(Rac)-NRL-1049 dihydrochloride
(Rac)-NRL-1049 is the racemic mixture of NRL-1049 (BA-1049 (free base)) (HY-162596). NRL-1049 is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations.
For research use only. We do not sell to patients.
- CAS No.: 863638-93-1
- Formula: C16H23Cl2N3O2S
- Molecular Weight:392.34
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Chemical Information
-
CAS No. 863638-93-1
-
Molecular Weight 392.34
-
Formula C16H23Cl2N3O2S
-
SMILES
CC(C1CCN(CC1)S(=O)(C2=C3C=CN=CC3=CC=C2)=O)N.Cl.Cl
-
Synonyms
(Rac)-BA-1049
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
[1]. Mulder IA, et al. The novel ROCK2 selective inhibitor NRL-1049 preserves the blood-brain barrier after acute injury. J Cereb Blood Flow Metab. 2024 Jun 4:271678X241238845. [Content Brief]
[2]. Madden S, et al. Safety, Tolerability, and Pharmacokinetics of NRL-1049, a Rho-Associated Kinase Inhibitor, in Healthy Volunteers: A Phase 1, First-in-Human, Single-Ascending Dose, Randomized, Placebo-Controlled Trial. CNS Drugs. 2025;39(9):865-877. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)