TASP0390325
Based on 1 Customer Validation
TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.
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: 99.67%
- CAS 番号: 1642187-96-9
- 分子式: C25H30Cl2FN5O4
- 分子量:554.44
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Vasopressin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
TASP0390325 shows a high affinity and potent antagonist activity for V1B receptors[1].
TASP0390325 dose-dependently inhibits [3H]-AVP binding to recombinant human V1B receptors with the IC50 value of 2.72 nM[1].
TASP0390325 also inhibits [3H]-AVP binding to rat anterior pituitary membranes, with the IC50 value of 2.22 nM[1].
TASP0390325 potently attenuates the 2.5 nM AVP-induced increase in [Ca2+]i, with IC50 values of and 20.2 nM[1].
Pretreatment with TASP0390325 inhibits the retention of 11C-TASP699 in a dose-dependent manner. Binding of 11C-TASP699 to monkey pituitary slices is specifically localized to the anterior lobe. The radioligand binding is inhibited by TASP0390325 in a concentration-dependent manner. The IC50 value of TASP0390325 is 2.16 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Oral administration of TASP0390325 also exerts antidepressant effects in two models of depression (a forced swimming test and an olfactory bulbectomy model)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley (SD) rats (211-246 g)[1]
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Dosage:0.3 and 1 mg/kg (TASP0390325 is suspended in 0.5% methylcellulose 400)
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Administration:Oral administration
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Result:Antagonized the increase in plasma ACTH levels induced by CRF/dDAVP in rats at a dose of 1 mg/kg. In contrast, 0.3 and 1.0 mg/kg itself did not significantly affect basal ACTH levels.
化学情報
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CAS 番号 1642187-96-9
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性状 Solid
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分子量 554.44
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分子式 C25H30Cl2FN5O4
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Color White to off-white
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SMILES
O=C(CN1C(C2=CC(OCCCN3CCOCC3)=CN=C2N=C1C4=CC=C(C(Cl)=C4)F)=O)NC(C)C.Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 50 mg/mL (90.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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
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データシート (274 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. M Iijima, et al. Antidepressant and anxiolytic profiles of newly synthesized arginine vasopressin V1B receptor antagonists: TASP0233278 and TASP0390325. Br J Pharmacol. 2014 Jul;171(14):3511-25. [Content Brief]
[2]. Kazumi Koga, et al. High-Contrast PET Imaging of Vasopressin V 1B Receptors with a Novel Radioligand, 11C-TASP699. J Nucl Med. 2017 Oct;58(10):1652-1658. [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 (sealed storage, away from moisture). 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 | 1.8036 mL | 9.0181 mL | 18.0362 mL | 45.0905 mL |
| 5 mM | 0.3607 mL | 1.8036 mL | 3.6072 mL | 9.0181 mL | |
| 10 mM | 0.1804 mL | 0.9018 mL | 1.8036 mL | 4.5091 mL | |
| 15 mM | 0.1202 mL | 0.6012 mL | 1.2024 mL | 3.0060 mL | |
| 20 mM | 0.0902 mL | 0.4509 mL | 0.9018 mL | 2.2545 mL | |
| 25 mM | 0.0721 mL | 0.3607 mL | 0.7214 mL | 1.8036 mL | |
| 30 mM | 0.0601 mL | 0.3006 mL | 0.6012 mL | 1.5030 mL | |
| 40 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 1.1273 mL | |
| 50 mM | 0.0361 mL | 0.1804 mL | 0.3607 mL | 0.9018 mL | |
| 60 mM | 0.0301 mL | 0.1503 mL | 0.3006 mL | 0.7515 mL | |
| 80 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5636 mL |
TASP0390325 関連分類
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