863638-93-1
Chemical Structure
(Rac)-NRL-1049 dihydrochloride
Synonym(s): (Rac)-BA-1049
- CAS No.: 863638-93-1
- Formula:C16H23Cl2N3O2S
- Molecular Weight:392.34
InChIKey: ZGHFCJWOBKWTQK-UHFFFAOYSA-N
SMILES: CC(C1CCN(CC1)S(=O)(C2=C3C=CN=CC3=CC=C2)=O)N.Cl.Cl
Biological Activity: (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[1][2].
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(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. | |||||||||||||||||||||
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- [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]
Keywords
