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Elobixibat

Cat. No. M10815
Elobixibat Structure
Synonym:

A 3309

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Quality Control & Documentation
Biological Activity

Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor, IC50 Values were 0.53±0.17 nM (human IBAT), 0.13±0.03 nM (mouse IBAT), 5.8± 1.6 nM (canine IBAT).

Chemical Information
Molecular Weight 695.89
Formula C36H45N3O7S2
CAS Number 439087-18-0
Solubility (25°C) DMSO ≥ 200 mg/mL
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] Anna Ozaki, et al. Oncologist. Elobixibat Effectively Relieves Chronic Constipation in Patients with Cancer Regardless of the Amount of Food Intake

[2] Lehar Khanna, et al. Aliment Pharmacol Ther. Review article: Elobixibat: a novel treatment for chronic constipation

[3] Daigo Kamei, et al. BMC Gastroenterol. Elobixibat alleviates chronic constipation in hemodialysis patients: a questionnaire-based study

[4] Victor Chedid, et al. Expert Rev Gastroenterol Hepatol. Elobixibat for the treatment of constipation

[5] Banny S Wong, et al. Expert Opin Investig Drugs. Elobixibat for the treatment of constipation

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Keywords: Elobixibat, A 3309 supplier, inhibitors, activators


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