NF157 | CAS#104869-26-3 | P2X Receptor Antagonist

NF157
featured

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532343

CAS#: 104869-26-3

Description: NF157 is a purinergic receptor antagonist that potently inhibits P2Y11 receptor activity (IC50 = 463 nM). NF157 displays selectivity for P2Y11 and P2X1 receptors over P2Y1, P2Y2 , P2X2, P2X3, P2X4 and P2X7 receptors. NF157 also inhibits NAD+-induced activation of human granulocytes.

Chemical Structure

NF157

CAS# 104869-26-3

Instruction

Theoretical Analysis

MedKoo Cat#: 532343
Name: NF157
CAS#: 104869-26-3
Chemical Formula: C49H34F2N6O23S6
Exact Mass: 1,304.00
Molecular Weight: 1,305.190
Elemental Analysis: C, 45.09; H, 2.63; F, 2.91; N, 6.44; O, 28.19; S, 14.74

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350
50mg	USD 1280
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: NF157; NF 157; NF-157.

IUPAC/Chemical Name: 8-[[4-fluoro-3-[[3-[[3-[[2-fluoro-5-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonic acid

InChi Key: UDVIAMRWOLIUAE-UHFFFAOYSA-N

InChi Code: InChI=1S/C49H34F2N6O23S6/c50-33-9-7-25(47(60)54-35-11-13-39(83(69,70)71)31-19-29(81(63,64)65)21-41(43(31)35)85(75,76)77)17-37(33)56-45(58)23-3-1-5-27(15-23)52-49(62)53-28-6-2-4-24(16-28)46(59)57-38-18-26(8-10-34(38)51)48(61)55-36-12-14-40(84(72,73)74)32-20-30(82(66,67)68)22-42(44(32)36)86(78,79)80/h1-22H,(H,54,60)(H,55,61)(H,56,58)(H,57,59)(H2,52,53,62)(H,63,64,65)(H,66,67,68)(H,69,70,71)(H,72,73,74)(H,75,76,77)(H,78,79,80)

SMILES Code: O=S(C1=C2C(NC(C3=CC=C(F)C(NC(C4=CC=CC(NC(NC5=CC=CC(C(NC6=CC(C(NC7=C8C(S(=O)(O)=O)=CC(S(=O)(O)=O)=CC8=C(S(=O)(O)=O)C=C7)=O)=CC=C6F)=O)=C5)=O)=C4)=O)=C3)=O)=CC=C(S(=O)(O)=O)C2=CC(S(=O)(O)=O)=C1)(O)=O

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: >2 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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,305.19 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
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:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

1: Dreisig K, Kornum BR. A critical look at the function of the P2Y11 receptor. Purinergic Signal. 2016 Sep;12(3):427-37. doi: 10.1007/s11302-016-9514-7. Epub 2016 May 31. PubMed PMID: 27246167; PubMed Central PMCID: PMC5023629.

2: Hara S, Kobayashi M, Kuriiwa F, Mukai T, Mizukami H. Different mechanisms of hydroxyl radical production susceptible to purine P2 receptor antagonists between carbon monoxide poisoning and exogenous ATP in rat striatum. Free Radic Res. 2014 Nov;48(11):1322-33. doi: 10.3109/10715762.2014.951842. Epub 2014 Sep 2. PubMed PMID: 25096805.

3: Nagakura C, Negishi Y, Tsukimoto M, Itou S, Kondo T, Takeda K, Kojima S. Involvement of P2Y11 receptor in silica nanoparticles 30-induced IL-6 production by human keratinocytes. Toxicology. 2014 Aug 1;322:61-8. doi: 10.1016/j.tox.2014.03.010. Epub 2014 May 2. PubMed PMID: 24793913.

4: Pliyev BK, Ivanova AV, Savchenko VG. Extracellular NAD(+) inhibits human neutrophil apoptosis. Apoptosis. 2014 Apr;19(4):581-93. doi: 10.1007/s10495-013-0948-x. PubMed PMID: 24292505.

5: Nobbio L, Visigalli D, Mannino E, Fiorese F, Kassack MU, Sturla L, Prada V, De Flora A, Zocchi E, Bruzzone S, Schenone A. The diadenosine homodinucleotide P18 improves in vitro myelination in experimental Charcot-Marie-Tooth type 1A. J Cell Biochem. 2014 Jan;115(1):161-7. doi: 10.1002/jcb.24644. PubMed PMID: 23959806.

