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BVT 2733 

Cat. No.: HY-18054 Purity: 99.82%
Handling Instructions

BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.

For research use only. We do not sell to patients.

BVT 2733 Chemical Structure

BVT 2733 Chemical Structure

CAS No. : 376640-41-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 86 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 78 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease[1].

IC50 & Target

IC50: 96 nM (mouse 11β-HSD1)
IC50: 3341 nM (human 11β-HSD1)[1]

In Vitro

BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 µM) reduces MCP-1 expression in fully differentiation adipocytes[3].
BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium in J774.1 macrophages by Elisa[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[3]

Cell Line: Differentiation adipocytes
Concentration: 100 μM
Incubation Time: 24 hours
Result: Down-regulated MCP-1 mRNA level.
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[2].
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Collagen-induced arthritis (CIA) mice[2]
Dosage: 100 mg/kg
Administration: Oral administration; twice daily; 2 weeks
Result: Reduced synovial inflammation and joint destruction.
Animal Model: C57BL/6J mice[3]
Dosage: 100 mg/kg
Administration: Oral administration; dosed (09.00 and 17.00 h); last 4 weeks
Result: Improved metabolic homeostasis and suppressed the inflammation of adipose tissue in diet-induced obese mice. 
Molecular Weight

428.96

Formula

C₁₇H₂₁ClN₄O₃S₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (116.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3312 mL 11.6561 mL 23.3122 mL
5 mM 0.4662 mL 2.3312 mL 4.6624 mL
10 mM 0.2331 mL 1.1656 mL 2.3312 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
BVT 2733
Cat. No.:
HY-18054
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