2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. CGP 36742

CGP 36742  (Synonyms: SGS-742)

目录号: HY-121599 纯度: ≥98.0%
COA 产品使用指南 技术支持

CGP 36742 (SGS-742) 是一种有口服活性且具有选择性的 GABAB 受体拮抗剂 (IC50 = 36 µM)。CGP 36742 具有血脑屏障 (BBB) 渗透性，可提高认知能力。CGP 36742 可用于抑郁症研究。

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CGP 36742

CGP 36742 Chemical Structure

CAS No. : 123690-78-8

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥1320
In-stock
1 mg ￥545
In-stock
5 mg ￥1200
In-stock
10 mg ￥2150
In-stock
25 mg ￥4000
In-stock
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100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of CGP 36742:

CGP 36742 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a blood-brain barrier (BBB) penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study[1][2][3][4].

IC50 & Target

IC50: 32 μM (GABAB)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Oocyte IC50
38 μM
Compound: 7, CGP-36742
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
508 μM
Compound: 7, CGP-36742
Antagonist activity at human recombinant GABAA alpha1beta2gamma2L receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAA alpha1beta2gamma2L receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
62 μM
Compound: 7, CGP-36742
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
62 μM
Compound: 2, SGS742
Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
[PMID: 18528996]
体外研究
(In Vitro)

CGP 36742 阻断 CA1 锥体神经元中的晚期抑制性突触后电位 (i.p.s.p.)[2]。
CGP 36742 (1 μM) 可有效阻止犬尿酸拮抗 N-methyl-d-aspartate (NMDA) (HY-17551) 诱导的大鼠脑切片去甲肾上腺素释放[4]。
CGP 36742 (1 μM) 可增加 NMDA 处理的海马切片中生长抑素样免疫反应 (SRIF-LI) 的释放[4]。

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

CGP 36742 相关抗体:
体内研究
(In Vivo)

CGP 36742 (10-30 mg/kg；腹腔注射；试验前 30 分钟) 在小鼠强迫游泳试验中表现出抗抑郁样活性[1]。
CGP 36742 (10 mg/kg；腹腔注射；每天一次，连续 14 天) 对大鼠嗅球切除 (OB) 抑郁症模型有效[1]。
CGP 36742 (30-200 mg/kg；口服；间隔 2.5-3 小时累积给药) 可阻断麻醉大鼠中由巴氯芬引起的离子电渗的神经元抑制[2]。
CGP 36742 (1-10 mg/kg；静脉注射；试验前 25-30 分钟) 剂量依赖性地减弱了延迟 > 100 ms 时的成对脉冲抑制[2]。
CGP 36742 (50-1000 mg/kg；静脉注射或口服；一次或两次) 可以穿透雄性 Sprague-Dawley 大鼠的血脑屏障[3]。

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

Animal Model: Male Albino Swiss mice (22-26 g)[1]
Dosage: 10, 30 mg/kg
Administration: Intraperitoneal injection (i.p.); 30 min before test
Result: Significantly reduced the immobility time in the forced swim test at both doses (10 mg/kg by 32% and 30 mg/kg by 40%).
Had no effect on the spontaneous locomotor activity in mice.
Animal Model: Male Wistar rats (200-250 g), olfactory bulbectomy model[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.); once daily for 14 d
Result: Single administration did not alter the olfactory bulbectomy (OB)-induced learning deficit, induced following bulbectomy.
Restored the learning deficit in OB rats (five trials) without affecting performance in sham-operated animals.
Reduced the OB-related increase in the number of rearings + peepings.
Animal Model: Male rats (weighing 280-320 g)[2]
Dosage: 30-200 mg/kg
Administration: Oral gavage (p.o.); administered in a cumulative manner at intervals of 2.5-3 h.
Result: Antagonized baclofen-induced inhibitory effects on spontaneously firing cortical neurons in a dose-dependent manner.
Animal Model: Male Sprague-Dawley rats (200-325 g)[3]
Dosage: 50, 100, 200, 500, 1000 mg/kg
Administration: Intravenous injection (i.v.) via tail vein of 50, 100, 200 mg/kg, oral gavage (p.o.) of 500, 1000 mg.kg; in two rats given an i.v. injection of 100 mg/kg, a second i.v. injection of 100 mg/kg was given after 6 h and samples were collected for another 6 h.
Result: The appearance in the rat brain frontal cortex after i.v. injection was seen in the first 30 min dialyzate collected and peaked in the 1 h dialysate.
Removed or metabolized from brain in dialyzates collected 3 h post-injection.
The presence was again seen 30 min after the second 100 mg/kg i.v. injection administered 6 h after the first injection.
Showed the appearance in the third ventricle of the rat brain after two i.v. injections of 100 mg/kg with an interval of 6 h.
Showed that the highest concentrations were seen 1.5 or 2 h after the p.o..
Clinical Trial
分子量

179.20

Formula

C7H18NO2P
CAS 号
性状

固体

颜色

White to light 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
细胞实验： 

H2O 中的溶解度 : 125 mg/mL (697.54 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.5804 mL 27.9018 mL 55.8036 mL
5 mM 1.1161 mL 5.5804 mL 11.1607 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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

只
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
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

COA (279 KB) HNMR (191 KB) MS (72 KB)

产品使用指南 (1538 KB)
参考文献

CGP 36742 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。-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
H2O 1 mM 5.5804 mL 27.9018 mL 55.8036 mL 139.5089 mL
5 mM 1.1161 mL 5.5804 mL 11.1607 mL 27.9018 mL
10 mM 0.5580 mL 2.7902 mL 5.5804 mL 13.9509 mL
15 mM 0.3720 mL 1.8601 mL 3.7202 mL 9.3006 mL
20 mM 0.2790 mL 1.3951 mL 2.7902 mL 6.9754 mL
25 mM 0.2232 mL 1.1161 mL 2.2321 mL 5.5804 mL
30 mM 0.1860 mL 0.9301 mL 1.8601 mL 4.6503 mL
40 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4877 mL
50 mM 0.1116 mL 0.5580 mL 1.1161 mL 2.7902 mL
60 mM 0.0930 mL 0.4650 mL 0.9301 mL 2.3251 mL
80 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7439 mL
100 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3951 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

CGP 36742123690-78-8SGS-742CGP36742CGP-36742SGS742SGS 742GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorblood-barrierdepressionInhibitorinhibitorinhibit

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