| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Odevixibat (formerly known as A-4250; AZD-8294; A-4250; AR-H 064974; Bylvay) is a novel, potent and orally bioavailable inhibitor of ileal bile acid transporter (IBAT) with the potential to be used for the treatment of primary biliary cirrhosis. As of July 2021, Odevixibat has been approved in the United States and in the European Union for the treatment of progressive familial intrahepatic cholestasis (PFIC).
| ln Vivo |
Odevixibat (A4250) (0.01% (w/w) in feed; 4 weeks) ameliorates sclerosing cholangitis and dramatically lowers serum levels of BA, alkaline phosphatase, and alanine aminotransferase, as well as the expression of pro-inflammatory and pro-fibrotic genes in the liver and bile duct proliferation in Mdr2-/-mice [1]. Additionally, while stimulating Ntcp and Cyp7a1, Odevixibat (A4250) considerably lowers bile flux and bile BA output, which coincides with reduced bsep transcription [1].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Eightweeks old Mdr2-/- (Abcb4-/-) mice (cholestatic liver injury and sclerosing cholangitis model) [1]
Doses: 0.01% (w/w) in feed Administration time: 4-week Experimental Results: Cholestasis diminished in mouse liver and bile duct injury model. |
| References |
[1]. Baghdasaryan A, et al. Inhibition of intestinal bile acid absorption improves cholestatic liver and bile duct injury in a mouse model of sclerosing cholangitis.J Hepatol. 2016 Mar;64(3):674-81.
|
| Molecular Formula |
C37H48N4O8S2
|
|---|---|
| Molecular Weight |
740.93
|
| Exact Mass |
740.2914
|
| CAS # |
501692-44-0
|
| Related CAS # |
501692-44-0;2409081-01-0 (hydrate);Odevixibat HCl;
|
| SMILES |
CC[C@H](NC([C@H](NC(COC1=C(SC)C=C(C2=C1)N(C3=CC=CC=C3)CC(CCCC)(CCCC)NS2(=O)=O)=O)C4=CC=C(O)C=C4)=O)C(O)=O
|
| Chemical Name |
(S)-2-((R)-2-(2-((3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydrobenzo[f][1,2,5]thiadiazepin-8-yl)oxy)acetamido)-2-(4-hydroxyphenyl)acetamido)butanoic acid
|
| Synonyms |
AZD8294 A4250 AR-H064974AZD-8294 A-4250 AR-H-064974Bylvay
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~166.67 mg/mL (~224.95 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 41.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4.17 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 41.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3497 mL | 6.7483 mL | 13.4966 mL | |
| 5 mM | 0.2699 mL | 1.3497 mL | 2.6993 mL | |
| 10 mM | 0.1350 mL | 0.6748 mL | 1.3497 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA