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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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S C Mah et al.
Peptides, 9(3), 595-600 (1988-05-01)
The interaction of an antagonist of arginine vasopressin (AVP), d(CH2)5-D-Tyr(Et)VAVP, with renal tubular V2 receptors were studied in medullary membrane preparations from kidneys of Sprague-Dawley and Brattleboro rats. In both rat strains, V2 receptors had comparable KD and Bmax values
A H Tang et al.
Life sciences, 43(5), 399-403 (1988-01-01)
Water diuresis was produced in rats after s.c. injections of d(CH2)5,D-Ile2,Ile4-AVP (compound 1) and d(CH2)5,Tyr(OEt)2Val4-AVP (compound 2). Compound 1 is known to be a more potent antagonist against the antidiuretic effect, while Compound 2 is a more potent antagonist against
V2-like vasopressin receptor mobilizes intracellular Ca2+ in rat medullary collecting tubules.
Champigneulle, A., et al.
The American Journal of Physiology, 265 (1993)
J F Liard
The American journal of physiology, 255(6 Pt 2), H1325-H1329 (1988-12-01)
We examined the hypothesis that V2-like receptors might contribute to the hemodynamic response seen after blockade of the vasoconstrictor (V1) effect of arginine vasopressin (AVP) in nonhypotensive hemorrhage. Seven chronically instrumented dogs were bled 15 ml/kg within 15 min on
L B Kinter et al.
The Journal of pharmacology and experimental therapeutics, 241(3), 797-803 (1987-06-01)
Vasopressin antagonism and water diuresis (aquaresis) is demonstrated after i.p. or i.v. administration of vasopressin antagonists in a primate species, the squirrel monkey (Saimiri sciureus). Antagonism of vasopressin-stimulated renal medullary adenylate cyclase activity was evaluated in vitro; the most potent
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