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| SKU | Size | Availability |
Price | Qty |
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I654939-1ml
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1ml |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$278.90
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| Specifications & Purity | 10mM in DMSO |
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| Biochemical and Physiological Mechanisms | 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-len |
| Storage Temp | Desiccated,Store at -80°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
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) |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Smiles | CN1C(=O)C2=C(N(N=C2N3C1=NC4C3CCC4)CC5=CC=C(C=C5)C6=NC(=CC=C6)F)NC7=CC=CC=C7.OP(=O)(O)O |
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| Molecular Weight | 605.6 |