A-803467 |
Catalog No.GC15701
One-Click Copy Product Info
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A-803467 is a tetrodotoxin-resistant Nav1.8 sodium channel blocker which can block human Nav1.8 with an IC50 of 8nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 944261-79-4
Sample solution is provided at 25 µL, 10mM.
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A-803467 is a tetrodotoxin-resistant Nav1.8 sodium channel blocker which can block human Nav1.8 with an IC50 of 8nM [1, 2]. A-803467 can effectively block experimental inflammatory and neuropathic pain caused by the Nav1.8 channel [1].
A-803467 (7.5μM; 2h) enhanced the intracellular [3H]-MX accumulation in ABCG2-transfected HEK293 cells [2]; A-803467 (7.5μM; 0, 30, 60, 120min) significantly blocked the intracellular [3H]-MX efflux from ABCG2-transfected cells [2]; A-803467 (100nM) caused significant current blocking in HEK-293 cells expressing the human Nav1.8 sodium channel [1]; A-803467 (30nM) shortened action potential in mouse ventricular myocytes at slow frequency (0.1Hz) stimulus current [3]; A-803467 (30nM; 15min) reduced frequency of diastolic Ca2+ waves in human atrial cardiomyocytes from patients with sinus rhythm [4].
A-803467 (10, 30, 100mg/kg; i.p.) potently reduced thermal hyperalgesia in the complete Freund’s adjuvant (CFA) Sprague-Dawley (SD) rat model of inflammatory pain [1]; A-803467 (10, 30, 100mg/kg; i.p.) reduced mechanical allodynia in the L5/L6 spinal nerve injury model of SD rats [1]; A-803467 (10, 30, 100mg/kg; i.p.) reduced mechanical allodynia in the chronic constriction injury of the sciatic nerve model of SD rats [1]; A-803467 (10mg/rat; i.a.) reduced joint pain of male Wistar rats which induced by monoiodoacetate (MIA) [5].
References:
[1] Jarvis M F, Honore P, Shieh C C, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat [J]. Proceedings of the National Academy of Sciences of the United States of America, 2007, 104(20): 8520-8525.
[2] Anreddy N, Patel A, Zhang Y K, et al. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo [J]. Oncotarget, 2015, 6(36): 39276-39291.
[3] Yang T, Atack T C, Stroud D M, et al. Blocking Scn10a channels in heart reduces late sodium current and is antiarrhythmic [J]. Circulation research, 2012, 111(3): 322-332.
[4] Pabel S, Ahmad S, Tirilomis P, et al. Inhibition of Nav1.8 prevents atrial arrhythmogenesis in human and mice [J]. Basic research in cardiology, 2020, 115(2): 20.
[5] Schuelert N, McDougall J J. Involvement of Nav1.8 sodium ion channels in the transduction of mechanical pain in a rodent model of osteoarthritis [J]. Arthritis research & therapy, 2012, 14(1): R5.
| Cell experiment [1]: | |
Cell lines | HEK293 |
Preparation Method | ABCG2-transfected cells were established by transfecting HEK293 cell with pcDNA3.1 vector containing a full-length ABCG2, and then ABCG2-transfected cells were incubated with [3H]-MX (a kind of substrate of ABCG2), with or without 7.5μM A-803467 for 2h. |
Reaction Conditions | 7.5μM; 2h |
Applications | A-803467 significantly enhanced the intracellular [3H]-MX accumulation in ABCG2-transfected cells. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Unilateral inflammation of rats was induced by injecting CFA (complete Freund’s adjuvant), A-803467 was injected 90min after CFA injection, the behavioral testing for thermal hyperalgesia was conducted 2d later. |
Dosage form | 10, 30, 100mg/kg; i.p. |
Applications | A-803467 potently reduced thermal hyperalgesia in the CFA model of inflammatory pain. |
[1] Anreddy N, Patel A, Zhang Y K, et al. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo [J]. Oncotarget, 2015, 6(36): 39276-39291. | |
| Cas No. | 944261-79-4 | SDF | |
| Chemical Name | 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide | ||
| Canonical SMILES | COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC | ||
| Formula | C19H16ClNO4 | M.Wt | 357.79 |
| Solubility | ≥ 13.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7949 mL | 13.9747 mL | 27.9494 mL |
| 5 mM | 559 μL | 2.7949 mL | 5.5899 mL |
| 10 mM | 279.5 μL | 1.3975 mL | 2.7949 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)