| 产品描述: | InformationBT-11 is an orally activelanthionine synthetase C-like 2 (LANCL2)binding compound for treating inflammatory bowel disease (IBD) (Kd value of 7.7 µM). |
| 体内研究: |
The oral treatment with BT-11 (8 mg/kg/d) in a mouse model of inflammatory bowel disease results in lowering the disease activity index, decreasing colonic inflammatory lesions by 4-fold, and suppressing inflammatory markers (e.g., TNF-α, and interferon-γ) in the gut. Furthermore, studies in LANCL2−/− mice demonstrates that loss of LANCL2 abrogates beneficial actions of BT-11, suggesting high selectivity for the target. Oral treatment with BT-11 (8 mg/kg/day) ameliorates colitis in mice. Initial safety assessment in rats indicates that oral treatment with BT-11 at high doses has an excellent safety profile up to 1000 mg/kg/day. BT-11 is well tolerated in rats, and may hold promise as an orally active therapeutic for Crohn’s disease. One hour after oral administration of a single dose of 80 mg/kg, BT-11 has a maximal concentration of 21 ng/mL; the half-life is 3 hours. |
| 参考文献: |
1. Carbo A, et al. An N,N-Bis(benzimidazolylpicolinoyl)piperazine (BT-11): A Novel Lanthionine Synthetase C-Like 2-Based Therapeutic for Inflammatory Bowel Disease. J Med Chem. 2016 Nov 23;59(22):10113-10126. 2. Bissel P, et al. Exploratory Studies With BT-11: A Proposed Orally Active Therapeutic for Crohn's Disease. Int J Toxicol. 2016 Sep;35(5):521-9. 3. Tubau-Juni N, et al. First-in-class topical therapeutic omilancor ameliorates disease severity and inflammation through activation of LANCL2 pathway in psoriasis. Sci Rep. 2021 Oct 6;11(1):19827. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.892 ml |
9.46 ml |
18.919 ml |
| 5 mM |
0.378 ml |
1.892 ml |
3.784 ml |
| 10 mM |
0.189 ml |
0.946 ml |
1.892 ml |
| 50 mM |
0.038 ml |
0.189 ml |
0.378 ml |
|
| 注意: |
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