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.
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- CAS No.: 1684439-46-0
- 화학식: C145H248N50O44S4
- 분자량:3524.09
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보관:
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
- 순도&문서
- 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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분자량 3524.09
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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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