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Chemical Structure| 376640-41-4 Chemical Structure| 376640-41-4

Structure of BVT 2733
CAS No.: 376640-41-4

Chemical Structure| 376640-41-4

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BVT 2733 is a small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1(11β-HSD1).

4.5 *For Research Use Only !

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Product Details of BVT 2733

CAS No. :376640-41-4
Formula : C17H21ClN4O3S2
M.W : 428.96
SMILES Code : O=S(C1=CC=CC(Cl)=C1C)(NC2=NC(CC(N3CCN(C)CC3)=O)=CS2)=O
MDL No. :MFCD13152134
InChI Key :YDPRNGAPPNPYQQ-UHFFFAOYSA-N
Pubchem ID :6918651

Safety of BVT 2733

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
THP-1 cells 100 μM 1 h BVT.2733, a selective inhibitor of 11β-HSD1 enzymatic activity, reduced the mRNA expression of pro-inflammatory cytokines and IL-1β protein secretion in LPS-induced THP-1 cells. Iran J Basic Med Sci. 2023 Mar;26(3):374-379
3T3-L1 preadipocytes 50-100 μM 24 h To evaluate the effect of BVT.2733 on the expression of inflammatory genes in PA or LPS-activated preadipocytes. Results showed that BVT.2733 reduced mRNA levels of MCP-1 and IL-6. PLoS One. 2012;7(7):e40056
J774A.1 macrophages 25-100 μM 24 h To evaluate the effect of BVT.2733 on the expression of inflammatory genes in PA or LPS-activated macrophages. Results showed that BVT.2733 reduced mRNA levels of MCP-1 and IL-6. PLoS One. 2012;7(7):e40056

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice High fat diet-induced obesity model Oral 100 mg/kg Twice daily for four weeks To evaluate the effect of BVT.2733 on obesity and inflammation. Results showed that BVT.2733 decreased body weight, improved glucose tolerance and insulin sensitivity, and reduced the expression of inflammation-related genes and macrophage infiltration in adipose tissue. PLoS One. 2012;7(7):e40056
C57BL/6 mice High-fat diet-induced obese mouse model Intraperitoneal injection 50 mg/kg Once daily for 30 days BVT 2733 attenuates high-fat diet-induced hepatic steatosis and liver injury, reduces lipolysis in adipose tissues and lipogenesis in the liver. Drug Des Devel Ther. 2021 May 31;15:2309-2324

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.31mL

4.66mL

2.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Alberts P, Engblom L, et al. Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice. Diabetologia. 2002 Nov;45(11):1528-32. Epub 2002 Sep 18.

[2]Wang L, Liu J, et al. 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.

[3]Zhang L, Dong Y, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94.

[4]Alberts P, Engblom L, Edling N, Forsgren M, Klingström G, Larsson C, Rönquist-Nii Y, Ohman B, Abrahmsén L. Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice. Diabetologia. 2002 Nov;45(11):1528-32. doi: 10.1007/s00125-002-0959-6. Epub 2002 Sep 18. PMID: 12436336.

[5]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. PMID: 22768329; PMCID: PMC3388048.

[6]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. PMID: 23938253.

 

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