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.
Product information
CAS Number: 1449473-97-5
Molecular Weight: 274.36
Formula: C15H22N4O
Chemical Name: (2R,3S)-3-amino-3-(5-tert-butyl-1H-1,3-benzodiazol-2-yl)-2-methylpropanamide
Smiles: C[C@H]([C@H](N)C1NC2=CC=C(C=C2N=1)C(C)(C)C)C(N)=O
InChiKey: APWZIFIAVVFPNT-PELKAZGASA-N
InChi: InChI=1S/C15H22N4O/c1-8(13(17)20)12(16)14-18-10-6-5-9(15(2,3)4)7-11(10)19-14/h5-8,12H,16H2,1-4H3,(H2,17,20)(H,18,19)/t8-,12+/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (182.24 mM; Need ultrasonic).
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-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.
Products are for research use only. Not for human use.
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