NECA |
カタログ番号GC15304
One-Click Copy Product Info
|
NECAはアデノシン受容体の非選択性の作動剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 35920-39-9
Sample solution is provided at 25 µL, 10mM.
NECAはアデノシン受容体の非選択性の作動剤である[1]。NECAはアデノシン受容体を活性化することで、細胞内cAMPのレベルを調節し、よって抗炎症、血管拡張、神経活動の抑制、心臓保護、免疫調節などの多くの細胞生理プロセスを影響する[2-3]。
H9c2細胞で、NECA (0.1–10μM；20分間)は、H2O2誘発のGSK-3βリン酸化とGRP94の発見を遮断した[4]。骨格筋細胞で、NECA (100nM、10μM；19時間)はCPT1Bを調節し、LCADを刺激し、ACCβ mRNA遺伝子の発見を阻害する[5]。HREC細胞で、NECA (10μM；24-72時間)は細胞の増殖を時間依存的に増やした[6]。
低酸素性多血症マウスモデルで、NECA (0.05、0.1µmol/kg；静脈内注射；単回注射)は、低酸素性赤血球増多症のマウスで、血清エリスロポエチンのレベルを著しく増やした[7]。免疫のみのマウスで、NECA (50μL；1mM；鼻腔内投与；単回投与)の投与は、気管支肺胞洗浄液中の総細胞数（TCC）、好中球と好酸球で著しい増加を起こした[8]。
References:
[1]. Knapp C M, Foye M M, Cottam N, et al. Adenosine agonists CGS 21680 and NECA inhibit the initiation of cocaine self-administration[J]. Pharmacology Biochemistry and Behavior, 2001, 68(4): 797-803.
[2]. Elsherbiny N M, Abd El Galil K H, Gabr M M, et al. Reno-protective effect of NECA in diabetic nephropathy: implication of IL-18 and ICAM-1[J]. European Cytokine Network, 2012, 23(3): 78-86.
[3]. Li L, Chen J, Wang Z, et al. NECA alleviates inflammatory responses in diabetic retinopathy through dendritic cell toll-like receptor signaling pathway[J]. Frontiers in Immunology, 2024, 15: 1415004.
[4]. Xing F, Han H, He Y, et al. Roles of endoplasmic reticulum stress in NECA‐induced cardioprotection against ischemia/reperfusion injury[J]. Oxidative Medicine and Cellular Longevity, 2017, 2017(1): 2490501.
[5]. Haddad M. The effect of NECA, CGS 21680, PSB 603 on fatty acid transport and oxidation in skeletal muscle cells[J]. International Journal of Pharmaceutical Sciences and Research, 2016, 7(12): 4827.
[6]. Grant M B, Davis M I, Caballero S, et al. Proliferation, migration, and ERK activation in human retinal endothelial cells through A2B adenosine receptor stimulation[J]. Investigative ophthalmology & visual science, 2001, 42(9): 2068-2073.
[7]. Nakashima J, Ohigashi T, Brookins J W, et al. Effects of 5′-N-ethylcarboxamideadenosine (NECA) on erythropoietin production[J]. Kidney international, 1993, 44(4): 734-740.
[8]. El-Hashim A Z, Abduo H T, Rachid O M, et al. Intranasal administration of NECA can induce both anti-inflammatory and pro-inflammatory effects in BALB/c mice: Evidence for A2A receptor sub-type mediation of NECA-induced anti-inflammatory effects[J]. Pulmonary Pharmacology & Therapeutics, 2009, 22(3): 243-252.
| 細胞実験[1]: | |
細胞株 | H9c2細胞 |
準備方法 | 細胞をリン酸緩衝の生理食塩水（PBS）で二回洗浄し、その後は、実験の前、Tyrode溶液で2時間インキュベートした。ミトコンドリア膜電位、GSK-3βのリン酸化とGRP94に対するNECAの影響を検査する為に、細胞を800μMのH2O2に20分間暴露し、酸化損傷を起こした。広い範囲の濃度のNECA (0.1–10μM)を、H2O2への暴露の10分前に投与した。酸化損傷に対するNECA誘発の心筋保護におけるERSとcGMP/PKGシグナル伝達経路の役割を調査する研究で、細胞を0.1μM NECA/20mM 2-DG/0.1μM KT5823に20分間暴露した。2-DGとKT5823を10分間塗布し、その後細胞をNECAに暴露した。 |
反応条件 | 0.1–10μM；20分間 |
アプリケーション | NECAはH2O2誘発のGSK-3βリン酸化とGRP94の発見を遮断した。 |
| 動物実験 [2]: | |
動物モデル | 低酸素性多血症マウス（EHPCM）モデル |
準備方法 | この体内実験は、低酸素性多血症マウス（EHPCM）モデルを使い、マウスを低圧低酸素環境に長時間暴露することで赤血球増多症を誘発した。低酸素処理の終了後の3から6日目の間、NECAを静脈内または腹腔内投与し、最後に、短期間の低酸素刺激を再び投与した。その後、マウスの血液、腎臓と肝臓を採取し、血清と組織におけるEpo（エリスロポエチン）の含有量を検出し、Epo産生におけるNECAの体内調節作用を評価した。 |
投与形態 | 0.05、0.1µmol/kg；静脈内；単回注射 |
アプリケーション | NECAは、低酸素性赤血球増多症のマウスで、血清Epoレベルを著しく増やした。 |
References: | |
| Cas No. | 35920-39-9 | SDF | |
| Chemical Name | (2S,3S,4R,5S)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,4-dihydroxytetrahydrofuran-2-carboxamide | ||
| Canonical SMILES | O[C@H]1[C@@H](N2C3=NC=NC(N)=C3N=C2)O[C@H](C(NCC)=O)[C@H]1O | ||
| Formula | C12H16N6O4 | M.Wt | 308.3 |
| 溶解度 | ≥ 15.35mg/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. |
||
| 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 | 3.2436 mL | 16.218 mL | 32.4359 mL |
| 5 mM | 648.7 μL | 3.2436 mL | 6.4872 mL |
| 10 mM | 324.4 μL | 1.6218 mL | 3.2436 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)