Rosuvastatin | China | Manufacturer | Henan Fengda Chemical Co., Ltd

Price	$10	$6	$2
Package	1KG	100KG	1000KG

Product Details

Product Name: Rosuvastatin	CAS No.: 287714-41-4
Min. Order: 1KG	Purity: 99%
Supply Ability: g-kg-tons, free sample is available	Release date: 2024/04/28
Lead time: In stock	Packaging: bottle/drum/bucket/IBC, as request.
Delivery: By sea, by air, by express	Origin: Manufacturer

1. Product information

Name	rosuvastatin
Synonym	More Synonyms

Description	Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> HMG-CoA Reductase (HMGCR) Research Areas >> Metabolic Disease
References	[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44. [2]. Schneck, D.W., et al., The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther, 2004. 75(5): p. 455-63. [3]. Kim, Y.S., et al., Rosuvastatin suppresses the inflammatory responses through inhibition of c-Jun N-terminal kinase and Nuclear Factor-kappaB in endothelial cells. J Cardiovasc Pharmacol, 2007. 49(6): p. 376-83. [4]. Carswell, C.I., G.L. Plosker, and B. Jarvis, Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7. [5]. Stalker, T.J., A.M. Lefer, and R. Scalia, A new HMG-CoA reductase inhibitor, rosuvastatin, exerts anti-inflammatory effects on the microvascular endothelium: the role of mevalonic acid. Br J Pharmacol, 2001. 133(3): p. 406-12.

Description

Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].

Related Catalog

Signaling Pathways >> Metabolic Enzyme/Protease >> HMG-CoA Reductase (HMGCR)

Research Areas >> Metabolic Disease

References

[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44.

[2]. Schneck, D.W., et al., The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther, 2004. 75(5): p. 455-63.

[3]. Kim, Y.S., et al., Rosuvastatin suppresses the inflammatory responses through inhibition of c-Jun N-terminal kinase and Nuclear Factor-kappaB in endothelial cells. J Cardiovasc Pharmacol, 2007. 49(6): p. 376-83.

[4]. Carswell, C.I., G.L. Plosker, and B. Jarvis, Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.

[5]. Stalker, T.J., A.M. Lefer, and R. Scalia, A new HMG-CoA reductase inhibitor, rosuvastatin, exerts anti-inflammatory effects on the microvascular endothelium: the role of mevalonic acid. Br J Pharmacol, 2001. 133(3): p. 406-12.

Density	1.368 g/cm3
Boiling Point	745.6ºC at 760 mmHg
Molecular Formula	C22H28FN3O6S
Molecular Weight	481.54
Flash Point	404.7ºC
PSA	152.13000
LogP	2.14780
Vapour Pressure	2.38E-23mmHg at 25°C
Index of Refraction	1.597
Storage condition	2-8°C

2. Packaging

For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.

Or smaller package 1kg/bottle, 10kgs/bottle as request.

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3. Shipping

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4. Contact information

For more details, pls contact us freely.

Mob: 86 17630971917

WhatsApp/Skype/Wechat/LINE: 86 17630971917

Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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Henan Fengda Chemical Co., Ltd

Min. Order:	1KG
Supply Ability:	g-kg-tons, free sample is available
Update Time:	2024-04-28