TargetMol

PF 05089771 tosylate

Product Code:
 
TAR-T7502
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T7502-1mg1mg£116.00
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TAR-T7502-5mg5mg£163.00
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TAR-T7502-10mg10mg£203.00
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TAR-T7502-25mg25mg£400.00
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Further Information

Bioactivity:
PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50: ?10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50: 10/20 μM). PF-05089771 is also 1, 000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold.
CAS:
1430806-04-4
Formula:
C25H20Cl2FN5O6S3
Molecular Weight:
672.54
Pathway:
Membrane transporter/Ion channel
Purity:
0.98
SMILES:
Cc1ccc(cc1)S(O)(=O)=O.Nc1[nH]ncc1-c1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1cscn1
Target:
Sodium Channel

References

Alexandrou A.J., et al. Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release. PLoS One 11(4), e0152405 (2016).