Nav1.7 inhibitorCAS# 1355631-24-1 |
- MK-5172 hydrate
Catalog No.:BCC1763
CAS No.:1350462-55-3
- MK-5172 sodium salt
Catalog No.:BCC1765
CAS No.:1425038-27-2
- Telaprevir (VX-950)
Catalog No.:BCC2107
CAS No.:402957-28-2
- Asunaprevir (BMS-650032)
Catalog No.:BCC1374
CAS No.:630420-16-5
- Danoprevir (RG7227)
Catalog No.:BCC2106
CAS No.:850876-88-9
- Vaniprevir
Catalog No.:BCC2030
CAS No.:923590-37-8
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1355631-24-1 | SDF | Download SDF |
PubChem ID | 56589663 | Appearance | Powder |
Formula | C15H11Cl3FNO4S | M.Wt | 426.67 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble in DMSO | ||
Chemical Name | 5-chloro-4-[(3,4-dichlorophenoxy)methyl]-2-fluoro-N-methylsulfonylbenzamide | ||
SMILES | CS(=O)(=O)NC(=O)C1=CC(=C(C=C1F)COC2=CC(=C(C=C2)Cl)Cl)Cl | ||
Standard InChIKey | VHPXWPAGHGHDCK-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C15H11Cl3FNO4S/c1-25(22,23)20-15(21)10-6-12(17)8(4-14(10)19)7-24-9-2-3-11(16)13(18)5-9/h2-6H,7H2,1H3,(H,20,21) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Nav1.7 inhibitor Dilution Calculator
Nav1.7 inhibitor Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.3437 mL | 11.7187 mL | 23.4373 mL | 46.8746 mL | 58.5933 mL |
5 mM | 0.4687 mL | 2.3437 mL | 4.6875 mL | 9.3749 mL | 11.7187 mL |
10 mM | 0.2344 mL | 1.1719 mL | 2.3437 mL | 4.6875 mL | 5.8593 mL |
50 mM | 0.0469 mL | 0.2344 mL | 0.4687 mL | 0.9375 mL | 1.1719 mL |
100 mM | 0.0234 mL | 0.1172 mL | 0.2344 mL | 0.4687 mL | 0.5859 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
Nav1.7 inhibitor is a potent Nav1.7 inhibitor.
- Schisanlignone A
Catalog No.:BCN3628
CAS No.:135557-67-4
- Cudraxanthone L
Catalog No.:BCN6187
CAS No.:135541-40-1
- AGI-5198
Catalog No.:BCC2293
CAS No.:1355326-35-0
- Mutant IDH1-IN-1
Catalog No.:BCC6403
CAS No.:1355326-21-4
- 2,3-Dihydro-12,13-dihydroxyeuparin
Catalog No.:BCN7189
CAS No.:135531-75-8
- ML 190
Catalog No.:BCC6308
CAS No.:1355244-02-8
- CYM 50260
Catalog No.:BCC6259
CAS No.:1355026-60-6
- Cabazitaxel intermediate
Catalog No.:BCN7432
CAS No.:1354900-65-4
- Araliadiol
Catalog No.:BCC8835
CAS No.:1354638-93-9
- Strontium Ranelate
Catalog No.:BCC3858
CAS No.:135459-87-9
- Rehmapicrogenin
Catalog No.:BCN8507
CAS No.:135447-39-1
- 7-O-Prenylscopoletin
Catalog No.:BCN3547
CAS No.:13544-37-1
- Pneumocandin B0
Catalog No.:BCC5436
CAS No.:135575-42-7
- Parsonsianidine
Catalog No.:BCN2109
CAS No.:135601-81-9
- Fmoc-D-His(Trt)-OH
Catalog No.:BCC3504
CAS No.:135610-90-1
- Coccineone B
Catalog No.:BCN6464
CAS No.:135626-13-0
- CP 80633
Catalog No.:BCC7463
CAS No.:135637-46-6
- 17-Methylparsonsianidine
Catalog No.:BCN2093
CAS No.:135637-68-2
- Fmoc-Cha-OH
Catalog No.:BCC3160
CAS No.:135673-97-1
- Narchinol B
Catalog No.:BCN7796
CAS No.:1356822-09-7
- ent-3-Oxokaurane-16,17-diol
Catalog No.:BCN6188
CAS No.:135683-73-7
- AZD-3463
Catalog No.:BCC3907
CAS No.:1356962-20-3
- HG-14-10-04
Catalog No.:BCC5392
CAS No.:1356962-34-9
- N-Acetylglycyl-D-glutamic acid
Catalog No.:BCC6634
CAS No.:135701-69-8
The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels.[Pubmed:27587537]
Mol Pharmacol. 2016 Nov;90(5):540-548.
