A histamine H4 receptor antagonist
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Adriforant (hydrochloride hydrate)

Item No. 43638

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N4-(cyclopropylmethyl)-6-[(3R)-3-(methylamino)-1-pyrrolidinyl]-2,4-pyrimidinediamine, dihydrochloride hydrate
CAS Number
2096455-90-0
Synonyms
  • PF-3893787
  • ZPL-389
Molecular Formula
C13H22N6 • 2HCl [XH2O]
Formula Weight
335.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
CN[C@H]1CN(C2=NC(N)=NC(NCC3CC3)=C2)CC1.Cl.O.Cl
InChi Code
InChI=1S/C13H22N6.2ClH.H2O/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9;;;/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18);2*1H;1H2/t10-;;;/m1.../s1
InChi Key
ZSCRXFDQDVRGJM-FYBBWCNBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    Adriforant is a histamine H4 receptor antagonist (Ki = 6.17 nM).1 It prevents histamine-induced shape change, CD11b protein upregulation, and actin polymerization in isolated human eosinophils (IC50s = 0.65, 4.9, and 1.3 nM, respectively). Adriforant (10 µM) inhibits histamine-induced calcium influx in primary mouse dorsal root ganglion neurons.2 In vivo, adriforant (50 mg/kg per day) decreases ear thickness and reduces basophils, eosinophils, neutrophils, and T cell infiltration in a mouse model of atopic dermatitis induced by MC903 (calcipotriol; Item No. 10009599).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mowbray, C.E., Bell, A.S., Clarke, N.P., et al. Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: A novel histamine H4 receptor antagonist. Bioorg. Med. Chem. Lett. 21(21), 6596-6602 (2011).

    2. Uluckan, Ö., Bruno, S., Wang, Y., et al. Adriforant is a functional antagonist of histamine receptor 4 and attenuates itch and skin inflammation in mice. Eur. J. Pharmacol. 945:175533, (2023).