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132956-87-7

132956-87-7 Structure

132956-87-7 Structure
IdentificationBack Directory
[Name]

A 71915
[CAS]

132956-87-7
[Synonyms]

A 71915
A-71915TFA
RC-{Cyclohexyl-Ala}-GGRIDRI-{d-Tic}-RC
H-Arg-Cys-b-cyclohexyl-Ala-Gly-Gly-Arg-Ile-Asp-Arg-Ile-D-Tic-Arg-Cys-NH2
(Arg6,b-cyclohexyl-Ala8,D-Tic16,Arg17,Cys18)-Atrial Natriuretic Factor (6-18) aMide (Mouse, rabbit, rat)
(Arg6,β-cyclohexyl-Ala8,D-Tic16,Arg17,Cys18)-Atrial Natriuretic Factor (6-18) amide (mouse, rabbit, rat)
10H-[1,2,5,8,11,14,17,20,23,26,29,32,35]Dithiaundecaazacyclooctatriacontino[11,10-b]isoquinoline,cyclic peptide deriv
(Arg,β-cyclohexyl-Ala,D-Tic1,Arg1,Cys1)-Atrial Natriuretic Factor (6-18) amide (mouse, rabbit, rat) trifluoroacetate salt
L-Cysteinamide, L-arginyl-L-cysteinyl-3-cyclohexyl-L-alanylglycylglycyl-L-arginyl-L-isoleucyl-L-α-aspartyl-L-arginyl-L-isoleucyl-(3R)-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-arginyl-, cyclic (2→13)-disulfide
[Molecular Formula]

C69H117N25O16S2
[MDL Number]

MFCD00672741
[MOL File]

132956-87-7.mol
[Molecular Weight]

1616.97
Chemical PropertiesBack Directory
[density ]

1.52±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[pka]

4.00±0.10(Predicted)
[color ]

White to off-white
[Water Solubility ]

Soluble to 1 mg/ml in water
[Sequence]

Arg-Cys-{Cha}-Gly-Gly-Arg-Ile-Asp-Arg-Ile-{d-Tic}-Arg-Cys-NH2 (Disulfide bridge: Cys2-Cys13)
Safety DataBack Directory
[WGK Germany ]

WGK 3
[Storage Class]

11 - Combustible Solids
Hazard InformationBack Directory
[Description]

A 71915 is an atrial natricuretic factor receptor antagonist. It blocks physiological effects of angiotensin.
[Uses]

A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells[1].
[in vivo]

A 71915 (5 μl; i.m.; 25-30 g male CD-1 mice) affects BNP (1 nmol)- and GRP (0.1 nmol)-induced scratching[2]. A 71915 (30 μg/ kg/ day) inhibits NS-398 on blood pressure decreased[3].

Animal Model:Rat (Male Sprague-Dawley); weighing 150-180 g[3]
Dosage:30 μg/kg/day; infused for 3 weeks
Administration:via a mini-osmotic pump
Result:The inhibitory effect of NS-398 on blood pressure was attenuated by the pretreatment with A 71915 (30 μg/kg/day).
[storage]

Store at -20°C
[References]

[1] Delporte C, et al. Discovery of a potent atrial natriuretic peptide antagonist for ANPA receptors in the human neuroblastoma NB-OK-1 cell line. Eur J Pharmacol. 1992;224(2-3):183-188. DOI:10.1016/0014-2999(92)90803-c
[2] Kiguchi N, et al. Spinal Functions of B-Type Natriuretic Peptide, Gastrin-Releasing Peptide, and Their Cognate Receptors for Regulating Itch in Mice. DOI:10.1124/jpet.115.229997
[3] Park BM, et al. Attenuation of renovascular hypertension by cyclooxygenase-2 inhibitor partly through ANP release. Peptides. 2015;69:1-8. DOI:10.1016/j.peptides.2015.03.022
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