ITI-214

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 functionsIn VitroITI-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. .In VivoITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg . 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.Form:SolidIC50& Target:PDE1 58 pM (Ki) PDE1A 33 pM (Ki) PDE1B 380 pM (Ki) PDE1C 35 pM (Ki)

Specifications & Purity: 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 functionsIn VitroITI-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. .In VivoITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg . 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.Form:SolidIC50& Target:PDE1 58 pM (Ki) PDE1A 33 pM (Ki) PDE1B 380 pM (Ki) PDE1C 35 pM (Ki)

Grade: Moligand™

Molecular Formula: C29H29FN7O5P

Molecular Weight: 605.56

PubChem CID: 72704434

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

Storage Temperature: Protected from light;Store at -20°C;Argon charged

Shipped in: Ice chest + Ice pads

UPC:

42301503

Weight:

1.09 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

I647238-25mg

Country of Origin:

China

CAS:

1642303-38-5

Product Size:

25mg

Harmonized Tariff Code:

2931.90.90