Rho-Kinase-IN-2 NEW
| Price | $1439 | $2539 | $4169 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-04-27 |
Product Details
| Product Name: Rho-Kinase-IN-2 | CAS No.: 2573071-18-6 |
| Supply Ability: 10g | Release date: 2025/04/27 |
Product Introduction
Bioactivity
| Name | Rho-Kinase-IN-2 |
| Description | Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK) with CNS penetration, exhibiting a high affinity for ROCK2 with an IC50 of 3 nM. This compound is of potential interest for further investigations in Huntington's disease research [1]. |
| In vitro | Treatment with Rho-Kinase-IN-2 (0-10 mM) for 1 hour led to concentration-dependent alterations in phosphorylation levels, specifically an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation, observed across A7r5 and PANC1 cell lines. Western Blot Analysis confirmed these effects, quantifying the potency of Rho-Kinase-IN-2 in modulating AKT and MYPT1 phosphorylation with EC50 and IC50 values of 28 nM and 14 nM, respectively. |
| In vivo | Administering Rho-Kinase-IN-2 orally at 10 mg/kg six times at intervals of 0.5, 1, 2, 4, 8, and 12 hours demonstrated a dose- and time-dependent engagement with ROCK1 and ROCK2 targets. Similar administration at doses of 10 or 20 mg/kg, either once daily (QD) or twice daily (BID) for two weeks, exhibited excellent tolerability. A single dose ranging from 1-20 mg/kg revealed a direct dose- and time-dependent correlation between brain exposure and MYPT1 phosphorylation status. Moreover, a single administration at 10 or 20 mg/kg resulted in decreased mean arterial, systolic, diastolic blood pressures, and heart rate. Continuous treatment at 10 mg/kg twice daily for 90 days led to lower-than-expected brain concentrations. These findings were consistent across various animal models, including male C57BL/6 mice, 3-4-month-old heterozygote Q175DN KI and wild-type littermate mice, heterozygote HTT zQ175DN knock-in mice, and CD1 mice, demonstrating the compound’s pharmacodynamics and pharmacokinetics profiles in preclinical settings. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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