A-803467 |
カタログ番号GC15701
One-Click Copy Product Info
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A-803467はテトロドトキシン耐性のNav1.8ナトリウムチャネル遮断剤であり、8nMのIC50でヒトNav1.8を遮断できる。
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はテトロドトキシン耐性のNav1.8ナトリウムチャネル遮断剤であり、8nMのIC50でヒトNav1.8を遮断できる[1, 2]。A-803467は、Nav1.8チャネルによる実験性炎症と神経痛を効果的に遮断できる[1]。
ABCG2遺伝子導入HEK293細胞で、A-803467 (7.5μM；2時間)は細胞内[3H]-MXの蓄積を増強した[2]；A-803467 (7.5μM；0、30、60、120分間)は、ABCG2遺伝子導入の細胞から、細胞内[3H]-MXの流出を著しく遮断した[2]；A-803467 (100nM)は、ヒトNav1.8ナトリウムチャネルを発見するHEK-293細胞で、著しい電流遮断を起こした[1]；A-803467 (30nM)は、低周波（0.1Hz）刺激電流で、マウス心室筋細胞で、活動電位を短くした[3]；A-803467 (30nM；15分間)は、洞調律の患者から、ヒト心房心筋細胞における拡張期Ca2+波の頻度を減らした[4]。
A-803467 (10、30、100mg/kg；腹腔内注射)は炎症疼痛の完全Freundアジュバント（CFA）Sprague-Dawley（SD）ラットモデルで、温熱性痛覚過敏を有力に減らした[1]；A-803467 (10、30、100mg/kg；腹腔内注射)は、SDラットのL5/L6脊髄神経損傷モデルで、機械的異痛症を減らした[1]；A-803467 (10、30、100mg/kg；腹腔内注射)は、SDラットの坐骨神経の慢性狭窄損傷モデルで、機械的異痛症を減らした[1]；A-803467 (10mg/rat; i.a.)は、モノヨード酢酸（MIA）による、雄のWistarラットの関節痛を減らした[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.
| 細胞実験[1]: | |
細胞株 | HEK293 |
準備方法 | ABCG2遺伝子導入細胞を、全長ABCG2遺伝子を含有するpcDNA3.1ベクターをHEK293細胞に遺伝子導入することで作成し、続いてABCG2遺伝子導入細胞を、7.5μM A-803467のある/ない状態で、[3H]-MX (ABCG2の基質の一種)と2時間インキュベートした。 |
反応条件 | 7.5μM；2時間 |
アプリケーション | ABCG2遺伝子導入の細胞で、A-803467は細胞内[3H]-MXの蓄積を著しく増強した。 |
| 動物実験 [2]: | |
動物モデル | 雄のSprague-Dawleyラット |
準備方法 | CFA（完全Freundアジュバント）を注射することで、ラットの片側性炎症を誘発した。CFA注射の90分後に、A-803467をCFA注射の90分後に注射し、2日後に、温熱性痛覚過敏の行動試験を行った。 |
投与形態 | 10、30、100mg/kg；腹腔内注射 |
アプリケーション | A-803467は炎症疼痛のCFAモデルで、温熱性痛覚過敏を有力に減らした。 |
[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 |
| 溶解度 | ≥ 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 | |||
|
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)
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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.)