TASP 0390325

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Cat.No. 5729 - TASP 0390325 | C25H29ClFN5O4.HCl | CAS No. 1642187-96-9
Description: Potent and selective V1B receptor antagonist; orally bioavailable
Chemical Name: 2-(3-Chloro-4-fluorophenyl)-N-(1-methylethyl)-6-[3-(4-morpholinyl)propoxy]-4-oxo-pyrido[2,3-d]pyrimidine-3(4H)-acetamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective V1B receptor antagonist (IC50 = 2.22 nM for rat pituitary receptor). Exhibits no significant affinity for 85 other receptors, ion channels and transporters at 10 μM, including V1A and V2. Increases ACTH levels in rats. Orally bioavailable. Antidepressant and anxiolytic.

Technical Data

M. Wt 554.44
Formula C25H29ClFN5O4.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1642187-96-9
PubChem ID 86765292
InChI Key NUIXGNLBPARAII-UHFFFAOYSA-N
Smiles O=C(NC(C)C)CN1C(C2=CC(OCCCN3CCOCC3)=CN=C2N=C1C4=CC=C(F)C(Cl)=C4)=O.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 55.44 100
DMSO 55.44 100

Preparing Stock Solutions

The following data is based on the product molecular weight 554.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.8 mL 9.02 mL 18.04 mL
5 mM 0.36 mL 1.8 mL 3.61 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Iijima et al (2014) Antidepressant and anxiolytic profiles of newly synthesized arginine vasopressin V1B receptor antagonists: TASP0233278 and TASP0390325. Br J Pharmacol. 171 3511 PMID: 24654684


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Keywords: TASP 0390325, supplier, TASP0390325, vasopressin, receptors, antagonists, antagonism, potent, selective, V1B, anxiolytic, antidepressant, Vasopressin, Receptors, Vasopressin, Receptors, Tocris Bioscience

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