TASP 0390325

Pricing Availability   Qty
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 (1)
Reviews
Literature (1)

Biological Activity for TASP 0390325

TASP 0390325 is a 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.

Compound Libraries for TASP 0390325

TASP 0390325 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for TASP 0390325

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TASP 0390325

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

Preparing Stock Solutions for TASP 0390325

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

Select a batch to recalculate based on the batch molecular weight:
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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References for TASP 0390325

References are publications that support the biological activity of the product.

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, TASP 0390325 supplier, TASP0390325, vasopressin, receptors, antagonists, antagonism, potent, selective, V1B, anxiolytic, anxiety, antidepressant, depression, Vasopressin, Receptors, 5729, Tocris Bioscience

1 Citation for TASP 0390325

Citations are publications that use Tocris products. Selected citations for TASP 0390325 include:

Campos-Lira et al (2019) Dynamic Modulation of Mouse Locus Coeruleus Neurons by Vasopressin 1a and 1b Receptors. Front Neurosci 12 919 PMID: 30618551


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.