Rhosin hydrochloride
(Synonyms: G04) 目录号 : GC32729
An inhibitor of the Rho-GEF protein-protein interaction
Cas No.:1281870-42-5
Sample solution is provided at 25 µL, 10mM.
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Rhosin is an inhibitor of the protein-protein interaction between Rho and guanine nucleotide exchange factors (GEFs).1 It inhibits RhoA activity when used at concentrations of 10 and 30 ?M and selectively reduces the number and size of MCF-7 breast cancer cell mammospheres over MCF-10A non-cancerous cell mammospheres. It also inhibits migration and invasion of MCF-7 cells and human mammary epithelial cells expressing RhoC. Rhosin (30 ?M) increases neurite outgrowth in PC12 cells. It prevents social defeat stress-induced hyperexcitability and increases spine density in nucleus accumbens dopamine 1 receptor medium spiny neurons (D1-MSNs) when administered post-social defeat stress in a mouse model of depression at a dose of 40 mg/kg.2 It also prevents social defeat stress-induced social avoidance and reductions in sucrose preference in the same model.
1.Shang, X., Marchioni, F., Sipes, N., et al.Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPasesChem. Biol.19(6)699-710(2012) 2.Francis, T.C., Gaynor, A., Chandra, R., et al.The selective RhoA inhibitor rhosin promotes stress resiliency through enhancing D1-medium spiny neuron plasticity and reducing hyperexcitabilityBiol. Psychiatry85(12)1001-1010(2019)
| Cas No. | 1281870-42-5 | SDF | |
| 别名 | G04 | ||
| Canonical SMILES | O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4.[H]Cl | ||
| 分子式 | C20H19ClN6O | 分子量 | 394.86 |
| 溶解度 | DMSO : 100 mg/mL (253.25 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5325 mL | 12.6627 mL | 25.3254 mL |
| 5 mM | 0.5065 mL | 2.5325 mL | 5.0651 mL |
| 10 mM | 0.2533 mL | 1.2663 mL | 2.5325 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet