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Merck
CN

V4253

[β-巯基-β,β-环戊亚甲基丙酰1, O-Et-Tyr2, Val4, Arg8]-加压素

≥97% (HPLC)

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关于此项目

经验公式（希尔记法）:
C53H75N13O11S2
化学文摘社编号:
77453-01-1
分子量:
1134.37
NACRES:
NA.32
PubChem Substance ID:
329829049
UNSPSC Code:
51111800
MDL number:
MFCD00076752
Biological source:
synthetic (organic)
Form:
powder
Assay:
≥97% (HPLC)

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InChI

1S/C53H77N13O11S2/c1-4-77-34-19-17-33(18-20-34)26-36-46(71)62-37(25-32-13-7-5-8-14-32)48(73)65-44(31(2)3)50(75)63-38(27-41(54)67)47(72)64-39(30-78-79-53(28-43(69)60-36)21-9-6-10-22-53)51(76)66-24-12-16-40(66)49(74)61-35(15-11-23-58-52(56)57)45(70)59-29-42(55)68/h5,7-8,13-14,17-20,31,35-40,44H,4,6,9-12,15-16,21-30H2,1-3H3,(H2,54,67)(H2,55,68)(H,59,70)(H,60,69)(H,61,74)(H,62,71)(H,63,75)(H,64,72)(H,65,73)(H4,56,57,58)/t35-,36-,37-,38-,39-,40-,44-/m0/s1

SMILES string

CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc4ccccc4)NC2=O)C(C)C)C(=O)N5CCC[C@H]5C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(N)=O)cc1

InChI key

SDFJYGJKEXYVCG-ZZTMPEIHSA-N

biological source

synthetic (organic)

assay

≥97% (HPLC)

form

powder

solubility

water: 1 mg/mL, clear, colorless

shipped in

ambient

storage temp.

−20°C

Quality Level

200

Gene Information

human ... AVPR1A(552), AVPR2(554), OXT(5020), OXTR(5021)
mouse ... AVPR1A(54140), AVPR2(12000)
rat ... AVPR1A(25107), AVPR2(25108), OXT(18429), OXTR(18430)

Application

[Beta-Mercapto-beta, beta-cyclopentamethylenepropionyl1, O-Et-Tyr2, Val4, Arg8]-Vasopressin is a potent V1a and V2 vasopressin receptor anatgonist, used for examining the impact of vasopressin V1receptor blockade in rats.The product was also be used for visualizing cell surface V1a receptors in rat hepatocytes by using high-affinity fluorescent linear antagonist, Rhm8 -PVA.

Biochem/physiol Actions

Vasopressin also known as antidiuretic hormone (ADH) or argipressin can stimulate three acid-base transporters and hence increases the capability of the cell to regulate pHi.ADH can induce reversible translocation of aquaporin-CD water channels from intracellular vesicles to apical plasma membrane, which in turn increases the water permeability of collecting duct cells.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H332

Hazard Classifications

Acute Tox. 4 Inhalation

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000267635
SLCQ8849
0000267635
SLCQ5706
031M1823V

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M Manning et al.
Journal of peptide science : an official publication of the European Peptide Society, 3(1), 31-46 (1997-01-01)
We report the solid-phase synthesis and some pharmacological properties of 12 position three modified analogues (peptides 1-12) of the potent non-selective antagonist of the antidiuretic (V2-receptor), vasopressor (V1a-receptor) responses to arginine vasopressin (AVP) and of the uterine contracting (OT-receptor) responses
J Filep et al.
The American journal of physiology, 253(5 Pt 2), F952-F958 (1987-11-01)
To investigate the role of arginine vasopressin (AVP) in the maintenance of blood pressure in deoxycorticosterone (DOC)-salt hypertension, the effects of specific pressor and antidiuretic antagonists of AVP were studied in conscious, freely moving rats with established malignant DOC-salt hypertension.
M Bosch-Marcé et al.
Gastroenterology, 109(1), 217-223 (1995-07-01)
It has recently been described that kappa-opioid receptor agonists inhibit antidiuretic hormone secretion and promote water excretion in humans and experimental animals. The aim of this study was to evaluate the aquaretic efficacy of the kappa-opioid receptor agonist RU 51599
M K Sun et al.
European journal of pharmacology, 304(1-3), 63-71 (1996-05-23)
We examined whether vasomotor neurons in the rostroventrolateral reticular nucleus of the medulla oblongata might be responsible for an acute increase in arterial pressure, elicited by application of angiotensin II in the central nervous system, as suggested by others. In
H Tsushima et al.
Japanese journal of pharmacology, 66(2), 241-246 (1994-10-01)
We investigated the effects of angiotensin II (Ang II), microinjected into the supraoptic (SON) and paraventricular (PVN) nuclei of rats, on the urine outflow rate and underlying mechanisms. Ang II produced antidiuretic effects in a dose-dependent manner with ED50 values
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