1. Membrane Transporter/Ion Channel
  2. Sodium Channel

PF-06305591 

Cat. No.: HY-114301
Handling Instructions

PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.

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

PF-06305591 Chemical Structure

PF-06305591 Chemical Structure

CAS No. : 1449473-97-5

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5 mg USD 180 Get quote

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  • Biological Activity

  • Technical Information

  • References

Description

PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile[1].

IC50 & Target

IC50: 15 nM (NaV1.8)[1].

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[1].

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[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6448 mL 18.2242 mL 36.4485 mL
5 mM 0.7290 mL 3.6448 mL 7.2897 mL
10 mM 0.3645 mL 1.8224 mL 3.6448 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

274.36

Formula

C₁₅H₂₂N₄O

CAS No.

1449473-97-5

SMILES

CC(C)(C)C1=CC=C(NC([[email protected]]([[email protected]@H](C)C(N)=O)N)=N2)C2=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-06305591
Cat. No.:
HY-114301
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PF-06305591

Cat. No.: HY-114301