BT-11 - CAS 1912399-75-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C30H24N8O2
Molecular Weight:
528.56
COA:
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Targets:
AChE
Description:
BT-11, the extract of dried root of Polygala tenuifolia Willdenow, is an orally available LANCL2 binding compound for treating inflammatory bowel disease. In addition, BT-11 inhibited acetylcholinesterase (AChE) activity in a dose-dependent and non-competitive manner (IC50= 263.7 μg/ml).
Synonyms:
[4-[6-(1H-benzimidazol-2-yl)pyridine-2-carbonyl]piperazin-1-yl]-[6-(1H-benzimidazol-2-yl)pyridin-2-yl]methanone
Solubility:
DMSO: ≥30 mg/mL
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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Boiling Point:
923.4±75.0 ℃ at 760 Torr
Density:
1.424±0.06 g/cm3
InChIKey:
MVHWZNBAQIGPOQ-UHFFFAOYSA-N
InChI:
1S/C30H24N8O2/c39-29(25-13-5-11-23(31-25)27-33-19-7-1-2-8-20(19)34-27)37-15-17-38(18-16-37)30(40)26-14-6-12-24(32-26)28-35-21-9-3-4-10-22(21)36-28/h1-14H,15-18H2,(H,33,34)(H,35,36)
Canonical SMILES:
C1CN(CCN1C(=O)C2=CC=CC(=N2)C3=NC4=CC=CC=C4N3)C(=O)C5=CC=CC(=N5)C6=NC7=CC=CC=C7N6
1.Activation of LANCL2 by BT-11 Ameliorates IBD by Supporting Regulatory T Cell Stability Through Immunometabolic Mechanisms.
Leber A;Hontecillas R;Zoccoli-Rodriguez V;Bassaganya-Riera J Inflamm Bowel Dis. 2018 Apr 28. doi: 10.1093/ibd/izy167. [Epub ahead of print]
Background: ;Inflammatory bowel disease (IBD) afflicts 5 million people and is increasing in prevalence. There is an unmet clinical need for safer and effective treatments for IBD. The BT-11 is a small molecule oral therapeutic that ameliorates IBD by targeting lanthionine synthetase C-like 2 (LANCL2) and has a benign safety profile in rats.;Methods: ;Mdr1a-/-, dextran sodium sulphate , and adoptive transfer mouse models of colitis were employed to validate therapeutic efficacy and characterize the mechanisms of therapeutic efficacy of BT-11. In vitro cultures of CD4+ T cell differentiation and human peripheral blood mononuclear cells from Crohn's disease patients were used to determine its potential for human translation.;Results: ;BT-11 reduces inflammation in multiple mouse models of IBD. Oral treatment with BT-11 increases the numbers of lamina propria regulatory T cells (Tregs) in a LANCL2-dependent manner. In vitro, BT-11 increases the differentiation in Treg phenotypes, the upregulation of genes implicated in Treg cell stability, and conditions Treg cells to elicit greater suppressive actions. These immunoregulatory effects are intertwined with the ability of BT-11 to regulate late stage glycolysis and tricarboxylic acid cycle.
2.Effects of BT-11 on memory in healthy humans.
Lee JY;Kim KY;Shin KY;Won BY;Jung HY;Suh YH Neurosci Lett. 2009 Apr 24;454(2):111-4. doi: 10.1016/j.neulet.2009.03.024. Epub 2009 Mar 11.
We previously reported that BT-11, the extract of dried roots of Polygala tenuifolia Willdenow, had neuroprotective effects and improved scopolamine- and stress-induced amnesia in rats. It also blocked the activity of acetylcholinesterase and enhanced glucose utilization in the rat brain. Therefore, we examined whether BT-11 could enhance memory in healthy humans. This study was a randomized, double-blind, placebo-controlled, parallel-group study of BT-11 in healthy adults. The participants were given capsules of BT-11 or placebo 3 times daily for 4 weeks. The Korean version of the California Verbal Learning Test (K-CVLT) and the Self-Ordered Pointing Test (SOPT) were used to assess verbal memory and working memory, respectively. The subjects in BT-11-treated group showed more significant increases in immediate recall on the K-CVLT than those in the placebo-treated group. In a comparison within each group, the subjects' scores on most subtests of the K-CVLT were significantly increased by both placebo and BT-11 treatment. Interestingly, the subjects' scores on the recognition subtest of the K-CVLT were significantly increased by BT-11 treatment but not by placebo treatment. Also, BT-11 treatment significantly reduced the number of errors on the SOPT, whereas placebo treatment did not.
3.An N,N-Bis(benzimidazolylpicolinoyl)piperazine (BT-11): A Novel Lanthionine Synthetase C-Like 2-Based Therapeutic for Inflammatory Bowel Disease.
Carbo A;Gandour RD;Hontecillas R;Philipson N;Uren A;Bassaganya-Riera J J Med Chem. 2016 Nov 23;59(22):10113-10126. Epub 2016 Nov 15.
Lanthionine synthetase C-like 2 (LANCL2), a novel therapeutic target for inflammatory and autoimmune diseases and diabetes, exerts anti-inflammatory and insulin-sensitizing effects. This study reports the first LANCL2-based therapeutics for inflammatory bowel disease (IBD). Analogues of 1 (ABA) and 2 (NSC61610) were screened by molecular docking, then synthesized and analyzed for binding to LANCL2 by surface plasmon resonance. Piperazine-1,4-diylbis(6-benzo[d]imidazole-2-yl)pyridine-2-yl)methanone, 7, was identified as the lead LANCL2-binding compound for treating IBD. The oral treatment with 7 (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 7, suggesting high selectivity for the target. In conclusion, 7 merits continued development as a LANCL2-based, first-in-class orally active therapeutic for IBD.
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CAS 1912399-75-7 BT-11

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