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Home / Biochemicals / Small Molecules

PF-05089771

SKU : BHB21300281

A Potent and Selective Blocker of NaV1.7 Channel

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Alomone Labs

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Mfr.No.	P-315, P-315_10 mg, P-315_25 mg, P-315_5 mg, P-315_50 mg
Description	PF-05089771 (#P-315) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C18H12Cl2FN5O3S2.
Background	PF-05089771 is a synthetic arylsulfonamide compound that acts as a potent, state dependent and selective inhibitor of human NaV1.7 channel.PF-05089771 interacts with the voltage-sensor domain (VSD) of domain IV of the channel and demonstrates a strong preference for inactivated channels with inhibition that develops in a slow rate1,2. It inhibits half-inactivated human NaV1.7 channels with an IC50 of 11 nM and an IC50 of ~10 uM for resting channels1. The compound is currently being used to explore the NaV1.7 channel blockade for the treatment of acute or chronic pain conditions3,4.NaV1.7 channel plays an important role in the human pain signaling pathway and it is an important therapeutic target for treatment of chronic pain.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	10 nM - 1 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
Cas Number	1235403-62-9
Molecular Weight	500.34
Solubility	Up to 50 mM in DMSO, also soluble in methanol.Centrifuge all product preparations before use (10000 x g 5 min).
Target	NaV1.7 channels
Source	Synthetic
Activity	PF-05089771 is a novel, potent, state-dependent and selective inhibitor of NaV1.7, shown to inhibit half-inactivated human NaV1.7 channels with IC50 of 11 nM via interaction with the domain IV, and tested for clinical application in human microdose studies1-3.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: 4-(2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide.

Purity	>97%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: -20°C.

Product Manual	SDS

Reference	Alexandrou, A.J. et al. (2016) PLoS ONE 11, e0152405. Theile, J.W. et al. (2016) Mol. Pharmacol. 90, 540. Jones, H.M. et al. (2016) Clin Pharmacokinet. 55, 875. Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445. Alexandrou, A.J. et al. (2016) PLoS ONE 11, e0152405. Theile, J.W. et al. (2016) Mol. Pharmacol. 90, 540. Jones, H.M. et al. (2016) Clin Pharmacokinet. 55, 875.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300281-1	P-315_10 mg	10 mg	$117		Add to Cart
BHB21300281-2	P-315_25 mg	25 mg	$235		Add to Cart
BHB21300281-3	P-315_5 mg	5 mg	$66		Add to Cart
BHB21300281-4	P-315_50 mg	50 mg	$406		Add to Cart

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