2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. ROCK
  4. NRL-1049

NRL-1049  (Synonyms: BA-1049 free base)

Cat. No.: HY-162596 Purity: 99.96%
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NRL-1049 (BA-1049 (free base)) 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.

NRL-1049

NRL-1049 Chemical Structure

CAS No. : 1973494-16-4

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NRL-1049 Related Antibodies

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Description

NRL-1049 (BA-1049 (free base)) 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].

IC50 & Target[1]

ROCK1

26 μM (IC50)

ROCK2

0.59 μM (IC50)

In Vitro

NRL-1049 potently and selectively inhibits purified recombinant ROCK2, with an IC50 of 0.59 μM, and is 43-fold more selective for ROCK2 than ROCK1[1].
NRL-1049 (10 μM) inhibits ROCK1, ROCK2, and eight additional human protein kinases by greater than 95%[1].
NRL-1049 (0.01-1000 μM; 1 hour prior to LPA stimulation) concentration-dependently inhibits LPA-induced ROCK activity (measured via MLC2 phosphorylation) in hBMVECs, with an EC50 of 26.3 μM after 1 hour of pre-incubation[1].
NRL-1049 (50 μM; 1 hour incubation) inhibits LPA-induced ROCK activity in HUVECs by 15% after 1 hour of incubation, with the effect fully reversed within 1 hour of compound washout[1].
NRL-1049 (1 μM) leads to mouse, cynomolgus monkey, and human hepatocytes producing the active metabolite NRL-2017, rat hepatocytes producing NRL-2017 and an inactive N-oxide metabolite, and dog hepatocytes producing no detectable metabolites[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NRL-1049 Related Antibodies
Parmacokinetics
Species Dose Route T1/2
Mice[1] 10 mg/kg i.p. 0.33 h
Rat[1] 10 mg/kg i.p. 0.89 h
In Vivo

NRL-1049 (10-20 mg/kg; i.p., s.c., oral; single dose, continuous, via drinking water; 24 hours) prevents seizure development, reduces ipsilesional brain water content, and diminishes Evans Blue extravasation to near-sham levels, preserving blood-brain barrier integrity after cortical cryoinjury in C57BL/6 mice[1].
NRL-1049 (10 mg/kg; i.p.; single dose 15 minutes post-reperfusion) significantly reduces Evans Blue extravasation, lowers the incidence of hemorrhagic transformation to 25%, and improves hemorrhage grade, preserving blood-brain barrier integrity after transient MCAO in spontaneously hypertensive rats[1].
NRL-1049 (1 mg/kg; p.o.; daily; 3-4 months) reduces CCM lesion burden and hemorrhage in CCM knockout mice, with sustained retention in vascular tissues[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male and female, 18-22 gram, cortical cryoinjury-induced acute brain injury)[1]
Dosage: 10 mg/kg plus 10 mg/h (brain water content, seizure monitoring); 20 mg/kg plus 100 mg/kg/day (Evans Blue extravasation)
Administration: i.p. (single dose immediately post-injury); s.c. (continuous via osmotic pump, 24 hours); oral (via drinking water, starting immediately post-injury)
Result: Prevented seizure development to 0% within 24 hours post-injury.
Showed significantly lower ipsilesional brain water content at 24 hours post-injury, with a strong trend toward lower water content as early as 1 hour post-injury.
Animal Model: Spontaneously hypertensive rats (SHR) (male, 170-300 gram, transient middle cerebral artery occlusion-induced ischemic stroke)[1]
Dosage: 10 mg/kg
Administration: i.p. (single dose 15 minutes post-reperfusion)
Result: Significantly reduced Evans Blue extravasation in the ischemic hemisphere compared to vehicle controls.
Reduced incidence of hemorrhagic transformation to 25% compared to 78% of vehicle-treated rats.
Achieved a significantly lower mean hemorrhage grade (0.43).
Molecular Weight

319.42

Formula

C16H21N3O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](C1CCN(CC1)S(=O)(C2=C3C=CN=CC3=CC=C2)=O)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (313.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1307 mL 15.6534 mL 31.3067 mL
5 mM 0.6261 mL 3.1307 mL 6.2613 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1307 mL 15.6534 mL 31.3067 mL 78.2669 mL
5 mM 0.6261 mL 3.1307 mL 6.2613 mL 15.6534 mL
10 mM 0.3131 mL 1.5653 mL 3.1307 mL 7.8267 mL
15 mM 0.2087 mL 1.0436 mL 2.0871 mL 5.2178 mL
20 mM 0.1565 mL 0.7827 mL 1.5653 mL 3.9133 mL
25 mM 0.1252 mL 0.6261 mL 1.2523 mL 3.1307 mL
30 mM 0.1044 mL 0.5218 mL 1.0436 mL 2.6089 mL
40 mM 0.0783 mL 0.3913 mL 0.7827 mL 1.9567 mL
50 mM 0.0626 mL 0.3131 mL 0.6261 mL 1.5653 mL
60 mM 0.0522 mL 0.2609 mL 0.5218 mL 1.3044 mL
80 mM 0.0391 mL 0.1957 mL 0.3913 mL 0.9783 mL
100 mM 0.0313 mL 0.1565 mL 0.3131 mL 0.7827 mL
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NRL-1049 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NRL-10491973494-16-4BA-1049NRL1049NRL 1049BA1049BA 1049ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKcerebral cavernous malformationROCK1hBMVECsHUVECsROCK2Rho-associated protein kinase 2spontaneously hypertensive ratsC57BL/6 miceischemic strokeacute brain injuryInhibitorinhibitorinhibit

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