| Company Name: |
Shanghai Yifei Biotechnology Co. , Ltd.
|
| Tel: |
021-65675885 18964387627 |
| Email: |
customer_service@efebio.com |
| Products Intro: |
Product Name:Rho-Kinase-IN-2
CAS:2573071-18-6
Purity:95.00% Package:2mg;5mg;25mg
|
| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:Rho-Kinase-IN-2
CAS:2573071-18-6
Package:2mg/RMB 1540;5mg/RMB 2610;25mg/RMB 9160
|
1-Piperazinecarboxamide, 4-(3-fluoro-4-pyridinyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methyl-, (2R)- manufacturers
- Rho-Kinase-IN-2
-
- $4169.00 / 100mg
-
2025-07-19
- CAS:2573071-18-6
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | 1-Piperazinecarboxamide, 4-(3-fluoro-4-pyridinyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methyl-, (2R)- Basic information |
| | 1-Piperazinecarboxamide, 4-(3-fluoro-4-pyridinyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methyl-, (2R)- Chemical Properties |
| Boiling point | 574.8±50.0 °C(Predicted) | | density | 1.192±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 13.26±0.40(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | 1-Piperazinecarboxamide, 4-(3-fluoro-4-pyridinyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methyl-, (2R)- Usage And Synthesis |
| Description | Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington's research[1]. Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation[1]. Western Blot Analysis[1] Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h) treatment shows dose- and time-dependent ROCK1 and ROCK2 target engagement[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment[1].
Rho-Kinase-IN-2 (oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate[1].
Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations[1]. | | Uses | Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research[1]. | | in vivo | Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h) treatment shows dose- and time-dependent ROCK1 and ROCK2 target engagement[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment[1].
Rho-Kinase-IN-2 (oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate[1].
Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations[1]. | Animal Model: | Male C57BL/6 mice[1] | | Dosage: | 10 mg/kg | | Administration: | Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h | | Result: | Observed dose- and time-dependent ROCK1 and ROCK2 TE, with a free brain KiNativ ROCK1 and ROCK2 IC50=～6 nM. |
| Animal Model: | 3?4 months old heterozygote Q175DN KI and wild-type littermate mice[1] | | Dosage: | 10 or 20 mg/kg | | Administration: | Oral adiministration; 10 or 20 mg/kg; once a day or twice a day; 2 weeks | | Result: | Scored neurological index normally at all doses although a slight loss in bodyweight (～2%) in the 20 mg/kg treatment group. |
| Animal Model: | Heterozygote HTT zQ175DN knock-in mice[1] | | Dosage: | 1-20 mg/kg | | Administration: | Oral adiministration; 1-20 mg/kg; once | | Result: | Remained over MYPT1 IC50 for over 2 h of the free brain at 10 mg/kg, and observed the dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum following acute in vivo dosing. |
| Animal Model: | CD1 mice[1] | | Dosage: | 10 and 20 mg/kg | | Administration: | Oral adiministration; 10 or 20 mg/kg; once | | Result: | Observed the decreases in the mean arterial (maximum change of 61.0 ± 8.5 mmHg from baseline), systolic (maximum change of 59.5 ± 8.4 mmHg from baseline), diastolic blood pressure (maximum change of 56.4 ± 9.0 mmHg from baseline), and heart rate (maximum change from predose of 107 bpm) when compared to the control group from ～0.5 to 2 h post dose. |
| Animal Model: | Heterozygote Q175DN KI mouse model of HD[1] | | Dosage: | 10 mg/kg | | Administration: | Oral adiministration; 10 mg/kg; twice a day; 90 days | | Result: | Led to lower-than-expected brain concentrations compared to single dosing. |
| | IC 50 | ROCK2: 3 nM (IC50) | | References | [1] Tammy Ladduwahetty, et al. Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease. J Med Chem. 2022 Jul 11. DOI:10.1021/acs.jmedchem.2c00474 |
| | 1-Piperazinecarboxamide, 4-(3-fluoro-4-pyridinyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-2-methyl-, (2R)- Preparation Products And Raw materials |
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