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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.67%
- CAS. Nr.: 1642187-96-9
- Formel: C25H30Cl2FN5O4
- Molecular Weight:554.44
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Speicherung:
-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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 1642187-96-9
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Appearance Solid
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Molecular Weight 554.44
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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 |
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