Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
Other Sizes |
|
ln Vitro |
Rho reducing agent H-1152 dihydrochloride has an IC50 of 12 nM for ROCK2. Lower inhibition of CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α Activity is also demonstrated by H-1152 dihydrochloride (H-1152 dihydrochloride P); the IC50 values are 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM [1]. With a Ki of 1.6 nM, 1152 dihydrochloride potently inhibits Rho, but its Ki of 0.63, 9.27, and 10.1 μM very mildly inhibits PKA, PKC, and MLCK. H-1152 dihydrochloride (0.1-10 μM) exhibits a strong inhibitory effect on MARCKS phosphorylation in LPA-treated cells, with an IC50 value of 2.5 μM; however, no discernible effect is observed in PDBu-treated cells [2]. Neuronal persistence rates do not recover in response to H-1152 dihydrochloride (0.5–10 μM). Additionally, H-1152 dihydrochloride (1, 5, or 10 μM) did not change the percentage of various neuronal morphologies. Furthermore, in BMP4 and LIF cultures, 10 μM of H-1152 dihydrochloride lengthens neurites [3].
|
---|---|
References |
[1]. Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52. Epub 2005 Sep 12.
[2]. Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16. [3]. Lie M, et al. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010 Aug 25;169(2):855-62 |
Molecular Formula |
C16H23CL2N3O2S
|
---|---|
Molecular Weight |
392.3437
|
CAS # |
871543-07-6
|
Related CAS # |
H-1152;451462-58-1;Glycyl H-1152 hydrochloride;913844-45-8
|
SMILES |
Cl[H].Cl[H].S(C1=C([H])C([H])=C([H])C2C([H])=NC([H])=C(C([H])([H])[H])C1=2)(N1C([H])([H])C([H])([H])C([H])([H])N([H])C([H])([H])[C@]1([H])C([H])([H])[H])(=O)=O
|
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) |
H2O : ~35.71 mg/mL (~91.02 mM)
DMSO : ~10 mg/mL (~25.49 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.30 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 20.8 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: ≥ 2.08 mg/mL (5.30 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 20.8 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: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (127.44 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5488 mL | 12.7440 mL | 25.4881 mL | |
5 mM | 0.5098 mL | 2.5488 mL | 5.0976 mL | |
10 mM | 0.2549 mL | 1.2744 mL | 2.5488 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.