R112

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

Description:R112 is a Syk inhibitor. R112 inhibited degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC(50)] = 353 nmol/L) or basophils (histamine release, EC(50) = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC(50) = 490 nmol/L). R112 also blocked leukotriene C4 production and all proinflammatory cytokines tested. Subsequent molecular characterization indicated that R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor (inhibitory constant [K(i)] = 96 nmol/L).

Price and Availability

R112, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 200mg may be 2 weeks.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 401780Name: R112CAS#: 575474-82-7Chemical Formula: C16H13FN4O2Exact Mass: 312.10225Molecular Weight: 312.3Elemental Analysis: C, 61.53; H, 4.20; F, 6.08; N, 17.94; O, 10.25

Synonym:R112; R112; R 112.

IUPAC/Chemical Name:3,3'-((5-fluoropyrimidine-2,4-diyl)bis(azanediyl))diphenol

InChi Key:TVKGTSHBQZEFEE-UHFFFAOYSA-N

InChi Code:InChI=1S/C16H13FN4O2/c17-14-9-18-16(20-11-4-2-6-13(23)8-11)21-15(14)19-10-3-1-5-12(22)7-10/h1-9,22-23H,(H2,18,19,20,21)

SMILES Code:FC1=CN=C(NC2=CC(O)=CC=C2)N=C1NC3=CC(O)=CC=C3

Technical Data

Additional Information

References

1: Rossi AB, Herlaar E, Braselmann S, Huynh S, TaylorV, Frances R, Issakani SD, Argade A, Singh R, Payan DG, Masuda ES.Identification of the Syk kinase inhibitor R112 by a human mast cellscreen. J Allergy Clin Immunol. 2006 Sep;118(3):749-55. Epub 2006 Jul28. PubMed PMID: 16950297.

2: Guyer BJ, Shimamoto SR, Bradhurst AL, Grossbard EB, Dreskin SC,Nelson HS. Mast cell inhibitor R112 is well tolerated and affectsprostaglandin D2 but not other mediators, symptoms, or nasal volumes ina nasal challenge model of allergic rhinitis. Allergy Asthma Proc. 2006May-Jun;27(3):208-13. PubMed PMID: 16913263.

3: Meltzer EO, Berkowitz RB, Grossbard EB. An intranasal Syk-kinaseinhibitor (R112) improves the symptoms of seasonal allergic rhinitis ina park environment. J Allergy Clin Immunol. 2005 Apr;115(4):791-6.PubMed PMID: 15806000.

4: Kang AK, Jenkins DJ, Wolever TM, Huff MW, Maguire GF, Connelly PW,Hegele RA. Apolipoprotein E R112; R251G: a carboxy-terminal variantfound in patients with hyperlipidemia and coronary heart disease. MutatRes. 1997 Sep;382(1-2):57-65. PubMed PMID: 9360638.