MedKoo Cat#: 555384 | Name: PF-06256142

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PF-06256142 is a potent and selective orthosteric agonist of the D1 receptor with D1 EC50=30 nM and D1 binding Ki = 12 nM. PF-06256142 may be useful for treatment of Parkinson’s disease (PD) and schizophrenia. PF-06256142 has reduced receptor desensitization relative to dopamine and other catechol-containing agonists. PF-06256142 has the (+)-Enantiomer with [α]20/D = +35.2 (c 0.32, CH2Cl2). The pharmacokinetic properties of PF-06256142 such as metabolic stability, high passive permeability, and low MDR and BCRP efflux ratios make this compound suitable for oral dosing and in vivo study.

Chemical Structure

PF-06256142
CAS#1609583-14-3 (rotation +)

Theoretical Analysis

MedKoo Cat#: 555384

Name: PF-06256142

CAS#: 1609583-14-3 (rotation +)

Chemical Formula: C21H16N4O2

Exact Mass: 356.1273

Molecular Weight: 356.39

Elemental Analysis: C, 70.77; H, 4.53; N, 15.72; O, 8.98

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
1609583-14-3 (rotation +) 1609583-15-4 (rotation -) 1609580-97-3 (racemic)
Synonym
PF-06256142; PF 06256142; PF06256142;
IUPAC/Chemical Name
(+)-4-(3-Methyl-4-(6-methylimidazo[1,2-a]pyrazin-5-yl)phenoxy)furo[3,2-c]-pyridine
InChi Key
HWAIAGZSWHOLLK-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H16N4O2/c1-13-11-15(27-21-17-6-10-26-18(17)5-7-23-21)3-4-16(13)20-14(2)24-12-19-22-8-9-25(19)20/h3-12H,1-2H3
SMILES Code
CC1=CC(OC2=NC=CC3=C2C=CO3)=CC=C1C4=C(N=CC5=NC=CN45)C
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
D1 receptor signaling is deficient in a variety of psychiatric, neurological, and endocrine disorders such as Parkinson’s disease (PD) and schizophrenia.

Preparing Stock Solutions

The following data is based on the product molecular weight 356.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Davoren JE, Nason DM, Coe J, Dlugolenski K, Helal CJ, Harris AR, LaChapelle E, Liang S, Liu Y, O'Connor RE, Orozco CC, Rai BK, Salafia M, Samas BM, Xu W, Kozak R, Gray D. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15. doi: 10.1021/acs.jmedchem.8b01622. [Epub ahead of print] PubMed PMID: 30431269.