產品描述: A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII. |
靶點:
Angiotensin Receptor;RAAS |
體內研究:
Infusion of Ang(1-7) and A-779 (400?ng/kg/min, s.c.) alone or combined for 6 weeks does not prevent uterus atrophy or inhibit the body weight gain of OVX rats. A-779 markedly elevates serum bone specific alkaline phosphatase (BALP), telopeptides of collagen type I (CTX), tartarate resistant acid phosphatase (TRAcP 5b), osteocalcin (OC) and urinary deoxypyridinoline (DPD). Infusion of Ang(1-7) and/or A-779 does not significantly change serum minerals concentrations in sham or OVX groups. A-779 in the OVX animals does not change AngII, Ang(1-7), AT1R, AT2R, ACE, ACE-2, Mas receptor, RANKL and OPG proteins expressions in relation to OVX group, while AngII (P?0.05), AT1R (P?0.05), ACE (P?0.01) and RANKL (P?0.01) expressions are significantly higher and Ang(1-7), AT2R, ACE-2, MasR and OPG are significantly (P?0.01) lower than sham group. Blocking of the G-protein coupled receptor (Mas) by A-779 markedly abolishes Ang(1-7) favorable effects on bone health suggesting the vital role of Mas receptor in mediating Ang(1-7) osteo-protective effects. Inhibition of Ang1-7 cascade by A-779 (400?ng/kg/min) significantly eradicates captopril protective effects on bone metabolism, mineralization and micro-structure. A-779 also restores OVX effects on RANKL expression and ACE-1/AngII/AT1R cascade and down-regulates OPG expression and ACE-2/Ang1-7/Mas pathway |
參考文獻:
1. Abuohashish HM, et al. Angiotensin (1-7) ameliorates the structural and biochemical alterations of ovariectomy-induced osteoporosis in rats via activation of ACE-2/Mas receptor axis. Sci Rep. 2017 May 23;7(1):2293. 2. Abuohashish HM, et al. ACE-2/Ang1-7/Mas cascade mediates ACE inhibitor, captopril, protective effects in estrogen-deficient osteoporotic rats. Biomed Pharmacother. 2017 Aug;92:58-68. 3. Yan WF, et al. Effects and related mechanism of angiotensin-(1-7) on Toll-like receptor 4-mediated oxidative stress in human umbilical vein endothelial cells. Zhonghua Xin Xue Guan Bing Za Zhi. 2017 Mar 24;45(3):223-229. |
溶解性:
0.1 M HCL : 25 mg/mL (28.64 mM; ultrasonic and adjust pH to 1 with HCl) H2O : 5 mg/mL (5.73 mM; Need ultrasonic) |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
1.146 ml |
5.728 ml |
11.455 ml |
5 mM |
0.229 ml |
1.146 ml |
2.291 ml |
10 mM |
0.115 ml |
0.573 ml |
1.146 ml |
50 mM |
0.023 ml |
0.115 ml |
0.229 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |