JP1302
Based on 2 publication(s) in Google Scholar
JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.68%
- CAS 番号: 80259-18-3
- 分子式: C24H24N4
- 分子量:368.47
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 JP1302
MoreAdrenergic Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
|
human α2C-adrenoceptor 28±2 nM (Ki) |
human α2B-adrenoceptor 1470±130 nM (Ki) |
human α2A-adrenoceptor 3150±50 nM (Ki) |
rodent α2D-adrenoceptor 1700±200 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
6.76 μM
Compound: GNF-Pf-3427
|
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
|
[PMID: 18579783] |
JP1302 shows about 100-fold higher affinity than for α2A or α2B[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JP1302 (5 μmol/kg, once) is capable of complete reversal of the impairment in PPI induced in Sprague-Dawley rats by the psychotomimetic NMDA receptor antagonist, phencyclidine and similar results are found in Wistar rats[1].
JP1302 (3 mg/kg, IV, once) significantly ameliorates renal dysfunction[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Sprague Dawley rats (8 weeks old)[3]
-
Dosage:3 mg/kg
-
Administration:IV, pre-treatment: administered 5 min before the induction of ischemia, post-treatment: injected 45 min after the initiation of reperfusion
-
Result:Significantly ameliorated renal dysfunction in the rats at 24 h after reperfusion. post-ischemic administration of JP-1302 significantly ameliorated renal dysfunction, histological damage and reduced apoptotic cells and pro-inflammatory cytokine mRNA expression.
化学情報
-
CAS 番号 80259-18-3
-
性状 Solid
-
分子量 368.47
-
分子式 C24H24N4
-
Color Brown to red
-
SMILES
CN1CCN(C2=CC=C(NC3=C(C=CC=C4)C4=NC5=CC=CC=C53)C=C2)CC1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Cell Rep Med
The sympathetic nervous system drives hyperinflammatory responses to Clostridioides difficile infection. [Abstract]2024 Oct 15;5(10):101771. PMID: 39368481 -
iScience
2026 Feb 23;29(3):115122. PMID: 41852725
溶剤 & 溶解度
DMSO : 50 mg/mL (135.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Tricklebank MD, et al. JP-1302: a new tool to shed light on the roles of alpha2C-adrenoceptors in brain. Br J Pharmacol. 2007 Feb;150(4):381-2. [Content Brief]
[2]. Sallinen J, et al. Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302. Br J Pharmacol. 2007 Feb;150(4):391-402. [Content Brief]
[3]. Shimokawa T, et al. Post-treatment with JP-1302 protects against renal ischemia/reperfusion-induced acute kidney injury in rats. J Pharmacol Sci. 2019 Mar;139(3):137-142. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7139 mL | 13.5696 mL | 27.1393 mL | 67.8481 mL |
| 5 mM | 0.5428 mL | 2.7139 mL | 5.4279 mL | 13.5696 mL | |
| 10 mM | 0.2714 mL | 1.3570 mL | 2.7139 mL | 6.7848 mL | |
| 15 mM | 0.1809 mL | 0.9046 mL | 1.8093 mL | 4.5232 mL | |
| 20 mM | 0.1357 mL | 0.6785 mL | 1.3570 mL | 3.3924 mL | |
| 25 mM | 0.1086 mL | 0.5428 mL | 1.0856 mL | 2.7139 mL | |
| 30 mM | 0.0905 mL | 0.4523 mL | 0.9046 mL | 2.2616 mL | |
| 40 mM | 0.0678 mL | 0.3392 mL | 0.6785 mL | 1.6962 mL | |
| 50 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3570 mL | |
| 60 mM | 0.0452 mL | 0.2262 mL | 0.4523 mL | 1.1308 mL | |
| 80 mM | 0.0339 mL | 0.1696 mL | 0.3392 mL | 0.8481 mL | |
| 100 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6785 mL |