1606975-12-5

1606975-12-5 structure

Name: BPN14770
Chemical Name: Bpn-14770
CAS Number: 1606975-12-5
Molecular Formula: C₁₉H₁₄ClF₃N₄O
Molecular Weight: 406.789
Create Date: 2020-01-12 10:16:57
Modify Date: 2024-01-02 16:42:15
BPN14770 (BPN-14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively, displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2 IC50 = 127 nM); BPN14770 is 17-fold less potent against mouse PDE4D7 (IC50 = 133 nM), binds to a primate-specific, N-terminal region of PDE4D; elevates brain cAMP and facilitates hippocampal long-term potentiation (LTP) in wild-type and humanized PDE4D mice, improves cognitive performance, antagonized the amnesic effects of scopolamine and increased cAMP signaling in brain, and increased BDNF and markers of neuronal plasticity associated with memory. Other Indication Phase 2 Clinical

Name	Bpn-14770
Synonyms	2-(4-{[2-(3-Chlorophenyl)-6-(trifluoromethyl)-4-pyrimidinyl]amino}phenyl)acetamide Bpn-14770 Benzeneacetamide, 4-[[2-(3-chlorophenyl)-6-(trifluoromethyl)-4-pyrimidinyl]amino]-

Description	BPN14770 (BPN-14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively, displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2 IC50 = 127 nM); BPN14770 is 17-fold less potent against mouse PDE4D7 (IC50 = 133 nM), binds to a primate-specific, N-terminal region of PDE4D; elevates brain cAMP and facilitates hippocampal long-term potentiation (LTP) in wild-type and humanized PDE4D mice, improves cognitive performance, antagonized the amnesic effects of scopolamine and increased cAMP signaling in brain, and increased BDNF and markers of neuronal plasticity associated with memory. Other Indication Phase 2 Clinical
References	References 1. Zhang C, et al. Neuropsychopharmacology. 2018 Oct;43(11):2299-2309. 2. Gurney ME, et al. Handb Exp Pharmacol. 2011;(204):167-92. 3. Gurney ME, et al. Sci Rep. 2017 Nov 7;7(1):14653. View Related Products by Target Phosphodiesterase (PDE) Other Indication