A histamine H4 receptor agonist
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VUF10460

Item No. 14665

Technical Information
Formal Name
4-(4-methyl-1-piperazinyl)-6-phenyl-2-pyrimidinamine
CAS Number
1028327-66-3
Molecular Formula
C15H19N5
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: 100mg/mL
λmax
245, 316 nm
SMILES
CN(CC1)CCN1C2=CC(C3=CC=CC=C3)=NC(N)=N2
InChi Code
InChI=1S/C15H19N5/c1-19-7-9-20(10-8-19)14-11-13(17-15(16)18-14)12-5-3-2-4-6-12/h2-6,11H,7-10H2,1H3,(H2,16,17,18)
InChi Key
NIJGWJIOMPHDBP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VUF10460 is a histamine H4 receptor agonist (Kis = 5.01 and 14.13 nM for the human and rat receptors, respectively).1,2 It is selective for the rat histamine H4 receptor over the rat histamine H3 receptor (Kis = 34.67 and 1,778.28 nM, respectively).2 VUF10460 (10 mg/kg) potentiates the formation of HCl-induced ulcers in the rat gastric mucosa, an effect that is not blocked by the histamine H4 receptor antagonist JNJ-7777120 (Item No. 10011925).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cowart, M.D., Altenbach, R.J., Liu, H., et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: A new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J. Med. Chem. 51(20), 6547-6557 (2008).

    2. Coruzzi, G., Adami, M., Pozzoli, C., et al. Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur J. Pharmacol. 669(1-3), 121-127 (2011).