A-803467
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MedKoo CAT#: 522388

CAS#: 944261-79-4

Description: A-803467 is a potent and selective blocker of NaV1.8 channels (IC50 values are 8, 2450, 6740, 7340 and 7380 nM for hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels respectively). A-803467 affects multiple biophysical characteristics of the canonical cardiac Nav1.5 channel and our data can be used to study potential applications of A-803467 as an antiarrhythmic drug. A-803467 attenuates spinal neuronal activity in neuropathic rats. A-803467 also attenuates neuropathic and inflammatory pain in the rat.


Chemical Structure

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A-803467
CAS# 944261-79-4

Theoretical Analysis

MedKoo Cat#: 522388
Name: A-803467
CAS#: 944261-79-4
Chemical Formula: C19H16ClNO4
Exact Mass: 357.07679
Molecular Weight: 357.79
Elemental Analysis: C, 63.78; H, 4.51; Cl, 9.91; N, 3.91; O, 17.89

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 2 Weeks
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 750.0 2 Weeks
500.0mg USD 1250.0 2 Weeks
1.0g USD 2150.0 2 Weeks
2.0g USD 3250.0 2 Weeks
5.0g USD 6750.0 2 Weeks
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Synonym: A-803467; A 803467; A803467.

IUPAC/Chemical Name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide

InChi Key: VHKBTPQDHDSBSP-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16ClNO4/c1-23-15-9-14(10-16(11-15)24-2)21-19(22)18-8-7-17(25-18)12-3-5-13(20)6-4-12/h3-11H,1-2H3,(H,21,22)

SMILES Code: O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)NC3=CC(OC)=CC(OC)=C3

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, not in water

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

Product Data:

Biological target: A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM.
In vitro activity: A-803467 changed sodium current inactivation kinetics and reduced peak sodium currents in a dose-dependent manner. The current (normalized to cell size)–voltage curves in control (DMSO) and in the presence of A-803467 at various concentrations are shown in Fig. 1D. Similar to raw current traces, the higher the A-803467 concentration, the lower the peak current density. Fig. 1E plots the peak sodium current densities at different A-803467 concentrations recorded from mouse cardiomyocytes at −30 mV. Compared to the control condition, the blocking effect of A-803467 was statistically significant at 3 and 10 µM (P<0.05 for both). Reference: Eur J Pharmacol. 2015 May 5;754:52-60. https://pubmed.ncbi.nlm.nih.gov/25701724/
In vivo activity: Systemic i.v. administration of A-803467 (10–30 mg/kg) attenuated both spontaneous and von Frey-evoked (10 g) firing of WDR neurons in SNL rats (Fig. 2). WDR responses to 10-g von Frey stimulation of the hindpaw was significantly (p < 0.05) decreased from baseline levels 5 min after injection of all doses. Spontaneous activity of WDR neurons was also significantly (p < 0.05) decreased 5 min after injection of the 20 and 30 mg/kg doses of A-803467 and remained significantly decreased for the rest of the recording period. Maximal effects were observed 35 min after injection, when 30 mg/kg of A-803467 reduced spontaneous firing by 97.7 ± 1.3% and decreased the evoked responses of WDR neurons by 94.4 ± 2.6%. At the 35-min time point, spontaneous and evoked WDR neuronal firing was also significantly (p < 0.05) attenuated by 20 mg/kg (66.2 ± 13.1% and 53.2 ± 18.4%, respectively) but not by 10 mg/kg A-803467. Reference: J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11 https://jpet.aspetjournals.org/content/324/3/1204.long

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.7 127.73
DMF 30.0 83.85
Ethanol 7.48 20.91

Preparing Stock Solutions

The following data is based on the product molecular weight 357.79 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. Anreddy N, Patel A, Zhang YK, Wang YJ, Shukla S, Kathawala RJ, Kumar P, Gupta P, Ambudkar SV, Wurpel JN, Chen ZS, Guo H. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Oncotarget. 2015 Nov 17;6(36):39276-91. doi: 10.18632/oncotarget.5747. PMID: 26515463; PMCID: PMC4770772. 2. Han Z, Jiang Y, Xiao F, Cao K, Wang DW. The effects of A-803467 on cardiac Nav1.5 channels. Eur J Pharmacol. 2015 May 5;754:52-60. doi: 10.1016/j.ejphar.2015.02.019. Epub 2015 Feb 19. PMID: 25701724. 3. Brozmanova M, Svajdova S, Pavelkova N, Muroi Y, Undem BJ, Kollarik M. The voltage-gated sodium channel NaV1.8 blocker A-803467 inhibits cough in the guinea pig. Respir Physiol Neurobiol. 2019 Dec;270:103267. doi: 10.1016/j.resp.2019.103267. Epub 2019 Aug 6. PMID: 31398537. 4. McGaraughty S, Chu KL, Scanio MJ, Kort ME, Faltynek CR, Jarvis MF. A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats. J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. doi: 10.1124/jpet.107.134148. Epub 2007 Dec 18. PMID: 18089840.
In vitro protocol: 1. Anreddy N, Patel A, Zhang YK, Wang YJ, Shukla S, Kathawala RJ, Kumar P, Gupta P, Ambudkar SV, Wurpel JN, Chen ZS, Guo H. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Oncotarget. 2015 Nov 17;6(36):39276-91. doi: 10.18632/oncotarget.5747. PMID: 26515463; PMCID: PMC4770772. 2. Han Z, Jiang Y, Xiao F, Cao K, Wang DW. The effects of A-803467 on cardiac Nav1.5 channels. Eur J Pharmacol. 2015 May 5;754:52-60. doi: 10.1016/j.ejphar.2015.02.019. Epub 2015 Feb 19. PMID: 25701724.
In vivo protocol: 1. Brozmanova M, Svajdova S, Pavelkova N, Muroi Y, Undem BJ, Kollarik M. The voltage-gated sodium channel NaV1.8 blocker A-803467 inhibits cough in the guinea pig. Respir Physiol Neurobiol. 2019 Dec;270:103267. doi: 10.1016/j.resp.2019.103267. Epub 2019 Aug 6. PMID: 31398537. 2. McGaraughty S, Chu KL, Scanio MJ, Kort ME, Faltynek CR, Jarvis MF. A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats. J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. doi: 10.1124/jpet.107.134148. Epub 2007 Dec 18. PMID: 18089840.

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1: Han Z, Jiang Y, Xiao F, Cao K, Wang DW. The effects of A-803467 on cardiac Nav1.5 channels. Eur J Pharmacol. 2015 May 5;754:52-60. doi: 10.1016/j.ejphar.2015.02.019. Epub 2015 Feb 19. PubMed PMID: 25701724.

2: Joshi SK, Honore P, Hernandez G, Schmidt R, Gomtsyan A, Scanio M, Kort M, Jarvis MF. Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models. J Pain. 2009 Mar;10(3):306-15. doi: 10.1016/j.jpain.2008.09.007. Epub 2008 Dec 13. PubMed PMID: 19070548.

3: McGaraughty S, Chu KL, Scanio MJ, Kort ME, Faltynek CR, Jarvis MF. A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats. J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. Epub 2007 Dec 18. PubMed PMID: 18089840.

4: Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. Epub 2007 May 2. PubMed PMID: 17483457; PubMed Central PMCID: PMC1895982.