PF-05089771
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MedKoo CAT#: 530305

CAS#: 1235403-62-9 (free base)

Description: 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.


Price and Availability

Size Price Shipping out time Quantity
200mg USD 1950 2 Weeks
500mg USD 2950 2 Weeks
1g USD 4350 2 Weeks
2g USD 6850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-30. Prices are subject to change without notice.

PF-05089771 purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530305
Name: PF-05089771
CAS#: 1235403-62-9 (free base)
Chemical Formula: C18H12Cl2FN5O3S2
Exact Mass: 498.9743
Molecular Weight: 500.3444
Elemental Analysis: C, 43.21; H, 2.42; Cl, 14.17; F, 3.80; N, 14.00; O, 9.59; S, 12.82


Related CAS #: 1235403-62-9 (free base)   1430806-04-4 (tosylate)  

Synonym: PF-05089771; PF 05089771; PF05089771; PF-05089771; PF05089771; PF 05089771.

IUPAC/Chemical Name: 4-(2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide

InChi Key: ZYSCOUXLBXGGIM-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H12Cl2FN5O3S2/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/h1-8,26H,(H3,22,24,25)

SMILES Code: O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=C(N)NN=C3)C=C1F)(NC4=CSC=N4)=O


Technical Data

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


References

1: 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. PubMed PMID: 27587537.

2: Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, Wilbrey A, Payne EC, Gutteridge A, Cox PJ, Doyle R, Printzenhoff D, Lin Z, Marron BE, West C, Swain NA, Storer RI, Stupple PA, Castle NA, Hounshell JA, Rivara M, Randall A, Dib-Hajj SD, Krafte D, Waxman SG, Patel MK, Butt RP, Stevens EB. 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. doi: 10.1371/journal.pone.0152405. PubMed PMID: 27050761; PubMed Central PMCID: PMC4822888.

3: Jones HM, Butt RP, Webster RW, Gurrell I, Dzygiel P, Flanagan N, Fraier D, Hay T, Iavarone LE, Luckwell J, Pearce H, Phipps A, Segelbacher J, Speed B, Beaumont K. Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels. Clin Pharmacokinet. 2016 Jul;55(7):875-87. doi: 10.1007/s40262-015-0365-0. PubMed PMID: 26895021.

4: Tang Z, Chen Z, Tang B, Jiang H. Primary erythromelalgia: a review. Orphanet J Rare Dis. 2015 Sep 30;10:127. doi: 10.1186/s13023-015-0347-1. Review. PubMed PMID: 26419464; PubMed Central PMCID: PMC4589109.

5: Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Review. PubMed PMID: 25060923.