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BT-11 Sale

目录号 : GC30803

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).

BT-11 Chemical Structure

Cas No.:1912399-75-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,047.00
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2mg
¥540.00
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5mg
¥900.00
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10mg
¥1,350.00
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50mg
¥4,050.00
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100mg
¥6,750.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

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.
[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.

化学性质

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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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。
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溶解性数据

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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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