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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Moligand™,10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Desiccated,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor ( K i of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with K i s of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions
In Vitro
ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (K i =?33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats Dosage: 0.1-10 mg/kg Administration: p.o. Result: Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.
IC50& Target:PDE1 58 pM (Ki) PDE1A 33 pM (Ki) PDE1B 380 pM (Ki) PDE1C 35 pM (Ki)
| Isomeric SMILES | CN1C(=O)C2=C(N(N=C2N3C1=N[C@H]4[C@@H]3CCC4)CC5=CC=C(C=C5)C6=NC(=CC=C6)F)NC7=CC=CC=C7.OP(=O)(O)O |
|---|---|
| Alternate CAS | 1642303-38-5;1160521-50-5(free base) |
| Molecular Weight | 605.56 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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