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BT-11
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BT-11图片
CAS NO:1912399-75-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 528.2
Formula C30H24N8O2
CAS No.1912399-75-7 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 30 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) O=C(N1CCN(C(C2=NC(C3=NC4=CC=CC=C4N3)=CC=C2)=O)CC1)C5=NC(C6=NC7=CC=CC=C7N6)=CC=C5
Synonyms BT-11; BT 11; BT11
实验参考方法
In Vitro

In vitro activity: BT-11 is a first-in-class, potent, orally available and selective modulator of LANCL2 (Lanthionine synthetase C-like 2) which is a novel therapeutic target for inflammatory and autoimmune diseases and diabetes, exerts anti-inflammatory and insulin-sensitizing effects. BT-11 at high doses has an excellent safety profile up to 1000 mg/kg/day. It has demonstrated therapeutic efficacy in 3 validated mouse models of colitis at doses as low as 8 mg/kg/d; It protects from IBD by targeting LANCL2. BT-11 has potential to be a safe and effective orally active therapeutic for IBD. The oral treatment with BT-11 (8 mg/kg/d) in a mouse model of IBD resulted 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 demonstrated that loss of LANCL2 abrogated beneficial actions of BT-11, suggesting high selectivity for the target. In conclusion, BT-11 merits continued development as a LANCL2-based, first-in-class orally active therapeutic for IBD.


Kinase Assay: LANCL2 engagement produces an increase of PKA, followed by an accumulation of cAMP in the cytoplasm. BT-11 treatment splenocytes shows a dose–response increase of cAMP production. BT-11 stimulates cAMP production by activating the LANCL2 pathway.

In VivoOral treatment with BT-11 at 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[1]. 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
Animal model Male Harlan Sprague Dawley rats and Wild type and LANCL2–/– male mice with IBD models
Formulation & Dosage 8 mg/kg/d for mouse model; 500 mg/kg and 80 mg/kg/d for rats; oral
References Int J Toxicol. 2016 Sep;35(5):521-9; J Med Chem. 2016 Nov 23;59(22):10113-10126.