S, Weber K, Koessler A, Kuhn S, Böeck M, et al. Role of Purinergic Receptor Expression and Function for Reduced Responsiveness to Adenosine Diphosphate in Washed Human Platelets. PLoS ONE. 2016;11:e0147370 pubmed publisher
Nishimura Y, McLaughlin N, Pan J, Goldstein S, Hafenstein S, Shimizu H, et al. The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate. PLoS Pathog. 2015;11:e1005184 pubmed publisher
Siuda E, McCall J, Al Hasani R, Shin G, Il Park S, Schmidt M, et al. Optodynamic simulation of β-adrenergic receptor signalling. Nat Commun. 2015;6:8480 pubmed publisher
Ren P, Zou G, Bailly B, Xu S, Zeng M, Chen X, et al. The approved pediatric drug suramin identified as a clinical candidate for the treatment of EV71 infection-suramin inhibits EV71 infection in vitro and in vivo. Emerg Microbes Infect. 2014;3:e62 pubmed publisher
Alefishat E, Alexander S, Ralevic V. Effects of NAD at purine receptors in isolated blood vessels. Purinergic Signal. 2015;11:47-57 pubmed publisher
He X, Zhang L, Chen Y, Remke M, Shih D, Lu F, et al. The G protein α subunit Gαs is a tumor suppressor in Sonic hedgehog-driven medulloblastoma. Nat Med. 2014;20:1035-42 pubmed publisher
Madoux F, Tredup C, Spicer T, Scampavia L, Chase P, Hodder P, et al. Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin ? and ?. Biopolymers. 2014;102:396-406 pubmed publisher
Ilatovskaya D, Palygin O, Levchenko V, Staruschenko A. Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol. 2013;305:C1050-9 pubmed publisher
Vergani A, Tezza S, D Addio F, Fotino C, Liu K, Niewczas M, et al. Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7. Circulation. 2013;127:463-75 pubmed publisher
Th xe9 xe2 tre E, Frederix K, Guilmain W, Delierneux C, Lecut C, Bettendorff L, et al. Overexpression of CD39 in mouse airways promotes bacteria-induced inflammation. J Immunol. 2012;189:1966-74 pubmed publisher
Ibáñez G, Shum D, Blum G, Bhinder B, Radu C, Antczak C, et al. A high throughput scintillation proximity imaging assay for protein methyltransferases. Comb Chem High Throughput Screen. 2012;15:359-71 pubmed
Cheng Y, Zhang Q, Meng Q, Xia T, Huang Z, Wang C, et al. Leucine deprivation stimulates fat loss via increasing CRH expression in the hypothalamus and activating the sympathetic nervous system. Mol Endocrinol. 2011;25:1624-35 pubmed publisher
Maloney S, Brass L, Diamond S. P2Y12 or P2Y1 inhibitors reduce platelet deposition in a microfluidic model of thrombosis while apyrase lacks efficacy under flow conditions. Integr Biol (Camb). 2010;2:183-92 pubmed publisher
Donnelly Roberts D, Namovic M, Han P, Jarvis M. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br J Pharmacol. 2009;157:1203-14 pubmed publisher
Kennedy C, Tasker P, Gallacher G, Westfall T. Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. J Neurosci. 2007;27:845-51 pubmed
Fresco P, Diniz C, Goncalves J. Facilitation of noradrenaline release by activation of adenosine A(2A) receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery. Cardiovasc Res. 2004;63:739-46 pubmed
product information
master code :
1391
SKU :
1391/10
product name :
NF 449
unit size :
10 mg (also 50 mg)
description :
Highly selective P2X1 antagonist
target :
P2X Receptor Antagonists
category :
Small Molecules
purity :
90%
observed molecular weight :
1505.06
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
NF 449 is a potent purinergic receptor antagonist that displays high selectivity for P2X1 (IC50 values are 0.28, 0.69, 120, 1820, 47000 and 300000 nM for rP2X1, rP2X1+5, rP2X2+3, rP2X3, rP2X2 and P2X4 receptors respectively). Provides antithrombotic protection in vivo . Also acts as a Gs -selective antagonist. Also inhibits DNA-binding activity of HMGA2 (IC50 = 0.43 M). . This product is supplied with a high degree of hydration and some residual NaCl, the amount of which are batch dependent. Please refer to the Certificate of Analysis to obtain the batch specific Net Product Content and the maximum solubility threshold to use in dilution calculations.
top caption :
Highly selective P2X1 antagonist
extended description :
Highly selective P2X1 antagonist
chemical name text :
4,4 ,4 ,4 -[Carbonylbis(imino-5,1,3-benzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzenedisulfonic acid, octasodium salt
formula :
C41H24N6Na8O29S8
formula text :
C41H24N6Na8O29S8
cas num :
627034-85-9
USD :
294 USD
product details :
Highly selective P2X1 antagonist
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK