| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Rhosin hydrochloride specifically targets RhoA by binding to it and inhibiting its interaction with guanine nucleotide exchange factors (GEFs) including LARG, DBL, LBC, p115 RhoGEF, and PDZ RhoGEF. This inhibition prevents the activation of RhoA, thereby blocking downstream signaling pathways such as ROCK-mediated contraction and motility. The compound does not affect Cdc42 or Rac1 signaling.
|
|---|---|
| ln Vitro |
Mammospheres produced from MCF7 cells exhibit dose-dependent reductions in RhoA and p-MLC1 activity, with an EC50 of ~30-50 μM. Additionally, mammosphere size and number in MCF7 cells are reduced [1].
In vitro, Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities in MCF7 cell-derived mammospheres with an EC50 of approximately 30-50 µM. It causes a decrease in the size and number of mammospheres in MCF7 cells. By suppressing RhoA or RhoC activity, Rhosin can inhibit mammary sphere formation by breast cancer cells, suppress invasion of mammary epithelial cells, and induce neurite outgrowth of PC12 cells in synergy with NGF. |
| ln Vivo |
The therapy of Russell (40 mg/kg; i.p.) inhibits social avoidance brought on by stress related to social defeat. In C57Bl6/J (Jackson) mice, Russell also prevents the sucrose preference deficit caused by failure [3]. ?Stress-induced social avoidance is lessened when Russell (30 μM; bilateral intranuclear accumbens (NAc) infusion) is used. In medium spiny neurons with the NAc dopamine 1 receptor, rosin inhibits the hyperexcitability brought on by stress (D1-MSN). Russell stops the excitatory transmission on NAc D1-MSNs from decreasing. In mice that fail, rosin increases spine density [3].
In vivo, Rhosin (40 mg/kg, i.p.) treatment prevents social avoidance caused by social defeat stress and blocks sucrose preference deficits induced by defeat in C57Bl/6J mice. Rhosin (30 µM; bilateral intra-Nucleus Accumbens infusions) attenuates stress-induced social avoidance and blocks stress-induced hyperexcitability in dopamine 1 receptor medium spiny neurons (D1-MSNs). It also prevents decreased excitatory transmission and enhances spine density in defeat mice. |
| Enzyme Assay |
The binding affinity of Rhosin hydrochloride to RhoA can be determined using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) assays. The compound is incubated with recombinant RhoA protein, and the dissociation constant (Kd) is calculated from the binding kinetics or thermodynamics. The Kd for Rhosin hydrochloride binding to RhoA has been reported as approximately 0.4 µM.
|
| Cell Assay |
To evaluate the cellular effects of Rhosin hydrochloride, cells such as MCF7 breast cancer cells are treated with the compound at various concentrations (e.g., 10-50 µM). The activity of RhoA and its downstream effector p-MLC1 is measured by Western blotting using specific antibodies. Mammosphere formation assays are performed to assess the compound's effect on cancer stem cell-like properties. The EC50 for inhibiting RhoA activity is determined from dose-response curves.
|
| Animal Protocol |
Animal/Disease Models: D1-GFP or D2-GFP hemizygous mice on C57BL/6J background [3]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Russell was administered systemically 15 minutes before failure to block RhoA activation. While failure Dramatically diminished the amount of time experimental mice spent interacting with new mice, giving Russell suppressed this effect without affecting motor behavior. For in vivo studies, Rhosin hydrochloride is typically administered to mice via intraperitoneal (i.p.) injection at doses such as 40 mg/kg. In models of social defeat stress, mice are subjected to repeated social defeat and then treated with Rhosin. Behavioral tests such as the social interaction test and sucrose preference test are performed to assess social avoidance and anhedonia. Brains are collected for biochemical and histological analysis, including assessment of dendritic spine density. |
| ADME/Pharmacokinetics |
Rhosin hydrochloride has a molecular weight of 394.86 and a formula of C20H19ClN6O. It is soluble in DMSO (10 mM) and should be stored at 4°C, sealed, and away from moisture. For long-term storage, it can be kept at -80°C for up to 2 years or at -20°C for 1 year.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for Rhosin hydrochloride are not detailed in the available literature. However, in vivo studies in mice at doses up to 40 mg/kg (i.p.) have been performed without reports of severe toxicity, indicating a degree of tolerability. As with any research compound, standard safety precautions should be taken when handling Rhosin hydrochloride.
|
| References |
|
| Additional Infomation |
Rhosin hydrochloride is a research tool used to study the role of RhoA in various biological processes, including cancer, cardiovascular disease, and neurological disorders. It has been shown to promote stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability. Rhosin hydrochloride is not a clinically approved drug but is valuable for preclinical studies investigating RhoA signaling.
|
| Molecular Formula |
C20H19CLN6O
|
|---|---|
| Molecular Weight |
394.8575
|
| Exact Mass |
394.13
|
| Elemental Analysis |
C, 60.84; H, 4.85; Cl, 8.98; N, 21.28; O, 4.05
|
| CAS # |
1281870-42-5
|
| Related CAS # |
Rhosin;1173671-63-0
|
| PubChem CID |
52998412
|
| Appearance |
Light yellow to yellow solid powder
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
28
|
| Complexity |
541
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
Cl[H].O=C([C@@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])[H])N([H])/N=C(/[H])\C1C([H])=C([H])C2C(C=1[H])=NC([H])=C([H])N=2
|
| InChi Key |
SFRGBDFQSLZYLF-GRYLRVQNSA-N
|
| InChi Code |
InChI=1S/C20H18N6O.ClH/c21-16(10-14-12-24-17-4-2-1-3-15(14)17)20(27)26-25-11-13-5-6-18-19(9-13)23-8-7-22-18;/h1-9,11-12,16,24H,10,21H2,(H,26,27);1H/b25-11+;/t16-;/m1./s1
|
| Chemical Name |
(2R)-2-amino-3-(1H-indol-3-yl)-N-[(E)-quinoxalin-6-ylmethylideneamino]propanamide;hydrochloride
|
| Synonyms |
Rhosin hydrochloride; Rhosin HCl; G04;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~126.63 mM)
H2O : ~16.67 mg/mL (~42.22 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
