[CAS NO. 1173239-39-8] PF-03463275

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PRODUCTS SPECIFICATIONS [1173239-39-8]

Catalog

HY-10716A

Brand

MCE

CAS

1173239-39-8

DESCRIPTION [1173239-39-8]

Overview

MDL	-
Molecular Weight	376.86
Molecular Formula	C19H22ClFN4O
SMILES	O=C(C(N=C1)=CN1C)N(CC(C=C2)=CC(Cl)=C2F)C[C@@H]3[C@](C4)([H])[C@@]3([H])CN4C

For research use only. We do not sell to patients.

Summary

PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a K _i of 11.6 nM. PF-03463275 has the potential for Schizophrenia research ^[1] ^[2] .

In Vivo

PF-03463275 (1-10 mg/kg; s.c.) attenuates oscillatory potentials (OPs) ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats ^[2]
Dosage:	1, 3 and 10 mg/kg
Administration:	S.c.
Result:	A dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from the dark-adapted rats.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01159626	Pfizer	Healthy	July 2010	Phase 1
NCT01911676	Yale University	Cognitive Impairments Associated With Schizophrenia	August 2013	Phase 2
NCT00977522	Pfizer	Schizophrenia	November 2009	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL ( 88.44 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6535 mL	13.2675 mL	26.5351 mL
5 mM	0.5307 mL	2.6535 mL	5.3070 mL
10 mM	0.2654 mL	1.3268 mL	2.6535 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.83 mg/mL (2.20 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.83 mg/mL (2.20 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 0.83 mg/mL (2.20 mM); Clear solution

* All of the co-solvents are available by MCE.