Voltage-gated sodium (Nav) channel inhibitors are used clinically as analgesics and local anesthetics. However, the absence of Nav channel isoform selectivity of current treatment options can result in adverse cardiac and central nervous system side effects, limiting their therapeutic utility. Human hereditary gain- or loss-of-pain disorders have demonstrated an essential role of Nav1.7 sodium channels in the sensation of pain, thus making this channel an attractive target for new pain therapies. We previously identified a novel, state-dependent human Nav1.7 selective inhibitor (PF-05089771, IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV. We further characterized the state-dependent interaction of PF-05089771 by systematically varying the voltage, frequency, and duration of conditioning prepulses to provide access to closed, open, and fast- or slow-inactivated states. The current study demonstrates that PF-05089771 exhibits a slow onset of block that is depolarization and concentration dependent, with a similarly slow recovery from block. Furthermore, the onset of block by PF-05089771 develops with similar rates using protocols that bias channels into predominantly fast- or slow-inactivated states, suggesting that channel inhibition is less dependent on the availability of a particular inactivated state than the relative time that the channel is depolarized. Taken together, the inhibitory profile of PF-05089771 suggests that a conformational change in the domain IV VSD after depolarization is necessary and sufficient to reveal a high-affinity binding site with which PF-05089771 interacts, stabilizing the channel in a nonconducting conformation from which recovery is slow.
Safety and Efficacy of a Topical Sodium Channel Inhibitor (TV-45070) in Patients With Postherpetic Neuralgia (PHN): A Randomized, Controlled, Proof-of-Concept, Crossover Study, With a Subgroup Analysis of the Nav1.7 R1150W Genotype.[Pubmed:28266963]
Clin J Pain. 2017 Apr;33(4):310-318.
OBJECTIVE: The objective was to evaluate the safety and efficacy of TV-45070 ointment, as a treatment for postherpetic neuralgia, and to explore the response in patients with the Nav1.7 R1150W gain-of-function polymorphism. MATERIALS AND METHODS: This was a randomized, placebo-controlled, 2-period, 2-treatment crossover trial. Patients with postherpetic neuralgia with moderate or greater pain received TV-45070 and placebo ointments, each applied twice daily for 3 weeks. The primary efficacy measure was the difference in change in mean daily pain score from baseline compared with the last week of placebo and active treatment. Secondary endpoints included responder rate analyses and a further exploratory analysis of response in carriers of the Nav1.7 R1150W polymorphism was conducted. RESULTS: Seventy patients were enrolled and 54 completed the study. TV-45070 was safe and well tolerated. No statistical difference was observed between treatments for the primary endpoint. However, the proportion of patients with >/=50% reduction in mean pain scores at week 3 was greater on TV-45070 than on placebo (26.8% vs. 10.7%, P=0.0039). Similarly, a greater proportion of patients on TV-45070 had a >/=30% reduction in mean pain scores at week 3 (39.3% on TV-45070 vs. 23.2% on placebo, P=0.0784). Of note, 63% of patients with the R1150W polymorphism versus 35% of wild-type carriers had a >/=30% reduction in mean pain score on TV-45070 at week 3 (no inferential analysis performed). CONCLUSIONS: The 50% responder analysis suggests a subpopulation may exist with a more marked analgesic response to TV-45070.The trend toward a larger proportion of responders within Nav1.7 R1150W carriers warrants further investigation.
Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor.[Pubmed:28045073]
Sci Rep. 2017 Jan 3;7:39662.
Pain places a devastating burden on patients and society and current pain therapeutics exhibit limitations in efficacy, unwanted side effects and the potential for drug abuse and diversion. Although genetic evidence has clearly demonstrated that the voltage-gated sodium channel, Nav1.7, is critical to pain sensation in mammals, pharmacological inhibitors of Nav1.7 have not yet fully recapitulated the dramatic analgesia observed in Nav1.7-null subjects. Using the tarantula venom-peptide ProTX-II as a scaffold, we engineered a library of over 1500 venom-derived peptides and identified JNJ63955918 as a potent, highly selective, closed-state Nav1.7 blocking peptide. Here we show that JNJ63955918 induces a pharmacological insensitivity to pain that closely recapitulates key features of the Nav1.7-null phenotype seen in mice and humans. Our findings demonstrate that a high degree of selectivity, coupled with a closed-state dependent mechanism of action is required for strong efficacy and indicate that peptides such as JNJ63955918 and other suitably optimized Nav1.7 inhibitors may represent viable non-opioid alternatives for the pharmacological treatment of severe pain.