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Samelisant free base

Cat. No. M28323
Samelisant free base Structure
Synonym:

SUVN-G3031 free base

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Biological Activity

Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.

Chemical Information
Molecular Weight 373.49
Formula C21H31N3O3
CAS Number 1394808-82-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Panagiotis V Samelis, et al. Cureus. Primary Congenital Hallux Varus: A Step-Cut Surgical Approach

[2] Evangelos Anagnostou, et al. Neurocirugia (Astur : Engl Ed). Two-step treatment of a giant skull vault hemangioma: A rare case report and literature review

[3] Panagiotis V Samelis, et al. Cureus. Factors Affecting Outcomes of Slipped Capital Femoral Epiphysis

[4] K A Ekmektzoglou, et al. Acta Gastroenterol Belg. Gastroesophageal junction and gastroesophageal junction carcinoma : a short update

[5] Maria Parapouli, et al. Appl Environ Microbiol. Characterization of a wild, novel nisin a-producing Lactococcus strain with an L. lactis subsp. cremoris genotype and an L. lactis subsp. lactis phenotype, isolated from Greek raw milk

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