bvt-2733

Cas：376640-41-4

Product Information：

bVT-2733 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, which attenuates obesity and inflammation in diet-induced obese mice. BVT-2733 protects osteoblasts against endogenous glucocorticoid induced dysfunction. BVT-2733 exhibits an anti-inflammatory effect on CIA. This protective effect is, at least partly, mediated by inhibition of the NF-κB and NLRP1 inflammasome signaling pathways. 11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1) plays an important role in inflammation. 11β-HSD1 inhibition may represent a potential therapeutic target for RA patients.

Chemical Formula: C17H21ClN4O3S2

Exact Mass: 428.07436

Molecular Weight: 428.95

Elemental Analysis: C, 47.60; H, 4.93; Cl, 8.26; N, 13.06; O, 11.19; S, 14.95

Synonym: 

BVT-2733

BVT 2733

BVT2733

BVT.2733

Chemical Name:

3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide

InChi Key: 

YDPRNGAPPNPYQQ-UHFFFAOYSA-N

InChi Code: 

InChI=1S/C17H21ClN4O3S2/c1-12-14(18)4-3-5-15(12)27(24,25)20-

17-19-13(11-26-17)10-16(23)22-8-6-21(2)7-9-22/h3-5,11H,6-10H2,1-2H3,(H,19,20)

Smiles Code:

CN1CCN(C(CC2=CSC(NS(=O)(C3=CC=CC(Cl)=C3C)=O)=N2)=O)CC1

Technical Data：

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 µM) reduces MCP-1 expression in fully differentiation adipocytes.

BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium in J774.1 macrophages by Elisa.

In Vivo：

BVT-2733 (oral administration; 100 mg/kg; twice daily; 2 weeks) attenuates the arthritis severity and anti-CII level and decreases the levels of serum TNF-α, IL-1β, IL-6 and IL-17 in CIA mice.

BVT 2733 (oral administration; 100 mg/kg; dosed (09.00 and 17.00 h); last 4 weeks) exhibits decreased body weight and enhanced glucose tolerance and insulin sensitivity when it compares to control mice. It also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo.

References：

1. Zhang L, Dong Y, Zou F, Wu M, Fan C, Ding Y. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94. doi: 10.1016/j.intimp.2013.07.015. Epub 2013 Aug 11. PubMed PMID: 23938253.

2. Wu L, Qi H, Zhong Y, Lv S, Yu J, Liu J, Wang L, Bi J, Kong X, Di W, Zha J, Liu F, Ding G. 11β-Hydroxysteroid dehydrogenase type 1 selective inhibitor BVT.2733 protects osteoblasts against endogenous glucocorticoid induced dysfunction. Endocr J. 2013;60(9):1047-58. Epub 2013 Jun 12. PubMed PMID: 23759754.

3. Liu J, Kong X, Wang L, Qi H, Di W, Zhang X, Wu L, Chen X, Yu J, Zha J, Lv S, Zhang A, Cheng P, Hu M, Li Y, Bi J, Li Y, Hu F, Zhong Y, Xu Y, Ding G. Essential roles of 11β-HSD1 in regulating brown adipocyte function. J Mol Endocrinol. 2013 Jan 11;50(1):103-13. doi: 10.1530/JME-12-0099. Print 2013 Feb. PubMed PMID: 23197361.

4. Wang L, Liu J, Zhang A, Cheng P, Zhang X, Lv S, Wu L, Yu J, Di W, Zha J, Kong X, Qi H, Zhong Y, Ding G. BVT.2733, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, attenuates obesity and inflammation in diet-induced obese mice. PLoS One. 2012;7(7):e40056. doi: 10.1371/journal.pone.0040056. Epub 2012 Jul 2. PubMed PMID: 22768329; PubMed Central PMCID: PMC3388048.

5. Liu J, Wang L, Zhang A, Di W, Zhang X, Wu L, Yu J, Zha J, Lv S, Cheng P, Hu M, Li Y, Qi H, Ding G, Zhong Y. Adipose tissue-targeted 11β-hydroxysteroid dehydrogenase type 1 inhibitor protects against diet-induced obesity. Endocr J. 2011;58(3):199-209. Epub 2011 Feb 17. PubMed PMID: 21325744.

Products are for research use only. Not for human use.