PF-06305591( PF06305591 | PF 06305591 )

Catalog No. M11932 CAS No. 1449473-97-5

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Datasheet

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HPLC

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Product Name

PF-06305591
Note

Research use only, not for human use.
Brief Description

PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels.
Description

PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels; displays excellent preclinical in vitro ADME and safety profile.Pain Phase 1 Discontinued.
In Vitro

PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability.
In Vivo

PF-06305591 (compound 9) has good rat bioavailability. PF-06305591 offers the possibility of investigating higher IC50 multiples of Nav1.8 blockade in the clinic, and therefore a more thorough evaluation of the role of NaV1.8 in the treatment of pain.
Synonyms

PF06305591 | PF 06305591
Pathway

Membrane Transporter/Ion Channel
Target

Sodium Channel
Recptor

Sodium Channel
Research Area

Neurological Disease
Indication

Pain

CAS Number

1449473-97-5
Formula Weight

274.368
Molecular Formula

C15H22N4O
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 140 mg/mL (510.28 mM)
SMILES

CC(C(C1=NC2=C(N1)C=C(C=C2)C(C)(C)C)N)C(=O)N
Chemical Name

(2R,3S)-3-amino-3-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)-2-methylpropanamide

1. Brown AD, et al. Bioorg Med Chem. 2019 Jan 1;27(1):230-239.

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