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V4253

Sigma-Aldrich

[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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About This Item

經驗公式（希爾表示法）:
C53H75N13O11S2
CAS號碼:
77453-01-1
分子量：:
1134.37
MDL號碼:
MFCD00076752
分類程式碼代碼:
51111800
PubChem物質ID:
329829049
NACRES:
NA.32
暫時無法取得訂價和供貨情況

生物源

synthetic (organic)

品質等級

200

化驗

≥97% (HPLC)

形狀

powder

溶解度

water: 1 mg/mL, clear, colorless

運輸包裝

ambient

儲存溫度

−20°C

SMILES 字串

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

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

InChI 密鑰

SDFJYGJKEXYVCG-ZZTMPEIHSA-N

基因資訊

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

Amino Acid Sequence

(1-Mercaptocyclohexyl)acetyl-Tyr(O-Ethyl)-Phe-Val-Asn-Cys-Pro-Arg-Gly-NH2 [Disulfide Bridge: 1-6]

應用

[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.[1]The product was also be used for visualizing cell surface V1a receptors in rat hepatocytes by using high-affinity fluorescent linear antagonist, Rhm8 -PVA.[2]

生化／生理作用

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.[3]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.[4]

象形圖

Exclamation mark
GHS07

訊號詞

Warning

危險聲明

H332

危險分類

Acute Tox. 4 Inhalation

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves

從最近期的版本中選擇一個：

分析證明 (COA)

Lot/Batch Number
SLCQ8849
0000267635
SLCQ5706
031M1823V
129K2051

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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
M Manning et al.
Journal of medicinal chemistry, 38(10), 1762-1769 (1995-05-12)
We report the solid-phase synthesis of the D-Cys6 analogues of arginine-vasopressin (AVP), peptide 1, of the selective AVP vasopressor (V1a receptor) antagonist [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid),2-O-methyltyrosine]arginine-vasopressin (d(CH2)5[Tyr(Me)2]-AVP, (A)), peptide 2, of the three nonselective antidiuretic/vasopressor (V2/V1a receptor) AVP antagonists d(CH2)5[Tyr(Et)2]VAVP (B), d(CH2)5[D-Tyr(Et)2]VAVP
Y Tsuboi et al.
Kidney international, 46(1), 237-244 (1994-07-01)
The present study was undertaken to determine whether a non-peptide arginine vasopressin (AVP) antagonist [5-dimethylamino-1-(4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetra hydro-1H- benzazepine] (OPC-31260) improves the impaired water excretion in rats with experimental liver cirrhosis. Male Wistar rats weighing 200 to 250 g were injected in
D Tran et al.
The journal of histochemistry and cytochemistry : official journal of the Histochemistry Society, 47(5), 601-616 (1999-04-28)
In freshly isolated rat hepatocyte multiplets, Ca2+ signals in response to vasopressin are highly organized. In this study we used specific probes to visualize, by fluorescence and confocal microscopy, the main signaling molecules involved in vasopressin-mediated Ca2+ responses. V1a receptors
W Y Chan et al.
Experimental physiology, 85 Spec No, 7S-18S (2000-05-05)
Synthetic oxytocin and vasopressin agonists and antagonists have become important tools for research and were instrumental in the identification of the four known receptor subtypes, V1a, V2, V1b (V3) and oxytocin, of these peptide hormones. However, the relative lack of
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