PF-05241328 | CAS#1387633-03-5 | Nav1.7 sodium channel inhibitor

MedKoo Cat#: 530927 | Name: PF-05241328

Description:

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

PF-05241328 is a potent and selective inhibitor of Human Nav1.7 Voltage-Dependent Sodium Channel. PF-05089771 provided the best opportunity to explore Nav1.7 blockade for the treatment of acute or chronic pain conditions.

Chemical Structure

PF-05241328

CAS#1387633-03-5

Theoretical Analysis

MedKoo Cat#: 530927

Name: PF-05241328

CAS#: 1387633-03-5

Chemical Formula: C19H21ClN4O4S

Exact Mass: 436.0972

Molecular Weight: 436.91

Elemental Analysis: C, 52.23; H, 4.84; Cl, 8.11; N, 12.82; O, 14.65; S, 7.34

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 750.00	2 Weeks
10mg	USD 1,250.00	2 Weeks

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Related CAS #

No Data

Synonym

PF-05241328; PF 05241328; PF05241328; PF-5241328; PF 5241328; PF5241328.

IUPAC/Chemical Name

1-(5-Chloro-6-(2-methylpropoxy)-3-pyridinyl)-3-methyl-N-(methylsulfonyl)-1H-indazole-5-carboxamide

InChi Key

RVTSXVZXEGFIPW-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H21ClN4O4S/c1-11(2)10-28-19-16(20)8-14(9-21-19)24-17-6-5-13(7-15(17)12(3)22-24)18(25)23-29(4,26)27/h5-9,11H,10H2,1-4H3,(H,23,25)

SMILES Code

O=C(C1=CC2=C(N(C3=CC(Cl)=C(OCC(C)C)N=C3)N=C2C)C=C1)NS(=O)(C)=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

The emergence of genetic data linking Nav1.7 sodium channel over- and under- expression to human pain signalling has led to an interest in the treatment of chronic pain through inhibition of Nav1.7 channels.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PF-05241328 is an inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.

In vitro activity:

TBD

In vivo activity:

TBD

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	100.0	228.88

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 436.91 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.

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:

TBD

In vitro protocol:

TBD

In vivo protocol:

TBD

1: 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.