1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. TPA-023B

TPA-023B 是一种高亲和力的口服活性的 GABAA 受体 α2/α3 亚型 (Ki 为 0.73 nM/2 nM) 部分激动剂和 α1 亚型 (Ki 为 1.8 nM) 拮抗剂。TPA-023B 具有非镇静抗焦虑特性。

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TPA-023B Chemical Structure

TPA-023B Chemical Structure

CAS No. : 425377-76-0

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5 mg ¥4000
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10 mg ¥6800
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties[1].

体外研究
(In Vitro)

TPA-023B also has high affinity for α5 subtype (Ki of 1.1 nM) of human recombinant GABAA receptor, but over 1500-fold lower for the α4- and α6 containing subtypes (Ki > 1000 nM). TPA-023B also has a comparable affinity for native rat GABAA receptors in different regions of the CNS (Ki of 0.32-0.99 nM in cerebellum, spinal cord and frontal cortex)[1].
TPA-023B antagonizes the ability of chlordiazepoxide to potentiate the GABA EC20-induced current in cells expressing the α1 subtype. More specifically, 3 μM chlordiazepoxide potentiates the GABA EC20 current by 105% and this effect could be reduced to 8% in the presence of 100 nM TPA-023B[1].

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

体内研究
(In Vivo)

TPA-023B gives dose- and time-dependent occupancy of rat brain GABAA receptors as measured using an in vivo [3H]flumazenil binding assay, with 50% occupancy corresponding to a respective dose and plasma drug concentration of 0.09 mg/kg and 19 ng/mL[1].
TPA-023B is anxiolytic in rodent and primate (squirrel monkey) models of anxiety (elevated plus maze, fear-potentiated startle, conditioned suppression of drinking, conditioned emotional response) yet has no significant effects in rodent or primate assays of ataxia and/or myorelaxation (rotarod, chain-pulling, lever pressing), up to doses (10 mg/kg) corresponding to occupancy of greater than 99%[1].

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

分子量

391.37

Formula

C21H15F2N5O

CAS 号
性状

固体

颜色

Light yellow to green yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (255.51 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 2.5551 mL 12.7756 mL 25.5513 mL
5 mM 0.5110 mL 2.5551 mL 5.1103 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。-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
参考文献

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。-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 2.5551 mL 12.7756 mL 25.5513 mL 63.8782 mL
5 mM 0.5110 mL 2.5551 mL 5.1103 mL 12.7756 mL
10 mM 0.2555 mL 1.2776 mL 2.5551 mL 6.3878 mL
15 mM 0.1703 mL 0.8517 mL 1.7034 mL 4.2585 mL
20 mM 0.1278 mL 0.6388 mL 1.2776 mL 3.1939 mL
25 mM 0.1022 mL 0.5110 mL 1.0221 mL 2.5551 mL
30 mM 0.0852 mL 0.4259 mL 0.8517 mL 2.1293 mL
40 mM 0.0639 mL 0.3194 mL 0.6388 mL 1.5970 mL
50 mM 0.0511 mL 0.2555 mL 0.5110 mL 1.2776 mL
60 mM 0.0426 mL 0.2129 mL 0.4259 mL 1.0646 mL
80 mM 0.0319 mL 0.1597 mL 0.3194 mL 0.7985 mL
100 mM 0.0256 mL 0.1278 mL 0.2555 mL 0.6388 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:
TPA-023B
目录号:
HY-19505
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