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Sigma-2 receptor antagonist 1

Cat. No. M14060
Sigma-2 receptor antagonist 1 Structure
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Biological Activity

Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.

Chemical Information
Molecular Weight 431.59
CAS Number 1802632-22-9
Solubility (25°C) DMSO 150 mg/mL
Storage 2-8°C, protect from light
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] Pilar Snchez-Blzquez, et al. The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception

[2] Ai-Fang Chen, et al. Sigma-2 Receptor as a Potential Drug Target

[3] Rita Turnaturi, et al. Exploiting the Power of Stereochemistry in Drug Action: 3-[(2 S,6 S,11 S)-8-Hydroxy-6,11-dimethyl-1,4,5,6-tetrahydro-2,6-methano-3-benzazocin-3(2 H)-yl]- N-phenylpropanamide as Potent Sigma-1 Receptor Antagonist

[4] Hayden R Schmidt, et al. The Molecular Function of σ Receptors: Past, Present, and Future

[5] Yu-Tong Sun, et al. Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands

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