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MedKoo Cat#: 526590 | Name: PF-05089771 tosylate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV. PF-05089771 exhibits a slow onset of block that is depolarization and concentration dependent, with a similarly slow recovery from block. 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.

Chemical Structure

PF-05089771 tosylate
CAS#1430806-04-4 (tosylate)

Theoretical Analysis

MedKoo Cat#: 526590

Name: PF-05089771 tosylate

CAS#: 1430806-04-4 (tosylate)

Chemical Formula: C25H20Cl2FN5O6S3

Exact Mass: 0.0000

Molecular Weight: 672.54

Elemental Analysis: C, 44.65; H, 3.00; Cl, 10.54; F, 2.82; N, 10.41; O, 14.27; S, 14.30

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 1,050.00 2 Weeks
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Related CAS #
1235403-62-9 (free base) 1430806-04-4 (tosylate)
Synonym
PF-05089771; PF05089771; PF 05089771 Tosylate
IUPAC/Chemical Name
4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-benzenesulfonamide Tosylate
InChi Key
NVKBPDYKPNYMDR-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H12Cl2FN5O3S2.C7H8O3S/c19-9-1-2-14(10(3-9)11-6-24-25-18(11)22)29-15-5-13(21)16(4-12(15)20)31(27,28)26-17-7-30-8-23-17;1-6-2-4-7(5-3-6)11(8,9)10/h1-8,26H,(H3,22,24,25);2-5H,1H3,(H,8,9,10)
SMILES Code
O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O.OS(=O)(C5=CC=C(C)C=C5)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
This study 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. Reference: Mol Pharmacol. 2016 Nov;90(5):540-548. https://pubmed.ncbi.nlm.nih.gov/27587537/
In vivo activity:
This study evaluated the antitussive effect of NaV1.7 blocker PF-05089771 administered systemically and topically in awake guinea pigs using capsaicin cough challenge. Compared to vehicle, peroral or inhaled PF-05089771 administration caused about 50-60 % inhibition of cough at the doses that did not alter respiratory rate. This study concludes that the NaV1.7 blocker PF-05089771 inhibits cough in a manner consistent with its electrophysiological effect on airway C-fibre nerve terminals. Reference: Respir Physiol Neurobiol. 2022 May;299:103856. https://pubmed.ncbi.nlm.nih.gov/35114369/
Solvent mg/mL mM comments
Solubility
DMF 33.0 49.07
DMSO 50.1 74.54
DMSO:PBS (pH 7.2) (1:4) 0.2 0.30
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 672.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Matthews RM, Bradley E, Griffin CS, Lim XR, Mullins ND, Hollywood MA, Lundy FT, McGarvey LP, Sergeant GP, Thornbury KD. Functional expression of NaV1.7 channels in freshly dispersed mouse bronchial smooth muscle cells. Am J Physiol Cell Physiol. 2022 Sep 1;323(3):C749-C762. doi: 10.1152/ajpcell.00011.2022. Epub 2022 Jul 25. PMID: 35876287. 2. Theile JW, Fuller MD, Chapman ML. 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. doi: 10.1124/mol.116.105437. Epub 2016 Sep 1. PMID: 27587537. 3. Brozmanova M, Buday T, Konarska M, Plevkova J. The effect of the voltage-gated sodium channel NaV1.7 blocker PF-05089771 on cough in the guinea pig. Respir Physiol Neurobiol. 2022 May;299:103856. doi: 10.1016/j.resp.2022.103856. Epub 2022 Jan 31. PMID: 35114369.
In vitro protocol:
1. Matthews RM, Bradley E, Griffin CS, Lim XR, Mullins ND, Hollywood MA, Lundy FT, McGarvey LP, Sergeant GP, Thornbury KD. Functional expression of NaV1.7 channels in freshly dispersed mouse bronchial smooth muscle cells. Am J Physiol Cell Physiol. 2022 Sep 1;323(3):C749-C762. doi: 10.1152/ajpcell.00011.2022. Epub 2022 Jul 25. PMID: 35876287. 2. Theile JW, Fuller MD, Chapman ML. 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. doi: 10.1124/mol.116.105437. Epub 2016 Sep 1. PMID: 27587537.
In vivo protocol:
1. Brozmanova M, Buday T, Konarska M, Plevkova J. The effect of the voltage-gated sodium channel NaV1.7 blocker PF-05089771 on cough in the guinea pig. Respir Physiol Neurobiol. 2022 May;299:103856. doi: 10.1016/j.resp.2022.103856. Epub 2022 Jan 31. PMID: 35114369.
Sun, S., J Cohen, C., & M Dehnhardt, C. (2014). Inhibitors of voltage-gated sodium channel Nav1. 7: patent applications since 2010. Pharmaceutical patent analyst, 3(5), 509-521.