NF 546

Selective P2Y11 agonist CAS# 1006028-37-0

NF 546

Catalog No. BCC7804----Order now to get a substantial discount!

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Quality Control of NF 546

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Chemical structure

NF 546

3D structure

Chemical Properties of NF 546

Cas No. 1006028-37-0 SDF Download SDF
PubChem ID 73755075 Appearance Powder
Formula C47H44N6Na4O17P4 M.Wt 1180.74
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in water with gentle warming
Chemical Name 4,4'-(Carbonylbis(imino-3,1-phenylene-carbonylimino-3,1-(4-methyl-phenylene)carbonylimino))-bis(1,3-xylene-alpha,alpha'-diphosphonic acid tetrasodium salt
SMILES CC1=C(C=C(C=C1)C(=O)NC2=C(C=C(C=C2)CP(=O)(O)[O-])CP(=O)(O)[O-])NC(=O)C3=CC(=CC=C3)NC(=O)NC4=CC=CC(=C4)C(=O)NC5=C(C=CC(=C5)C(=O)NC6=C(C=C(C=C6)CP(=O)(O)[O-])CP(=O)(O)[O-])C.[Na+].[Na+].[Na+].[Na+]
Standard InChIKey GSMUPMANKNAMAS-UHFFFAOYSA-J
Standard InChI InChI=1S/C47H48N6O17P4.4Na/c1-27-9-13-33(45(56)50-39-15-11-29(23-71(59,60)61)17-35(39)25-73(65,66)67)21-41(27)52-43(54)31-5-3-7-37(19-31)48-47(58)49-38-8-4-6-32(20-38)44(55)53-42-22-34(14-10-28(42)2)46(57)51-40-16-12-30(24-72(62,63)64)18-36(40)26-74(68,69)70;;;;/h3-22H,23-26H2,1-2H3,(H,50,56)(H,51,57)(H,52,54)(H,53,55)(H2,48,49,58)(H2,59,60,61)(H2,62,63,64)(H2,65,66,67)(H2,68,69,70);;;;/q;4*+1/p-4
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of NF 546

DescriptionP2Y11 agonist (pEC50 = 6.27). Exhibits selectivity for P2Y11 over a range of P2Y and P2X receptors.

NF 546 Dilution Calculator

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NF 546 Molarity Calculator

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Preparing Stock Solutions of NF 546

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 0.8469 mL 4.2346 mL 8.4693 mL 16.9385 mL 21.1732 mL
5 mM 0.1694 mL 0.8469 mL 1.6939 mL 3.3877 mL 4.2346 mL
10 mM 0.0847 mL 0.4235 mL 0.8469 mL 1.6939 mL 2.1173 mL
50 mM 0.0169 mL 0.0847 mL 0.1694 mL 0.3388 mL 0.4235 mL
100 mM 0.0085 mL 0.0423 mL 0.0847 mL 0.1694 mL 0.2117 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on NF 546

NF546 [4,4'-(carbonylbis(imino-3,1-phenylene-carbonylimino-3,1-(4-methyl-phenylene)-car bonylimino))-bis(1,3-xylene-alpha,alpha'-diphosphonic acid) tetrasodium salt] is a non-nucleotide P2Y11 agonist and stimulates release of interleukin-8 from human monocyte-derived dendritic cells.[Pubmed:19815812]

J Pharmacol Exp Ther. 2010 Jan;332(1):238-47.

The G protein-coupled P2Y(11) receptor is involved in immune system modulation. In-depth physiological evaluation is hampered, however, by a lack of selective and potent ligands. By screening a library of sulfonic and phosphonic acid derivatives at P2Y(11) receptors recombinantly expressed in human 1321N1 astrocytoma cells (calcium and cAMP assays), the selective non-nucleotide P2Y(11) agonist NF546 [4,4'-(carbonylbis(imino-3,1-phenylene-carbonylimino-3,1-(4-methyl-phenylene)carb onylimino))-bis(1,3-xylene-alpha,alpha'-diphosphonic acid) tetrasodium salt] was identified. NF546 had a pEC(50) of 6.27 and is relatively selective for P2Y(11) over P2Y(1), P2Y(2), P2Y(4), P2Y(6), P2Y(12), P2X(1), P2X(2), and P2X(2)-X(3). Adenosine-5'-O-(3-thio)triphosphate (ATPgammaS), a nonhydrolyzable analog of the physiological P2Y(11) agonist ATP, and NF546 use a common binding site as suggested by molecular modeling studies and their competitive behavior toward the nanomolar potency antagonist NF340 [4,4'-(carbonylbis(imino-3,1-(4-methyl-phenylene)carbonylimino))bis(naphthalene-2 ,6-disulfonic acid) tetrasodium salt] in Schild analysis. The pA(2) of NF340 was 8.02 against ATPgammaS and 8.04 against NF546 (calcium assays). NF546 was further tested for P2Y(11)-mediated effects in monocyte-derived dendritic cells. Similarly to ATPgammaS, NF546 led to thrombospondin-1 secretion and inhibition of lipopolysaccharide-stimulated interleukin-12 release, whereas NF340 inhibited these effects. Further, for the first time, it was shown that ATPgammaS or NF546 stimulation promotes interleukin 8 (IL-8) release from dendritic cells, which could be inhibited by NF340. In conclusion, we have described the first selective, non-nucleotide agonist NF546 for P2Y(11) receptors in both recombinant and physiological expression systems and could show a P2Y(11)-stimulated IL-8 release, further supporting the immunomodulatory role of P2Y(11) receptors.

Description

NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells.

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