Lysipressin acetate

目录号: GC64811纯度: >98%同义词: 赖氨加压素醋酸盐,Lysine vasopressin acetate; [Lys8]-Vasopressin acetate
Lysipressin acetate是溶压素的醋酸形式。

Lysipressin acetate
Cas No.: 83968-49-4
规格价格库存数量操作
2mg¥140.00现货
1
5mg¥224.00现货
1
10mg¥336.00现货
1
50mg¥840.00现货
1

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产品描述 Description

Lysipressin acetate is the acetate form of Lysipressin. Lysipressin is a nine-amino-acid peptide, which consists of a six-component loop formed by a disulfide bridge, two cysteine residues, and a side chain that includes three amino acid residues. Lysipressin is synthesized in the large cell nuclei of the anterior hypothalamus, stored in the posterior pituitary (neurohypophysis), and secreted into the blood. Depending on the amino acid in the 8th position (lysine or arginine), there are two forms of vasopressin: Lysipressin (lysine vasopressin) or arginine vasopressin [1].

Lysipressin acetate is an arginine vasopressin receptor 1A (V1A) receptor agonist that binds to rat and human V1A receptors (Kis = 1.2 and 10.1 nM, respectively) and Lysipressin acetate increases intracellular calcium levels in cultured rat and human aortic cells with half-maximal activation (Kact) values of 12 and 20.8 nM, respectively. On human cultured VSMCs, LVP and AVP dose-dependently stimulated PLC activity. AVP and LVP both induced dose-dependent and transient increase in [Ca2+]i in rat and human cultured VSMCs [2].

Lysipressin (Lysine vasopressin) is about 1/6 times as potent as Arginine vasopressin in inhibiting water diuresis in dogs when they are injected intravenously in equal vasopressor doses [3]. Lysipressin produce antidiuresis in the pig, without significantly altering glomerular filtration rate [3].

References:
[1]. Grigorjeva M E, Golubeva M G. The Role of Cholinergic Receptors in the Reactions of the Hemostasis System on Vasopressin[J]. Biology Bulletin Reviews, 2022, 12(6): 631-637.
[2]. Colson P H, Virsolvy A, Gaudard P, et al. Terlipressin, a vasoactive prodrug recommended in hepatorenal syndrome, is an agonist of human V1, V2 and V1B receptors: implications for its safety profile[J]. Pharmacological Research, 2016, 113: 257-264.
[3]. MUNSICK R A, SAWYER W H, Van Dyke H B. The antidiuretic potency of arginine and lysine vasopressins in the pig with observations on porcine renal function[J]. Endocrinology, 1958, 63(5): 688-693.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Vascular smooth muscle cells (VSMCs)

Preparation Method

VSMCs were isolated from rat aorta and from human uterine artery. hVSMC cells were pre-incubated 20 min at 37 °C in the presence of LiCl (2.10-2 M) with the protease inhibitor Bestatin (10-5 M) and BSA (0.1%), conditions known to reduce peptide degradation and thus terlipressin conversion into Lysipressin. Cells were further incubated in the same media for 2 or 30 additional min in the presence of terlipressin (10-5 M), Lysipressin (10-6 M) or with vehicle (control).

Reaction Conditions

10-6 M, 2 or 30 min

Applications

In the presence of protease inhibitors (bestatin and BSA) used to prevent terlipressin conversion into Lysipressin, no significant changes were observed for a short incubation-period (2 min) in either terlipressin or Lysipressin IPs accumulation. After a 30 min incubation period, terlipressin-induced accumulation of IPs was reduced in the presence of BSA and bestatin, but not suppressed.

References:

[1]. Colson P H, Virsolvy A, Gaudard P, et al. Terlipressin, a vasoactive prodrug recommended in hepatorenal syndrome, is an agonist of human V1, V2 and V1B receptors: implications for its safety profile[J]. Pharmacological Research, 2016, 113: 257-264.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
83968-49-4
同义词
赖氨加压素醋酸盐,Lysine vasopressin acetate; [Lys8]-Vasopressin acetate
分子式
C48H69N13O14S2
分子量
1116.27 g/mol
溶解性
DMSO : ≥ 100 mg/mL (89.58 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol