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A-803467

Cat. No. M2210
A-803467 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 50 In stock
50mg USD 160 In stock
200mg USD 450 In stock
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Quality Control
Biological Activity

A-803467 is a potent and selective Nav1.8 sodium channel blocker. A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is >100-fold selective vs. human Na(v)1.2, Na(v)1.3, Na(v)1.5, and Na(v)1.7 (IC50 values >or=1 microM). Administration of A-803467 (10-30 mg/kg i.v.) reduced mechanically evoked (10-g von Frey hair) and spontaneous WDR neuronal activity in SNL rats. A-803467 also dose-dependently reduced mechanical allodynia in a variety of rat pain models. A-803467 is the first small-molecule blocker of sodium channels which showing both high potency and significant subtype-selectivity among the sodium channel family.

Customer Product Validations & Biological Datas
Source Sci Rep (2017). Figure 6. A-803467
Method Measurement of LSG function
Cell Lines Left stellate ganglion
Concentrations 20 mM
Incubation Time -
Results As shown in Fig. 6A, the ganglion neurons in the DMSO group were mostly stained positive for TH (red) and negative for TUNEL (green). However, in the high-concentration A-803467 treatment group, most ganglion neurons stained positive for both TH and TUNEL.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 357.79
Formula C19H16ClNO4
CAS Number 944261-79-4
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

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.
McGaraughty S, et al. J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. PMID: 18089840.

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Jarvis MF, et al. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. PMID: 17483457.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: A-803467 supplier, Sodium Channel, inhibitors

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