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SB269652 

Cat. No. M29307
SB269652  Structure
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Biological Activity

SB269652 is an allosteric modulator of the dopamine D2 receptor (D2R). It is a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.

Chemical Information
Molecular Weight 426.55
Formula C27H30N4O
CAS Number 215802-15-6
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Anitha Kopinathan, et al. J Med Chem. Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity䲧瘀Ỵ瘁㧀痿羹皘的郘

[2] Ravi Kumar Verma, et al. PLoS Comput Biol. The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors

[3] Mario Rossi, et al. Mol Pharmacol. The First Negative Allosteric Modulator for Dopamine D2 and D3 Receptors, SB269652 May Lead to a New Generation of Antipsychotic Drugs

[4] Jeremy Shonberg, et al. J Med Chem. Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor

[5] J Robert Lane, et al. Nat Chem Biol. A new mechanism of allostery in a G protein-coupled receptor dimer

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Keywords: SB269652  supplier, Dopamine Receptor, inhibitors, activators

 
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