Description
PF-592379 is a potent dopamine D3 receptor agonist with an EC50 of 21 nM.
Product information
CAS Number: 710655-15-5
Molecular Weight: 235.33
Formula: C13H21N3O
Chemical Name: 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine
Smiles: C[C@H]1CO[C@@H](CN1CCC)C1C=CC(N)=NC=1
InChiKey: DFTCYTDJDXZFSK-JQWIXIFHSA-N
InChi: InChI=1S/C13H21N3O/c1-3-6-16-8-12(17-9-10(16)2)11-4-5-13(14)15-7-11/h4-5,7,10,12H,3,6,8-9H2,1-2H3,(H2,14,15)/t10-,12-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PF-592379 appears to be a full agonist (Emax=95%) when compared with the standard Pramipexole, a D2/D3 receptor agonist for the treatment of Parkinson’s disease. PF-592379 is a potent and selective dopamine 3 agonist with EC50 and Ki of 21 nM and 322 nM, respectively. In vitro binding assays show that PF-592379 (PF-592,379) selectively binds human D3 receptors with a high affinity (Ki=215 nM). Although PF-592379 also binds to human D4 receptors (Ki=4165 nM), it displays a 19-fold binding selectivity for human D3 over D4 receptors. PF-592379 fails to bind human D2 (Ki≥10 μM), D1 (Ki≥10 μM), or D5 (Ki≥10 μM) receptors at concentrations of up to 10 µM, and thus is at least 46-fold selective for D3 over D2, D1, and D5 receptors.
In Vivo:
PF-592379 is an oral dopamine 3 agonist in rat, and dog. PF-592379 has low-moderate clearance relative to liver blood flow of 6.3 and 8.5 mL/min/kg in dog and 44.8 and 58.2 mL/min/kg in rat. It has high permeability in Caco-2 cells and is completely absorbed in rat and dog pharmacokinetic studies with an oral bioavailability of 28% in both rats and 61 and 87% in the dogs.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.