PF-01247324

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

MedKoo CAT#: 532458

CAS#: 875051-72-2

Description: PF-01247324 is a novel selective and orally bioavailable Nav 1.8 channel blocker, attenuates nociception and sensory neuron excitability.


Chemical Structure

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PF-01247324
CAS# 875051-72-2

Theoretical Analysis

MedKoo Cat#: 532458
Name: PF-01247324
CAS#: 875051-72-2
Chemical Formula: C13H10Cl3N3O
Exact Mass: 328.99
Molecular Weight: 330.593
Elemental Analysis: C, 47.23; H, 3.05; Cl, 32.17; N, 12.71; O, 4.84

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: PF-01247324; PF 01247324; PF01247324.

IUPAC/Chemical Name: 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide

InChi Key: HPIUHDCRVYDAEJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H10Cl3N3O/c1-18-13(20)10-3-2-7(12(17)19-10)8-4-6(14)5-9(15)11(8)16/h2-5H,1H3,(H2,17,19)(H,18,20)

SMILES Code: O=C(C1=NC(N)=C(C2=CC(Cl)=CC(Cl)=C2Cl)C=C1)NC

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:
Biological target: PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
In vitro activity: The inhibition of Nav 1.8 channels by PF-01247324 was studied using in vitro patch-clamp electrophysiology and the oral bioavailability and antinociceptive effects demonstrated using in vivo rodent models of inflammatory and neuropathic pain. PF-01247324 inhibited native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50 : 331 nM) and in recombinantly expressed h Nav 1.8 channels (IC50 : 196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav 1.5 channels (IC50 : ∼10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50 : ∼10-18 μM). Native TTX-R currents in small-diameter rodent DRG neurons were inhibited with an IC50 448 nM, and the block of both human recombinant Nav 1.8 channels and TTX-R from rat DRG neurons was both frequency and state dependent. In vitro current clamp showed that PF-01247324 reduced excitability in both rat and human DRG neurons and also altered the waveform of the action potential. Reference: Br J Pharmacol. 2015 May;172(10):2654-70. https://pubmed.ncbi.nlm.nih.gov/25625641/
In vivo activity: The present study assessed the effect of per os (p.o.) dosing of a new orally bioavailable Nav1.8-selective blocker, PF-01247324, in transgenic mice expressing Nav1.8 in Purkinje neurons, and in wildtype mice in the experimental autoimmune encephalomyelitis (EAE) model. PF-01247324 was administered by oral gavage at 1000 mg/kg; control groups received an equal volume of vehicle. Behavioral assays of motor coordination, grip strength, and ataxia were performed. This study observed significant improvements in motor coordination and cerebellar-like symptoms in mice that received PF-01247324 compared to control littermates that received vehicle. Reference: PLoS One. 2015 Mar 6;10(3):e0119067. https://pubmed.ncbi.nlm.nih.gov/25747279/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.0 90.75
Ethanol 30.0 90.75
Ethanol:PBS (pH 7.2) (1:4) 0.2 0.60

Preparing Stock Solutions

The following data is based on the product molecular weight 330.59 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. Payne CE, Brown AR, Theile JW, Loucif AJ, Alexandrou AJ, Fuller MD, Mahoney JH, Antonio BM, Gerlach AC, Printzenhoff DM, Prime RL, Stockbridge G, Kirkup AJ, Bannon AW, England S, Chapman ML, Bagal S, Roeloffs R, Anand U, Anand P, Bungay PJ, Kemp M, Butt RP, Stevens EB. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. doi: 10.1111/bph.13092. Epub 2015 Apr 10. PMID: 25625641; PMCID: PMC4409913. 2. Shields SD, Butt RP, Dib-Hajj SD, Waxman SG. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. doi: 10.1371/journal.pone.0119067. PMID: 25747279; PMCID: PMC4352054.
In vitro protocol: 1. Payne CE, Brown AR, Theile JW, Loucif AJ, Alexandrou AJ, Fuller MD, Mahoney JH, Antonio BM, Gerlach AC, Printzenhoff DM, Prime RL, Stockbridge G, Kirkup AJ, Bannon AW, England S, Chapman ML, Bagal S, Roeloffs R, Anand U, Anand P, Bungay PJ, Kemp M, Butt RP, Stevens EB. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. doi: 10.1111/bph.13092. Epub 2015 Apr 10. PMID: 25625641; PMCID: PMC4409913.
In vivo protocol: 1. Shields SD, Butt RP, Dib-Hajj SD, Waxman SG. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. doi: 10.1371/journal.pone.0119067. PMID: 25747279; PMCID: PMC4352054.

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1: Shields SD, Butt RP, Dib-Hajj SD, Waxman SG. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. doi: 10.1371/journal.pone.0119067. eCollection 2015. PubMed PMID: 25747279; PubMed Central PMCID: PMC4352054.

2: Payne CE, Brown AR, Theile JW, Loucif AJ, Alexandrou AJ, Fuller MD, Mahoney JH, Antonio BM, Gerlach AC, Printzenhoff DM, Prime RL, Stockbridge G, Kirkup AJ, Bannon AW, England S, Chapman ML, Bagal S, Roeloffs R, Anand U, Anand P, Bungay PJ, Kemp M, Butt RP, Stevens EB. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. doi: 10.1111/bph.13092. Epub 2015 Apr 10. PubMed PMID: 25625641; PubMed Central PMCID: PMC4409913.