A GPR18 agonist
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PSB-KD107

Item No. 31393

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7,8,9-tetrahydro-9-[2-(1H-indol-3-yl)ethyl]-1,3-dimethyl-pyrimido[2,1-f]purine-2,4(1H,3H)-dione
CAS Number
955121-65-0
Molecular Formula
C20H22N6O2
Formula Weight
378.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
222, 302 nm
SMILES
O=C1C2=C(N(C)C(N1C)=O)N=C3N2CCCN3CCC4=CNC5=C4C=CC=C5
InChi Code
InChI=1S/C20H22N6O2/c1-23-17-16(18(27)24(2)20(23)28)26-10-5-9-25(19(26)22-17)11-8-13-12-21-15-7-4-3-6-14(13)15/h3-4,6-7,12,21H,5,8-11H2,1-2H3
InChi Key
PUJKERUFRDZALE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $90

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    5 mg

    $219

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    10 mg

    $392

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    Product Description

    PSB-KD107 is an agonist of the orphan G protein-coupled receptor GPR18 (EC50 = 0.56 µM in a β-arrestin recruitment assay using CHO cells expressing the human receptor).1,2 It is selective for GPR18 over GPR55, as well as cannabinoid 1 (CB1) and CB2 receptors, at 10 µM but also binds to the adenosine A2A receptor (Ki = 0.33 µM for the rat receptor).1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schoeder, C.T., Kaleta, M., Mahardhika, A.B., et al. Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18. Eur. J. Med. Chem. 155, 381-397 (2018).

    2. Schoeder, C.T., Mahardhika, A.B., Drabczyńska, A., et al. Discovery of tricyclic xanthines as agonists of the cannabinoid-activated orphan G‑protein-coupled receptor GPR18. ACS Med. Chem. Lett. (2020).

    3. Drabczyńska, A., Müller, C.E., Schiedel, A., et al. Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: Structure-activity relationships as adenosine A1 and A2A receptor ligands. Bioorg. Med. Chem. 15(22), 6956-6974 (2007).