(R)-LS01-64
(R)-LS01-64 is a blood-brain barrier-penetrant μ opioid receptor (MOR) partial agonist and dopamine D3 receptor (D3R) inhibitor. (R)-LS01-64 binds to human MOR and D3R with Ki values of 22.3 nM and 138 nM, respectively, activates MOR signaling, and inhibits D3R-mediated G protein activation. (R)-LS01-64 can be used for pain research.
For research use only. We do not sell to patients.
- CAS No.: 3056226-40-2
- Formula: C25H31ClN2O
- Molecular Weight:410.98
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
μ Opioid Receptor/MOR 22.3 nM (Ki) |
D3 Receptor 138 nM (Ki) |
In Vitro
(R)-LS01-64 (10 μM-0.01 nM; 10 min plus 30 min) is a MOR partial agonist (Nb33 Emax 26.7%; arrestin-3 Emax 50.3%) and a D3R antagonist with pIC50 7.03 (IC50 89.6 nM) in HEK293T BRET assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (male and female)[1]
-
Dosage:56 mg/kg; 100 mg/kg
-
Administration:i.p.; single injection
-
Result:At 56 mg/kg, produced delayed antinociception observed at the 60-min time point.
At 100 mg/kg, did not produce antinociception.
-
Animal Model:C57BL/6J (male and female)[1]
-
Dosage:56 mg/kg; 100 mg/kg
-
Administration:i.p.; single injection
-
Result:At 100 mg/kg, increased distance traveled at the 30-min and 60-min time points.
Locomotor activation was observed only at 100 mg/kg, not at 56 mg/kg.
Chemical Information
-
CAS No. 3056226-40-2
-
Molecular Weight 410.98
-
Formula C25H31ClN2O
-
SMILES
ClC(C=C1)=CC=C1[C@H](C2)[C@@H]2NCC[C@]3(CCOC4(CCCC4)C3)C5=CC=CC=N5
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(R)-LS01-64 Related Classifications
HY-190876 Related Classifications
Powered by Bioz