6: Djerada Z, Millart H. Intracellular NAADP increase induced by extracellular NAADP via the P2Y11-like receptor. Biochem Biophys Res Commun. 2013 Jun 28;436(2):199-203. doi: 10.1016/j.bbrc.2013.04.110. Epub 2013 May 31. PubMed PMID: 23726915.

7: Djerada Z, Peyret H, Dukic S, Millart H. Extracellular NAADP affords cardioprotection against ischemia and reperfusion injury and involves the P2Y11-like receptor. Biochem Biophys Res Commun. 2013 May 10;434(3):428-33. doi: 10.1016/j.bbrc.2013.03.089. Epub 2013 Apr 9. PubMed PMID: 23583195.

8: Sakaki H, Tsukimoto M, Harada H, Moriyama Y, Kojima S. Autocrine regulation of macrophage activation via exocytosis of ATP and activation of P2Y11 receptor. PLoS One. 2013;8(4):e59778. doi: 10.1371/journal.pone.0059778. Epub 2013 Apr 5. PubMed PMID: 23577075; PubMed Central PMCID: PMC3618444.

9: Ishimaru M, Tsukimoto M, Harada H, Kojima S. Involvement of P2Y₁₁ receptor in IFN-γ-induced IL-6 production in human keratinocytes. Eur J Pharmacol. 2013 Mar 5;703(1-3):67-73. doi: 10.1016/j.ejphar.2013.02.020. Epub 2013 Feb 24. PubMed PMID: 23461851.

10: Hara S, Mizukami H, Kuriiwa F, Mukai T. cAMP production mediated through P2Y(11)-like receptors in rat striatum due to severe, but not moderate, carbon monoxide poisoning. Toxicology. 2011 Oct 9;288(1-3):49-55. doi: 10.1016/j.tox.2011.07.001. Epub 2011 Jul 12. PubMed PMID: 21777648.

11: Klein C, Grahnert A, Abdelrahman A, Müller CE, Hauschildt S. Extracellular NAD(+) induces a rise in [Ca(2+)](i) in activated human monocytes via engagement of P2Y(1) and P2Y(11) receptors. Cell Calcium. 2009 Oct;46(4):263-72. doi: 10.1016/j.ceca.2009.08.004. Epub 2009 Sep 11. PubMed PMID: 19748117.

12: Ben Yebdri F, Kukulski F, Tremblay A, Sévigny J. Concomitant activation of P2Y(2) and P2Y(6) receptors on monocytes is required for TLR1/2-induced neutrophil migration by regulating IL-8 secretion. Eur J Immunol. 2009 Oct;39(10):2885-94. doi: 10.1002/eji.200939347. PubMed PMID: 19735076; PubMed Central PMCID: PMC5140286.

13: Vaughan KR, Stokes L, Prince LR, Marriott HM, Meis S, Kassack MU, Bingle CD, Sabroe I, Surprenant A, Whyte MK. Inhibition of neutrophil apoptosis by ATP is mediated by the P2Y11 receptor. J Immunol. 2007 Dec 15;179(12):8544-53. PubMed PMID: 18056402; PubMed Central PMCID: PMC2292245.

14: Moreschi I, Bruzzone S, Bodrato N, Usai C, Guida L, Nicholas RA, Kassack MU, Zocchi E, De Flora A. NAADP+ is an agonist of the human P2Y11 purinergic receptor. Cell Calcium. 2008 Apr;43(4):344-55. Epub 2007 Aug 17. PubMed PMID: 17707504.

15: Sundqvist M. Developmental changes of purinergic control of intestinal motor activity during metamorphosis in the African clawed frog, Xenopus laevis. Am J Physiol Regul Integr Comp Physiol. 2007 May;292(5):R1916-25. Epub 2007 Feb 1. PubMed PMID: 17272661.

16: Moreschi I, Bruzzone S, Nicholas RA, Fruscione F, Sturla L, Benvenuto F, Usai C, Meis S, Kassack MU, Zocchi E, De Flora A. Extracellular NAD+ is an agonist of the human P2Y11 purinergic receptor in human granulocytes. J Biol Chem. 2006 Oct 20;281(42):31419-29. Epub 2006 Aug 22. PubMed PMID: 16926152.

17: Ullmann H, Meis S, Hongwiset D, Marzian C, Wiese M, Nickel P, Communi D, Boeynaems JM, Wolf C, Hausmann R, Schmalzing G, Kassack MU. Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. J Med Chem. 2005 Nov 3;48(22):7040-8. PubMed PMID: 16250663.

Your view history

NF157 featured