| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Rho-Kinase-IN-2 (0–10 mM, 1 hour) therapy resulted in decreased MYPT1 phosphorylation and enhanced AKT phosphorylation [1].
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|---|---|
| ln Vivo |
Rho-Kinase-IN-2 (orally given; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 hours) therapy exhibited dose- and time-dependent ROCK1 and ROCK2 target engagement [1]. Rho-Kinase-IN-2 (oral; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment revealed excellent tolerance assessment [1]. Treatment with Rho-Kinase-IN-2 (oral; 1-20 mg/kg; once) indicates a direct dose- and time-dependent link between brain exposure and MYPT1 phosphorylation status [1]. Treatment with Rho-Kinase-IN-2 (oral; 10 or 20 mg/kg; once) decreases mean arterial pressure, systolic blood pressure, diastolic blood pressure, and heart rate [1]. Treatment with Rho-Kinase-IN-2 (orally; 10 mg/kg; twice daily; 90 days) resulted in lower than predicted brain concentrations [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: A7r5 and PANC1 Cell Tested Concentrations: 0-10 mM Incubation Duration: 1 hour Experimental Results: demonstrated concentration-dependent effects resulting in increased phosphorylation of AKT (EC50=28 nM) and diminished phosphorylation of MYPT1 (IC50 =14 nM). |
| Animal Protocol |
Animal/Disease Models: 3 to 4 months old heterozygous Q175DN KI and wild-type littermate mice [1]
Doses: 10 or 20 mg/kg Route of Administration: po (po (oral gavage)) 10 or 20 mg/kg; one time/day or twice a day; 2-week Experimental Results: Neurologic indices were normal at all doses, although body weight diminished slightly (∼2%) in the 20 mg/kg treatment group. Animal/Disease Models: Heterozygous HTT zQ175DN knock-in mice [1] Doses: 1-20 mg/kg Route of Administration: Oral; 1-20 mg/kg; Experimental Results: Maintained over MYPT1 in free brain at 10 mg/kg dose IC50 exceeded 2 hrs (hrs (hours)), and dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum was observed after acute in vivo administration. Animal/Disease Models: CD1 mice [1] Doses: 10 and 20 mg/kg Route of Administration: Oral; 10 or 20 mg/kg; Experimental Results: Mean arterial pressure (maximum change from baseline 61.0 ± 8.5 mmHg), Systolic blood pressure (maximum change from baseline was 59.5 ± 8.4 mmHg), diastolic blood pressure (maximum change from baseline was 56.4 ± 9.0 mmHg), heart rate wi |
| References |
| Molecular Formula |
C20H25FN4O2
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|---|---|
| Molecular Weight |
372.436507940292
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| Exact Mass |
372.196
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| CAS # |
2573071-18-6
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| PubChem CID |
155749520
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
495
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| Defined Atom Stereocenter Count |
2
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| SMILES |
N1(C(N[C@@H](C2=CC=CC(OC)=C2)C)=O)CCN(C2C=CN=CC=2F)C[C@H]1C
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| InChi Key |
CIPXFTLGPVQJKN-HUUCEWRRSA-N
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| InChi Code |
InChI=1S/C20H25FN4O2/c1-14-13-24(19-7-8-22-12-18(19)21)9-10-25(14)20(26)23-15(2)16-5-4-6-17(11-16)27-3/h4-8,11-12,14-15H,9-10,13H2,1-3H3,(H,23,26)/t14-,15-/m1/s1
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| Chemical Name |
(2R)-4-(3-fluoropyridin-4-yl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methylpiperazine-1-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~134.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.37 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 20.0 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 mg/mL (5.37 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 20.0 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 mg/mL (5.37 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 | 2.6850 mL | 13.4250 mL | 26.8500 mL | |
| 5 mM | 0.5370 mL | 2.6850 mL | 5.3700 mL | |
| 10 mM | 0.2685 mL | 1.3425 mL | 2.6850 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.
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