NSC 23766 trihydrochloride

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NSC 23766 trihydrochloride  纯度: 99.66%

NSC 23766 trihydrochloride 是 Rac1 激活的抑制剂。

NSC 23766 trihydrochloride

NSC 23766 trihydrochloride Chemical Structure

CAS No. : 1177865-17-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥584 In-stock
5 mg ¥500 In-stock
10 mg ¥880 In-stock
50 mg ¥3760 In-stock
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200 mg   询价  

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生物活性

NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.

体外研究
(In Vitro)

NSC 23766 (100 μM) treatment effectively inhibits polar body emission in a dose-dependent manner. NSC 23766 (200 μM) increases the percentage of morphologically abnormal spindles of oocytes. In NSC 23766-treated oocytes, the p-MAPK protein expression is significantly decreased[2]. NSC23766 (50 μM) plus 100 ng/mL Jagged1, GDF9 and BMP15, reduces the number of germLine cell cysts and increases the number of primordial follicles[3]. NSC23766 significantly inhibits GTP-Rac1 activity and phosphorylation of Rac1-PAK, ERKs and p38 MAPK in the spinal dorsal horn neurons[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NSC23766 (2.5 mg/kg/day, i.p.) significantly attenuates the onset of spontaneous diabetes in NOD mice, without significant effects on the growth (body weights) of the mice. NSC23766 significantly increases the expression of Rac1 and CHOP, a marker for ER-stress, in islets from NOD mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

530.96

Formula

C24H38Cl3N7

CAS 号

1177865-17-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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 : 33.33 mg/mL (62.77 mM; Need ultrasonic)

H2O : ≥ 32 mg/mL (60.27 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8834 mL 9.4169 mL 18.8338 mL
5 mM 0.3767 mL 1.8834 mL 3.7668 mL
10 mM 0.1883 mL 0.9417 mL 1.8834 mL

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 110 mg/mL (207.17 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Veluthakal R, et al. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model. Cell Physiol Biochem. 2016;39(2):760-7.

    [2]. Song SJ, et al. Inhibition of Rac1 GTPase activity affects porcine oocyte maturation and early embryo development. Sci Rep. 2016 Oct 3;6:34415

    [3]. Zhao L, et al. Rac1 modulates the formation of primordial follicles by facilitating STAT3-directed Jagged1, GDF9 and BMP15 transcription in mice. Sci Rep. 2016 Apr 6;6:23972

    [4]. Wang Y, et al. Involvement of Rac1 signalling pathway in the development and maintenance of acute inflammatory pain induced by bee venom injection. Br J Pharmacol. 2016 Mar;173(5):937-50

Kinase Assay
[4]

Briefly, fresh spinal cord tissue of the lumbar enlargement is homogenised in the presence of protease and phosphatase inhibitors and lysed with buffer. After being centrifuged at 12,000× g for 5 min at 4°C, the supernatants are collected and incubated with PAK-PBD beads at 4°C on a rotator for 1 h and then the beads are pelleted through centrifugation at 5000× g for 3 min at 4°C. The resulting pellet is resuspended in LaemmLi buffer and boiled for 2 min. The bead samples are subjected to Western blot analysis. Total Rac1 in each sample is also determined by Western blot analysis.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Balb/c control and NOD mice are at 7 weeks of age and are divided into four groups (n=8/group). At 8 weeks of age two groups of experimental animals (Balb/c and NOD) receive NSC23766 (2.5 mg/kg/day, i.p./daily) and other two groups, which serve as control Balb/c and NOD mice and receive equal volume of saline. The body weights and blood glucose are monitored every week for 34 weeks.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Veluthakal R, et al. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model. Cell Physiol Biochem. 2016;39(2):760-7.

    [2]. Song SJ, et al. Inhibition of Rac1 GTPase activity affects porcine oocyte maturation and early embryo development. Sci Rep. 2016 Oct 3;6:34415

    [3]. Zhao L, et al. Rac1 modulates the formation of primordial follicles by facilitating STAT3-directed Jagged1, GDF9 and BMP15 transcription in mice. Sci Rep. 2016 Apr 6;6:23972

    [4]. Wang Y, et al. Involvement of Rac1 signalling pathway in the development and maintenance of acute inflammatory pain induced by bee venom injection. Br J Pharmacol. 2016 Mar;173(5):937-50

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