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ITI-214 - 10mM in DMSO, high purity , CAS No.1642303-38-5(DMSO)

    Grade & Purity:
  • 10mM in DMSO
In stock
Item Number
I654939
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Availability
Price Qty
I654939-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$278.90

Basic Description

Specifications & Purity 10mM in DMSO
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)

Associated Targets(Human)

PDE5A Tclin cGMP-specific 3',5'-cyclic phosphodiesterase (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDE4A Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4A (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDE7B Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 7B (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDE1B Tclin Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

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
Molecular Weight 605.6

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Solution Calculators

Reviews

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