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.
For research use only. We do not sell to patients.
- CAS No.: 1684439-46-0
- Formula: C145H248N50O44S4
- Molecular Weight:3524.09
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
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.
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.
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Animal Model:Male rabbits (weight 2.3 kg, median age 5 months) with iliac artery endothelial trauma[3]
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Dosage:0.1 mg/kg/day (diluted with normal saline)
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Administration:Subcutaneous injection, once daily for 4 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1684439-46-0
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Molecular Weight 3524.09
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Formula C145H248N50O44S4
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Synonyms
Brain Natriuretic Peptide-32 human acetate; BNP-32 acetate
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Sequence
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH (Disulfide bridge: Cys10-Cys26)
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Sequence Shortening
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)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nesiritide acetate Related Classifications
HY-P0003A Related Classifications
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