PF 05089771 tosylate

Cat. No.: HY-12883B: Data Sheet Handling Instructions
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PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Na_v1.7 inhibitor, with IC₅₀ values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa_v1.7, cynNa_v1.7, dogNa_v1.7, ratNa_v1.7, and musNa_v1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.

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PF 05089771 tosylate 화학구조

CAS No. : 1430806-04-4

사이즈	재고	수량
1 mg	견적 받기 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
5 mg	견적 받기 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
10 mg	견적 받기 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
50 mg	견적 받기
100 mg	견적 받기

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고객리뷰

Based on 4 publication(s) in Google Scholar

Other Forms of PF 05089771 tosylate:

PF 05089771 In-stock

4 Publications Citing Use of MCE PF 05089771 tosylate

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

IC50: 11 nM (hNa_v1.7), 12 nM (cynNa_v1.7), 13 nM (dogNa_v1.7), 171 nM (ratNa_v1.7), 8 nM (musNa_v1.7)^[1]^[2].

In Vitro

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Na_v1.2 to 900-fold for Na_v1.3 and Na_v1.4)^[1].
PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5) whilst 100 nM resulted in complete block^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

672.56

화학식

C₂₅H₂₀Cl₂FN₅O₆S₃

CAS No.

1430806-04-4

SMILES

O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=C(N)NN=C3)C=C1F)(NC4=CSC=N4)=O.CC5=CC=C(S(O)(=O)=O)C=C5

선적

Room temperature in continental US; may vary elsewhere.

보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. [Content Brief]

[2]. Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548. [Content Brief]