Free shipping on all orders over $ 500

S-8921 

Cat. No. M28554
S-8921  Structure
Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?
Quality Control & Documentation
Biological Activity

S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.

Chemical Information
Molecular Weight 540.6
Formula C30H36O9
CAS Number 151165-96-7
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] Shingo Sakamoto, et al. Drug Metab Dispos. Identification of the transporters involved in the hepatobiliary transport and intestinal efflux of methyl 1-(3,4-dimethoxyphenyl)-3-(3-ethylvaleryl)-4-hydroxy-6,7,8-trimethoxy-2-naphthoate (S-8921) glucuronide, a pharmacologically active metabolite of S-䲧瘀Ỵ

[2] Shingo Sakamoto, et al. J Pharmacol Exp Ther. Glucuronidation converting methyl 1-(3,4-dimethoxyphenyl)-3-(3-ethylvaleryl)-4-hydroxy-6,7,8-trimethoxy-2-naphthoate (S-8921) to a potent apical sodium-dependent bile acid transporter inhibitor, resulting in a hypocholesterolemic action

[3] M L Booker. Curr Opin Investig Drugs. S-8921 (Shionogi)

[4] T Ichihashi, et al. J Pharmacol Exp Ther. Mechanism of hypocholesterolemic action of S-8921 in rats: S-8921 inhibits ileal bile acid absorption

[5] S Hara, et al. Life Sci. S-8921, an ileal Na+/bile acid cotransporter inhibitor decreases serum cholesterol in hamsters

Related Sodium Channel Products
ASN008

ASN008 is a permanently positively charged sodium channel blocker.
Psalmotoxin 1

Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a).
Jingzhaotoxin-III

Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms.
Huwentoxin-IV

Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively.
Phrixotoxin 3

Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively.
  Catalog
Abmole Inhibitor Catalog




Keywords: S-8921  supplier, Sodium Channel, inhibitors, activators

 
Get to Know Us
Customer Support
Resources
Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.