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Purity: ≥98%
A-803467 (A803467; A 803467) is a novel, potent and selective NaV1.8 sodium channel blocker with potential analgesic effects. It inhibits NaV1.8 sodium channel with an IC50 of 8 nM, and exhibits >100-fold more selectivity over human Nav1.2, 1.3, 1.5 and 1.7. A-803467 inhibits hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels with IC50 values of 8, 2450, 6740, 7340 and 7380 nM, 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.
| ln Vitro |
A-803467 reverses the multidrug resistance mediated by ABCG2 in a selective and significant manner. In cell lines transfected with ABCG2, A-803467 (7.5 μM) considerably amplifies the cytotoxicity of mitoxantrone and topotecan. MX build-up in cells transfected with ABCG2. At varying time intervals, A-803467 (7.5 μM; 0~120 minutes) substantially inhibits the intracellular [3H]-MX efflux from ABCG2-transfected cells. A-803467 increases ABCG2's ATPase activity[1].
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| ln Vivo |
In male NCR nude mice, A-803467 (35 mg/kg; po) exhibits no discernible toxicity[1]. When A-803467 and topotecan are combined, the growth of tumors in mice implanted with H460/MX20 cells that overexpress ABCG2 is greatly reduced. Restoring the sensitivity of cancers overexpressing the ABCG2 transporter to topotecan is accomplished by -803467, but tumors lacking ABCG2 expression are not significantly affected[1].
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| Animal Protocol |
Animal/Disease Models: Nude mice[1]
Doses: 35 mg/kg Route of Administration: Po Experimental Results: demonstrated no noticeable toxicity in the male NCR nude mice. |
| References |
[1]. Anreddy N, et al. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Oncotarget. 2015;6(36):39276-39291.
[2]. Jarvis MF, et al. 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;104(20):8520-8525. |
| Molecular Formula |
C19H16CLNO4
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| Molecular Weight |
357.79
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| CAS # |
944261-79-4
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| Related CAS # |
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| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C1=C([H])C([H])=C(C(N([H])C2C([H])=C(C([H])=C(C=2[H])OC([H])([H])[H])OC([H])([H])[H])=O)O1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7949 mL | 13.9747 mL | 27.9494 mL | |
| 5 mM | 0.5590 mL | 2.7949 mL | 5.5899 mL | |
| 10 mM | 0.2795 mL | 1.3975 mL | 2.7949 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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