Nesiritide acetate
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1684439-46-0
- 分子式: C145H248N50O44S4
- 分子量:3524.09
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Calcium Channel アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
体外実験
Nesiritide (1 nM-1 μM) acetate significantly decreases cell shortening in ventricular myocytes isolated from rat hearts in a dose-dependent manner[1].
Nesiritide (1 μM) acetate increases the V1/2 activation of the L-type calcium channel by 51.1% and decreases V1/2 inactivation by 31.8% in ventricular myocytes isolated from rat hearts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
Nesiritide (0.1 mg/kg/day; s.c.; once daily; 4 weeks) acetate protects endothelial function after balloon-induced trauma in the iliac artery in rabbits[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male rabbits (weight 2.3 kg, median age 5 months) with iliac artery endothelial trauma[3]
-
Dosage:0.1 mg/kg/day (diluted with normal saline)
-
Administration:Subcutaneous injection, once daily for 4 weeks
-
Result:Inhibited remodeling of rabbit iliac artery following endothelial trauma.
Reduced plasma levels of ET-1 and vWF.
Increased plasma level of NO, and decreased the ratio of PCNA positive expression.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 1684439-46-0
-
分子量 3524.09
-
分子式 C145H248N50O44S4
-
別名
Brain Natriuretic Peptide-32 human acetate; BNP-32 acetate
-
配列
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH (Disulfide bridge: Cys10-Cys26)
-
シーケンスの短縮
Ser-Pro-Lys-Met-Val-Gln-Gly-Ser-Gly-Cys-Phe-Gly-Arg-Lys-Met-Asp-Arg-Ile-Ser-Ser-Ser-Ser-Gly-Leu-Gly-Cys-Lys-Val-Leu-Arg-Arg-His (Disulfide bridge: Cys10-Cys26)
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
純度とドキュメンテーション
参考文献
[1]. Sodi R, et al. B-type natriuretic peptide (BNP) attenuates the L-type calcium current and regulates ventricular myocyte function. Regul Pept. 2008 Nov 29;151(1-3):95-105. [Content Brief]
[2]. Lazar HL, et al. Nesiritide enhances myocardial protection during the revascularization of acutely ischemic myocardium. J Card Surg. 2009 Sep-Oct;24(5):600-5. [Content Brief]
[4]. Liu SQ, et al. Treatment with nesiritide, a recombinant B-type natriuretic Peptide, reduces vascular remodeling following balloon-induced endothelial injuries in rabbits. Tohoku J Exp Med. 2010 Nov;222(3):219-23. [Content Brief]
[5]. Liu SQ, et al. Recombinant B-type natriuretic peptide nesiritide attenuates vascular remodelling by reducing plasma aldosterone in rabbits. Heart Lung Circ. 2012 Sep;21(9):551-5. [Content Brief]
[6]. Hobbs RE, et al. Therapeutic potential of nesiritide (recombinant b-type natriuretic peptide) in the treatment of heart failure. Expert Opin Investig Drugs. 1999 Jul;8(7):1063-72. [Content Brief]
[7]. Koller KJ, et al. Molecular biology of the natriuretic peptides and their receptors. Circulation. 1992 Oct;86(4):1081-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Nesiritide acetate 関連分類
HY-P0003A 関連分類
Powered by Bioz