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Bezafibrate,41859-67-0,IC-0201356
Click£º3457     Release date£º2012-3-1    Author£ºAdministrator    Source£ºOriginal

Bezafibrate,41859-67-0

Cat.No.:IC-0201356

Product Information

Biological Activity

Bezafibrate is an agonist of PPAR, with EC50s of 50 ¦ÌM, 60 ¦ÌM, 20 ¦ÌM for human PPAR¦Á, PPAR¦Ã and PPAR¦Ä, and 90 ¦ÌM, 55 ¦ÌM, 110 ¦ÌM for murine PPAR¦Á, PPAR¦Ã and PPAR¦Ä, respectively; Bezafibrate is used as an hypolipidemic agent.Bezafibrate is an agonist of PPAR, with EC50s of 90 ¦ÌM, 55 ¦ÌM, 110 ¦ÌM for murine PPAR¦Á, PPAR¦Ã and PPAR¦Ä, and 50 ¦ÌM, 60 ¦ÌM, 20 ¦ÌM for human PPAR¦Á, PPAR¦Ã and PPAR¦Ä, respectively[1]. Bezafibrate (> 200 ¦ÌM) shows significant cytotoxicity against human retinal microvascular endothelial cells (HRMECs) and human retinal pigment epithelial ARPE-19 cells. Bezafibrate (30-100 ¦ÌM) suppresses tumor necrosis factor (TNF)¦Á induced inflammatory factors and regulates TNF¦Á induced nuclear factor (NF)-¦ÊB transactivation in HRMEC. Bezafibrate inhibits VEGF-induced HRMECs migration, and inhibits interleukin (IL)-1¦Â-induced VEGF secretion of ARPE-19 cells[2].Bezafibrate (0.5%) markedly reduces plasma lipid and glucose levels, and increases islet area in the pancreas in TallyHo mice. Bezafibrate also improves energy expenditure and metabolic flexibility. Moreover, Bezafibrate ameliorates steatosis, modifies lipid composition and increases mitochondrial mass in the liver[3].

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

Quantity

Price($£©

Price(€)

Price(£¤/CNY£©

Price(£¤/JYP£©

100mg

$44.50

€53.40

£¤445.00

¥8,855.50

500mg

$85.00

€102.00

£¤850.00

¥16,915.00

1g

$120.00

€144.00

£¤1,200.00

¥23,880.00

 

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

361.82

Formula

C19H20ClNO4

CAS Number

41859-67-0

Purity

 >99.00%

Solubility

17.25mg/mL in DMSO

Storage

 -20¡æ

Reference

[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.

[2]. Usui-Ouchi A, et al. The peroxisome proliferator-activated receptor pan-agonist bezafibrate suppresses microvascular inflammatory responses of retinal endothelial cells and vascular endothelial growth factor production in retinal pigmented epithelial cells. Int Immunopharmacol. 2017 Nov;52:70-76.

[3]. Franko A, et al. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266.

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