2. GPCR/G Protein
  3. Angiotensin Receptor
  4. A-779 TFA

A-779 TFA 是一种选择性血管紧张素-(1-7) (Ang-(1-7)) 拮抗剂。A-779 TFA 可阻断 Arachidonic acid 释放、缓激肽增强效应和降压作用。A-779 TFA 在未孕大鼠中发挥利尿作用，在妊娠晚期大鼠中发挥抗利尿作用，还可抑制妊娠晚期大鼠的饲料摄入和饮水量。A-779 TFA 可减弱与血管紧张素-(1-7) 相关的前列环素、一氧化氮和血栓素 A2 的调控作用。A-779 TFA 可用于高血压的相关研究。

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Custom Peptide Synthesis

A-779 TFA

A-779 TFA Chemical Structure

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A-779 TFA 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A-779 TFA is a selective angiotensin-(1-7) (Ang-(1-7)) antagonist. A-779 TFA blocks Arachidonic acid release, bradykinin potentiation effects and hypotensive action. A-779 TFA exerts diuretic effects in non-pregnant rats, antidiuretic effects in late-pregnant rats, and also inhibits feed intake and water consumption in late-pregnant rats. A-779 TFA attenuates the regulatory effects of prostacyclin, nitric oxide and thromboxane A2 associated with angiotensin-(1-7). A-779 TFA can be used in studies related to hypertension[1][2][3][4].

体外研究
(In Vitro)

A-779 (10-10 to 10-6 M) 可强效与 125I-Ang-(1-7) TFA 竞争结合转染 Mas 的 CHO 细胞，其 IC50 为 0.3 nM[2]。
A-779 (10-8 M; 10 min pre-incubation prior to 15 min Ang-(1-7) incubation at 37°C) TFA 可阻断 Ang-(1-7) (HY-12403) 在 Mas 转染 CHO、COS 细胞中诱导的 [3H]-Arachidonic acid 释放[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

A-779 TFA 相关抗体:
体内研究
(In Vivo)

A-779 (24 μg/kg/h；静脉注射；持续输注；8 天) TFA 可使未交配雌性 Sprague Dawley 大鼠的尿量显著增加 126%[1]。
A-779 (24 μg/kg/h；静脉注射；持续输注；孕前 8 天至妊娠第 19 天) TFA 可使妊娠晚期的 Sprague Dawley 大鼠饲料消耗量显著降低 83%、尿量减少 76%，使妊娠中期饮水量降低 83%、妊娠晚期饮水量降低 80%，且对胎仔结局无影响[1]。
A-779 (80 ng/min 速率静脉持续输注) TFA 可显著减弱 Captopril (HY-B0368) 对清醒雄性 Wistar 大鼠体内缓激肽降压作用的增强效应[3]。
A-779 (48 µg/kg；静脉注射；单次给药；100 pM；与分离的主动脉环共同孵育) TFA 可部分阻断高盐诱导的高血压雄性 Dahl 盐敏感性大鼠中 Ang-(1-7) 引发的降压反应，并能抑制 Ang-(1-7) 介导的血管舒张/血管收缩类前列腺素、一氧化氮及 cGMP 水平的所有相关变化[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley (female, 9 weeks old)[1]
Dosage: 24 μg/kg/h
Administration: i.v.; continuous infusion; 8 days
Result: Increased urine volume by 126%.
Tended to decrease urinary osmolality.
Did not alter chow consumption and water intake relative to vehicle controls.
Animal Model: Sprague Dawley (female, originally 9 weeks old virgin, pregnant)[1]
Dosage: 24 μg/kg/h
Administration: i.v.; continuous infusion; 8 days pre-pregnancy through gestational day 19
Result: Decreased water consumption by 83% relative to vehicle controls in mid-pregnancy (gestational day 15).
Decreased chow consumption by 83%, decreased water consumption by 80%, and reduced urine volume by 76% relative to vehicle controls in late pregnancy (gestational day 19).
Tended to increase urinary osmolality in late pregnancy.
Had no significant effect on fluid/food intake-output balance, urinary sodium or potassium concentrations, maternal body weight, or fetal characteristics (body weight, length, number).
Animal Model: Wistar (male, 230-320 g)[3]
Dosage: 80 ng/min
Administration: i.v.; continuous infusion
Result: Produced a significant shift of the intravenous bradykinin dose-response curve, requiring approximately two-fold higher bradykinin doses to achieve the same hypotensive effect observed with captopril alone.
Significantly attenuated the captopril-induced potentiation of intra-arterial bradykinin's hypotensive effect.
Did not significantly alter bradykinin's hypotensive effect or baseline MAP when infused alone (without captopril).
Did not modify the pressor effect of angiotensin II.
Did not change captopril's inhibitory effect on angiotensin I's pressor response.
Did not alter the captopril-induced decrease in baseline MAP.
Animal Model: Dahl salt-sensitive (male, 4-5 weeks of age, high 8.0% NaCl salt diet for 2 weeks or low 0.3% NaCl salt diet)[4]
Dosage: 48 µg/kg (in vivo); 100 pmol (ex vivo tissue incubation)
Administration: i.v.; single dose (in vivo); incubated with isolated aortic rings (ex vivo)
Result: Blocked the maximal MAP reduction of -14 mm Hg induced by Ang-(1-7) in high salt diet rats, resulting in a significantly attenuated blood pressure decrease.
Prevented the Ang-(1-7)-induced increase in plasma 6-keto-PGF1α levels, maintaining levels near basal values.
Prevented the Ang-(1-7)-induced decrease in plasma TXB2 levels, maintaining levels near basal values.
Prevented the Ang-(1-7)-induced increase in plasma nitric oxide levels, maintaining levels near basal values.
Prevented the Ang-(1-7)-induced increase in aortic ring 6-keto-PGF1α levels (from 31 to 49 pg/mL/mg ring wt, maintained at 36 pg/mL/mg ring wt) and PGE2 levels (from basal 22 to Ang-(1-7)-induced 33 pg/mL/mg ring wt, maintained at 21 pg/mL/mg ring wt) in high salt diet rats.
Attenuated the Ang-(1-7)-induced decrease in aortic ring TXB2 levels (from basal 44 to Ang-(1-7)-induced 23 pg/mL/mg ring wt, increased to 37 pg/mL/mg ring wt) in high salt diet rats.
Prevented the Ang-(1-7)-induced increase in nitric oxide levels in aortic rings from both high and low salt diet rats.
Totally abolished the Ang-(1-7)-induced 52% increase in aortic ring cGMP levels (from basal 102 to Ang-(1-7)-induced 212 fmol/mg protein, maintained at 67 fmol/mg protein) in high salt diet rats.
Had no significant effect on MAP, plasma 6-keto-PGF1α, TXB2, nitric oxide, aortic ring 6-keto-PGF1α, PGE2, TXB2, nitric oxide, or cGMP levels compared to basal values in either diet group.
分子量

986.99

Formula

C41H61F3N12O13
Sequence

Asp-Arg-Val-Tyr-Ile-His-{d-Ala}
Sequence Shortening

DRVYIH-{d-Ala}
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

A-779 TFA 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-779A779A 779Angiotensin ReceptorMas-transfected CHO cellsWistar ratsarachidonic acidSprague Dawley ratsangiotensin-(1-7)bradykininvirgin ratsMas-transfected COS cellslate-gestation ratsMas protooncogene G protein-coupled receptorInhibitorinhibitorinhibit

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