| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TASP0390325 targets the arginine vasopressin receptor 1B (V1B receptor). It is a potent and selective V1B receptor antagonist. It has an IC50 of 2.22 nM for the rat pituitary receptor. It has no significant affinity for V1A and V2 receptors at 10 μM. By blocking V1B receptors, it modulates the stress response and HPA axis activity.
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| ln Vitro |
At the V1B receptor, TASP0390325 has strong antagonistic action and high affinity [1]. With an IC50 value of 2.72 nM, TASP0390325 dose-dependently inhibits [3H]-AVP binding to recombinant human V1B receptor[1]. At an IC50 value of 2.22 nM, TASP0390325 also prevents [3H]-AVP from binding to the rat anterior pituitary membrane[1]. With IC50 values of 20.2 nM and 20.2 nM, TASP0390325 efficiently attenuates the [Ca2+]i rise caused by 2.5 nM AVP[1]. Pretreatment with TASP0390325 decreases 11C-TASP699 retention in a dose-dependent way. Anterior lobe specific localization is observed upon binding of 11C-TASP699 to monkey pituitary slices. TASP0390325 exhibits concentration-dependent inhibition of radioligand binding. TASP0390325 has an IC50 value of 2.16 nM[2].
TASP0390325 is a potent and selective V1B receptor antagonist in vitro. It has an IC50 of 2.22 nM for the rat pituitary receptor. It shows no significant affinity for 85 other receptors, ion channels, and transporters at 10 μM, including V1A and V2. Specific details on assay conditions are not extensively provided. |
| ln Vivo |
In vivo, anterior pituitary V1B receptors are blocked by TASP0390325. The increase in plasma ACTH levels in rats produced by CRF/dDAVP was counteracted by oral treatment of TASP0390325, suggesting that TASP0390325 inhibits anterior pituitary V1B receptors in vivo. TASP0390325 (1 mg/kg) strongly inhibits the production of plasma ACTH in rats induced by CRF/dDAVP[1]. The forced swim test and the olfactory bulbectomy model are two depression models in which oral treatment of TASP0390325 also has antidepressant effects [1].
In vivo, TASP0390325 increases ACTH levels in rats. It has antidepressant and anxiolytic activities in rodents. It is orally active. Specific in vivo efficacy data, including dosing regimens and detailed behavioral results, are not extensively provided in the available literature. |
| Enzyme Assay |
In vitro receptor binding assays for TASP0390325 involve measuring affinity for the V1B receptor. Membrane preparations from rat pituitary or cells expressing recombinant V1B receptors are incubated with radiolabeled ligands and varying concentrations of TASP0390325. Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is collected by filtration and quantified by scintillation counting. IC50 values are calculated from competition curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing V1B receptors are cultured and treated with TASP0390325 at various concentrations. Receptor antagonism is measured by assessing inhibition of agonist-induced signaling pathways, such as calcium mobilization or cAMP accumulation. Cell viability is assessed using standard assays.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (211-246 g) [1]
Doses: 0.3 and 1 mg/kg (TASP0390325 suspended in 0.5% Methylcellulose 400) Route of Administration: Oral Experimental Results:Antagonism Plasma ACTH increased to levels induced in rats by a dose of 1 mg/kg CRF/dDAVP. In contrast, 0.3 and 1.0 mg/kg did not Dramatically affect basal ACTH levels by themselves. In vivo animal studies for TASP0390325 typically use rodent models to assess antidepressant and anxiolytic activity. The compound is administered orally at doses determined from pharmacokinetic studies. Behavioral tests such as the forced swim test, tail suspension test, or elevated plus maze are used to assess antidepressant and anxiolytic effects. ACTH levels are measured in plasma. |
| ADME/Pharmacokinetics |
TASP0390325 (CAS 1642187-96-9) has a molecular formula of C25H29ClFN5O4·HCl and a molecular weight of 554.44. It is a potent and orally active small molecule. It should be stored at -20°C. Detailed pharmacokinetic parameters are not extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for TASP0390325 are not extensively provided. As a V1B receptor antagonist, it would be expected to have a safety profile related to modulation of the stress response. The compound is for research use only. Standard toxicology assessments would be required for therapeutic development.
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| References |
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| Additional Infomation |
TASP0390325 is a potent and selective V1B receptor antagonist with an IC50 of 2.22 nM. It increases ACTH levels in rats and has antidepressant and anxiolytic activities in rodents. It has the potential use as an antidepressant and anxiolytic. No approved therapeutic status is reported.
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| Molecular Formula |
C25H30CL2FN5O4
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| Molecular Weight |
554.441207408905
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| Exact Mass |
553.165
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| CAS # |
1642187-96-9
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| PubChem CID |
86765292
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
796
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)NC(=O)CN1C(=NC2=C(C1=O)C=C(C=N2)OCCCN3CCOCC3)C4=CC(=C(C=C4)F)Cl.Cl
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| InChi Key |
NUIXGNLBPARAII-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H29ClFN5O4.ClH/c1-16(2)29-22(33)15-32-24(17-4-5-21(27)20(26)12-17)30-23-19(25(32)34)13-18(14-28-23)36-9-3-6-31-7-10-35-11-8-31;/h4-5,12-14,16H,3,6-11,15H2,1-2H3,(H,29,33);1H
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| Chemical Name |
2-[2-(3-chloro-4-fluorophenyl)-6-(3-morpholin-4-ylpropoxy)-4-oxopyrido[2,3-d]pyrimidin-3-yl]-N-propan-2-ylacetamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~180.36 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8036 mL | 9.0181 mL | 18.0362 mL | |
| 5 mM | 0.3607 mL | 1.8036 mL | 3.6072 mL | |
| 10 mM | 0.1804 mL | 0.9018 mL | 1.8036 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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