A PDE1 inhibitor
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ITI214

Item No. 30376

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6aR,9aS)-2-[[4-(6-fluoro-2-pyridinyl)phenyl]methyl]-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, monophosphate
CAS Number
1642303-38-5
Molecular Formula
C29H26FN7O • H3PO4
Formula Weight
605.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
CN1C2=N[C@@]3([H])[C@@](CCC3)([H])N2C4=NN(CC5=CC=C(C6=NC(F)=CC=C6)C=C5)C(NC7=CC=CC=C7)=C4C1=O.O=P(O)(O)O
InChi Code
InChI=1S/C29H26FN7O.H3O4P/c1-35-28(38)25-26(31-20-7-3-2-4-8-20)36(34-27(25)37-23-11-5-10-22(23)33-29(35)37)17-18-13-15-19(16-14-18)21-9-6-12-24(30)32-21;1-5(2,3)4/h2-4,6-9,12-16,22-23,31H,5,10-11,17H2,1H3;(H3,1,2,3,4)/t22-,23+;/m1./s1
InChi Key
ZPIAAFIYOPWWJL-RFPXDPOKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $90

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    5 mg

    $392

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    10 mg

    $696

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    Product Description

    ITI214 is an inhibitor of phosphodiesterase 1 (PDE1; Ki = 0.058 nM).1 It is selective for PDE1 over PDE2A, -3B, -4A, -5A, -6, -7B, -8A, -9A, -10A, and -11A (Kis = 0.16-18 µM). ITI214 (3 and 6 mg/kg) enhances novel object recognition in rats. It increases prefrontal cortex cAMP and cGMP levels in mice when administered at a dose of 50 mg/kg.2 ITI214 (0.1, 3, and 10 mg/kg) reverses MK-801-induced decreases in spontaneous alteration in the T-maze continuous alternation task in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, P., Zheng, H., Zhao, J., et al. Discovery of potent and selective inhibitors of phosphodiesterase 1 for the treatment of cognitive impairment associated with neurodegenerative and neuropsychiatric diseases. J. Med. Chem. 59(3), 1149-1164 (2016).

    2. Pekcec, A., Schülert, N., Stierstorfer, B., et al. Targeting the dopamine D1 receptor or its downstream signalling by inhibiting phosphodiesterase-1 improves cognitive performance. Br. J. Pharmacol. 175(14), 3021-3033 (2018).