PF 05089771 tosylate
Based on 4 publication(s) in Google Scholar
PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1430806-04-4
- 화학식: C25H20Cl2FN5O6S3
- 분자량:672.56
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
-
HY-19693
Cariporide
-
HY-12883
PF 05089771
-
HY-112065
PF-06869206
-
HY-12593
GS967
-
HY-B0703
Eslicarbazepine acetate
-
HY-19666
DPI 201-106
-
HY-15067
DNQX
-
HY-16787
ICA-121431
-
HY-19693R
Cariporide (Standard)
-
HY-B0703R
Eslicarbazepine acetate (Standard)
-
HY-19666R
DPI 201-106 (Standard)
-
HY-12593R
GS967 (Standard)
Publications Citing Use of MedChemExpress (MCE) PF 05089771 tosylate
More
Customer Validation & Images
-
Others
Biological Activity
IC50: 11 nM (hNav1.7), 12 nM (cynNav1.7), 13 nM (dogNav1.7), 171 nM (ratNav1.7), 8 nM (musNav1.7)[1][2].
PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4)[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1430806-04-4
-
분자량 672.56
-
화학식 C25H20Cl2FN5O6S3
-
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.
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Molecular determinant of low-voltage dependence of human Nav1.7 inactivation revealed by efficacy-based Nav1.7 selective inhibitor. [Abstract]2026 Feb 10;17(1):2559. PMID: 41667447
PF 05089771 tosylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Feb 10;17(1):2559. [Abstract]
Influence of PF-05089771 (PF-771), tetrodotoxin (TTX), lidocaine (LIDO), carbamazepine (CBZ), and lamotrigine (LTG) on ATX-induced membrane depolarization in HEK-293 cells stably expressing hNav1.7 (hNav1.7-HEK-293).
-
Nat Commun
2023 Jun 3;14(1):3224. PMID: 37270609 -
Front Pharmacol
Mechanisms Underlying Gastrodin Alleviating Vincristine-Induced Peripheral Neuropathic Pain. [Abstract]2021 Dec 16:12:744663. PMID: 34975470 -
FEBS J
Transcription factor mesenchyme homeobox protein 2 (MEOX2) modulates nociceptor function. [Abstract]2022 Jun;289(12):3457-3476. PMID: 35029322
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF 05089771 tosylate Related Classifications
HY-12883B Related Classifications
Powered by Bioz