2. GPCR/G Protein
  3. Vasopressin Receptor
  4. TASP0390325

TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.

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TASP0390325 Chemical Structure

TASP0390325 Chemical Structure

CAS No. : 1642187-96-9

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Based on 1 publication(s) in Google Scholar

TASP0390325 Related Antibodies

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Description

TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities[1].

In Vitro

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.

TASP0390325 Related Antibodies
In Vivo

TASP0390325 blocks the anterior pituitary V1B receptor in vivo. Oral administration of TASP0390325 antagonized the increase in plasma ACTH levels induced by CRF/dDAVP in rats, indicating that TASP0390325 blocks the anterior pituitary V1B receptor in vivo. TASP0390325 (1 mg/kg) significantly antagonizes CRF/dDAVP-induced plasma ACTH in rats[1].
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.

Animal Model: Male Sprague-Dawley (SD) rats (211-246 g)[1]
Dosage: 0.3 and 1 mg/kg (TASP0390325 is suspended in 0.5% methylcellulose 400)
Administration: Oral administration
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.
Molecular Weight

554.44

Formula

C25H30Cl2FN5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1C(C2=CC(OCCCN3CCOCC3)=CN=C2N=C1C4=CC=C(C(Cl)=C4)F)=O)NC(C)C.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (180.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

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
100 mM 0.0180 mL 0.0902 mL 0.1804 mL 0.4509 mL
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TASP0390325 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TASP03903251642187-96-9TASP 0390325TASP-0390325Vasopressin Receptorarginine vasopressinV1B receptordepressionanxietyHPA axisdepression modelsanxiolytic effectssocial interactionelevated plus-mazestress-induced hyperthermiaseparation-induced ultrasonic vocalizationInhibitorinhibitorinhibit

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