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

TASP0390325 是一种高亲和力的、具有口服活性的精氨酸加压素受体 1B(V1B 受体)拮抗剂,具有抗抑郁和抗焦虑活性。

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TASP0390325 Chemical Structure

TASP0390325 Chemical Structure

CAS No. : 1642187-96-9

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

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.
分子量

554.44

Formula

C25H30Cl2FN5O4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (180.36 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

参考文献

TASP0390325 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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.

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产品名称:
TASP0390325
目录号:
HY-117820
需求量: