Odevixibat
(Synonyms: A4250) 目录号 : GC63126
Odevixibat（A4250）是一种强效、选择性的肠道胆汁酸转运蛋白（IBAT）抑制剂，IC50值为0.16nM。
Cas No.:501692-44-0
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
Odevixibat（A4250）是一种强效、选择性的肠道胆汁酸转运蛋白（IBAT）抑制剂，IC50值为0.16nM[1]。Odevixibat通过减少肠道对胆汁酸的再吸收并促进结肠清除胆汁酸，从而降低血清胆汁酸水平[2]，Odevixibat已被用于血清胆汁酸调节和改善肝脏功能指标相关研究[3]。
在体内，Slc27a5−/−小鼠口服10mg/kg/day剂量的Odevixibat连续4周后，肝脏纤维化显著改善，表现为肝胶原沉积减少、α-SMA表达下降，同时肝功能指标得到提升[4]。在Mdr2−/−小鼠模型中，饲喂含0.01%（w/w）Odevixibat的饮食4周可明显缓解硬化性胆管炎症状，包括胆管损伤减轻、胆汁酸分泌减少以及粪便胆汁酸排泄增加[5]。
| 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 | |
| 别名 | A4250 | ||
| 分子式 | C37H48N4O8S2 | 分子量 | 740.93 |
| 溶解度 | DMSO : 166.67 mg/mL (224.95 mM; Need ultrasonic) | 储存条件 | Store at -20°C, stored under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 | 0.135 mL | 0.6748 mL | 1.3497 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet