bvt-2733

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.

Product information

CAS Number: 376640-41-4

Molecular Weight: 428.96

Formula: C17H21ClN4O3S2

Synonym:

BVT-2733

BVT.2733

BVT 2733

BVT2733

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

Smiles: CN1CCN(CC1)C(=O)CC1=CSC(NS(=O)(=O)C2=CC=CC(Cl)=C2C)=N1

InChiKey: YDPRNGAPPNPYQQ-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

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

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.

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