BT-11
目录号 : GC30803Omilancor (BT-11) is an orally active lanthionine synthetase C-like 2 (LANCL2) binding compound for treating inflammatory bowel disease (IBD) (Kd value of 7.7 ?M).
Cas No.:1912399-75-7
Sample solution is provided at 25 µL, 10mM.
Omilancor (BT-11) is an orally active lanthionine synthetase C-like 2 (LANCL2) binding compound for treating inflammatory bowel disease (IBD) (Kd value of 7.7 ?M).
In vitro measurement of cAMP in mouse splenocytes extracted from either WT or LANCL2?/? mice and treated with increasing doses of BT-11 demonstrates BT-11 stimulates cAMP production by activating the LANCL2 pathway[1].
Oral treatment with BT-11 (8 mg/kg/day) ameliorates colitis in mice. Safety assessment in rats indicateds that Oral treatment with BT-11 at high doses has an excellent safety profile up to 1000 mg/kg/day. In a dextran sodium sulfate colitis mouse model, oral administration of BT-11 upregulates the expression of IL-10 and downregulates the expression of TNF-α mRNA. It also upregulates LANCL2 expression in the gastrointestinal tract[1].
[1] Carbo A, et al. J Med Chem. 2016, 59(22):10113-10126.
Animal experiment: | Rats: Male Harlan Sprague Dawley rats are treated with a single oral dose of 500 mg/kg and 80 mg/kg/d for 14 days. Treated and control rats are observed for behavioral detriments, and blood and tissues are collected for clinical pathology and histopathological examination[2]. Mice: Wild type and LANCL2−/− male mice are treated with 8 mg/kg/d BT-11 over 8 weeks. Mice are sacrificed and spleens are collected for splenocytes isolation. Cell lysates are collected and cAMP intracellular concentration is measured[1]. |
References: [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. |
Cas No. | 1912399-75-7 | SDF | |
Canonical SMILES | O=C(N1CCN(C(C2=NC(C3=NC4=CC=CC=C4N3)=CC=C2)=O)CC1)C5=NC(C6=NC7=CC=CC=C7N6)=CC=C5 | ||
分子式 | C30H24N8O2 | 分子量 | 528.56 |
溶解度 | DMSO : ≥ 30 mg/mL (56.76 mM) | 储存条件 | Store at -20°C |
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制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.8919 mL | 9.4597 mL | 18.9193 mL |
5 mM | 0.3784 mL | 1.8919 mL | 3.7839 mL |
10 mM | 0.1892 mL | 0.946 mL | 1.8919 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
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