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BNP-32 (human) acetate salt

Names

[ CAS No. ]:
124584-08-3

[ Name ]:
BNP-32 (human) acetate salt

[Synonym ]:
Nesiritide
NESIRITIDE ACETATE
RS 45041-190 hydrochloride

Biological Activity

[Description]:

Nesiritide is an agonist of natriuretic peptide receptors (NPRs), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Sequence: 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.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Cancer
Peptides

[Target]

Kd: 7.3 Pm (NPR-A), 13 pM (NPR-C)[1].


[In Vitro]

Nesiritide is an agonist of natriuretic peptide receptor (NPR), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively[1]. ProBNP1-108 stimulates guanylyl cyclase-A (GC-A) to near-maximum activities but is 13-fold less potent than Nesiritide (BNP1-32). ProBNP1-108 binds human GC-A 35-fold less tightly than Nesiritide. Neither proBNP1–108 nor Nesiritide activates GC-B. The natriuretic peptide clearance receptor binds proBNP1-108 3-fold less tightly than Nesiritide. The half time for degradation of proBNP1-108 by human kidney membranes is 2.7-fold longer than for Nesiritide, and the time required for complete degradation is 6-fold longer. Nesiritide and proBNP1-108 are best fitted by first- and second-order exponential decay models, respectively[2].

[References]

[1]. Koller KJ, et al. Molecular biology of the natriuretic peptides and their receptors. Circulation. 1992 Oct;86(4):1081-8.

[2]. Dickey DM, et al. ProBNP(1-108) is resistant to degradation and activates guanylyl cyclase-A with reduced potency. Clin Chem. 2011 Sep;57(9):1272-8.


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C143H244N50O42S4

[ Molecular Weight ]:
3464.037

[ Exact Mass ]:
3461.737793

[ PSA ]:
1613.94000

[ LogP ]:
-16.34

[ Index of Refraction ]:
1.679

[ Storage condition ]:
-20°C

MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Different Susceptibility of B-Type Natriuretic Peptide (BNP) and BNP Precursor (proBNP) to Cleavage by Neprilysin: The N-Terminal Part Does Matter.

Clin. Chem. 62 , 617-22, (2016)

Protease neprilysin is known to be responsible for the degradation of natriuretic peptides. A recent heart failure (HF) drug, LCZ696 (Entresto(TM)), that combines a neprilysin inhibitor and an angiote...


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Related Compounds

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