Odevixibat (Synonyms: A4250) |
رقم الكتالوجGC63126
One-Click Copy Product Info
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Odevixibat (A4250) هو مثبط فعال وانتقائي وفعال عن طريق الفم لناقل حمض الصفراء (IBAT)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 501692-44-0
Sample solution is provided at 25 µL, 10mM.
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Odevixibat (A4250) is a potent and selective inhibitor of intestinal bile acid transporter (IBAT), with an IC50 value of 0.16nM[1]. Odevixibat reduces the reuptake of bile acids from the intestine to the serum and clears bile acids in the colon, thereby lowering the bile acid levels in the serum[2]. Odevixibat has been used to study the regulation of serum bile acids and improvement of liver parameters[3].
In vivo, Odevixibat treatment (10mg/kg/day; p.o.) for 4 weeks significantly ameliorated liver fibrosis, reduced hepatic collagen deposition and α-SMA expression, and improved liver function indicators in Slc27a5−/− mice[4]. In Mdr2−/− mice, dietary treatment with 0.01% (w/w) Odevixibat for 4 weeks significantly mitigated sclerotizing cholangitis, reduced bile duct damage, decreased bile acid secretion, and increased fecal bile acid excretion[5].
References:
[1] Wang Q, Han J, Sorochinsky A, et al. The latest FDA-approved pharmaceuticals containing fragments of tailor-made amino acids and fluorine[J]. Pharmaceuticals, 2022, 15(8): 999.
[2] Al Shaer D, Al Musaimi O, Albericio F, et al. 2021 FDA TIDES (peptides and oligonucleotides) harvest[J]. Pharmaceuticals, 2022, 15(2): 222.
[3] Thompson R J, Artan R, Baumann U, et al. Interim results from an ongoing, open-label, single-arm trial of odevixibat in progressive familial intrahepatic cholestasis[J]. Jhep Reports, 2023, 5(8): 100782.
[4] Wu K, Liu Y, Xia J, et al. Loss of SLC27A5 activates hepatic stellate cells and promotes liver fibrosis via unconjugated cholic acid[J]. Advanced Science, 2024, 11(2): 2304408.
[5] Baghdasaryan A, Fuchs C D, Österreicher C H, et al. Inhibition of intestinal bile acid absorption improves cholestatic liver and bile duct injury in a mouse model of sclerosing cholangitis[J]. Journal of hepatology, 2016, 64(3): 674-681.
| Animal experiment [1]: | |
Animal models | Slc27a5−/− mice |
Preparation Method | To inhibit hepatic accumulation of cholic acid, 8‐week‐old male WT and Slc27a5−/− mice received CCl4 injection for 6 weeks and daily gavages of vehicle or bile acid transporter inhibitor Odevixibat (10mg/kg/day) in the final 4 weeks. After 4 weeks of Odevixibat treatment, mice were fasted overnight and then sacrificed for analysis. Liver specimens were fixed in 4% paraformaldehyde and then embedded in paraffin. Liver sections were sliced into 4 µm thicknesses, deparaffinized, and hydrated and then stained by standard methods. To analyze hepatic morphology and assess liver fibrosis, H&E and Sirius Red staining were performed. Sections were immune‐stained with antibodies against α‐SMA (1:300) or RUNX2 (1:300) overnight at 4°C. Sections were then incubated with a secondary anti-rabbit or anti-mouse IgG and stained using 3,3′‐diaminobenzidine. The immunohistochemical staining was semi‐quantitatively analyzed using the immunoreactive scoring system. |
Dosage form | 10mg/kg/day for 4 weeks; p.o. |
Applications | Odevixibat treatment mitigated liver fibrosis in Slc27a5−/− mice and decreased the expression of α‐SMA and RUNX2 proteins. |
References: | |
| Cas No. | 501692-44-0 | SDF | |
| المرادفات | A4250 | ||
| Formula | C37H48N4O8S2 | M.Wt | 740.93 |
| الذوبان | DMSO : 166.67 mg/mL (224.95 mM; Need ultrasonic) | Storage | Store at -20°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3497 mL | 6.7483 mL | 13.4966 mL |
| 5 mM | 269.9 μL | 1.3497 mL | 2.6993 mL |
| 10 mM | 135 μL | 674.8 μL | 1.3497 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)