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  1. GPCR/G Protein
  2. Angiotensin Receptor
  3. A 779

A 779 是G蛋白偶聯(lián)受體Mas的有效拮抗劑,Mas受體為一種Ang1-7 receptor,區(qū)別于傳統(tǒng)的AngII。

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Custom Peptide Synthesis

A 779 Chemical Structure

A 779 Chemical Structure

CAS No. : 159432-28-7

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查看 Angiotensin Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.

IC50 & Target

AT2 Receptor

 

AT1 Receptor

 

體外研究
(In Vitro)

A-779 inhibits the effect of Ang-(1-7), which suppresses the proliferating cell nuclear antigen (PCNA) protein expression up-regulated by Ang II, but A-779 alone has no effect to induce proliferation and migration of VSMCs. Pretreatment with Ang-(1-7) significantly retards Ang II-induced inflammatory responses of VSMCs associated with up-regulated MCP-1, VCAM-1 and IL-1β expressions, and this effect of Ang-(1-7) is blocked by A-779. But A-779 alone has no effect to induce inflammatory response of VSMCs. Pretreatment VSMCs with Ang-(1-7) for 5 min significantly inhibits Akt and ERK1/2 phosphorylation induced by Ang II, and this effect is also blocked by A-779, but alone has no effect to induce phosphorylation of Akt and ERK1/2 in VSMCs[3].

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

體內(nèi)研究
(In Vivo)

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[1]. 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[2].

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

分子量

872.97

Formula

C39H60N12O11

CAS 號
性狀

固體

顏色

White to off-white

Sequence

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

Sequence Shortening

DRVYIH-{d-Ala}

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 18.18 mg/mL (20.83 mM; adjust pH to 2 with 1 M HCL; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.1455 mL 5.7276 mL 11.4551 mL
5 mM 0.2291 mL 1.1455 mL 2.2910 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.67%

參考文獻
Animal Administration
[1]

A bilateral OVX operation is use to induce postmenopausal osteoporosis in female Wistar albino rats. The animals are generally anesthetized using single IP injection of ketamine?+?xylazine combination (80?mg/kg and 5?mg/kg; respectively). After ligation, the ovaries are excised from a longitudinal incision made on the dorsolateral body region. Sham rats have the same procedure without the ligation and excision. The risk of postoperative infection is eliminated by applying fusidic acid topical antibiotic cream twice weekly for 4 weeks. Following the sham and OVX operations, animals are divided into eight groups (n?=?8/group) including, Sham, Sham?+?Ang(1-7), Sham?+?A-779, Sham?+?Ang(1-7)+A-779, OVX, OVX?+?Ang(1-7), OVX?+?A-779 and OVX?+?Ang(1-7)+A-779. Eight weeks following sham and OVX operations, osmotic pumps are implanted subcutaneously to deliver Ang(1-7) (200?ng/kg/min), A-779 (400?ng/kg/min) or a mixture of Ang(1-7) and A-779 (200?ng/kg/min and 400?ng/kg/min; respectively) for 6 consecutive weeks. Body weights of all animals are monitored and recorded at the beginning and every week throughout the study. Animals' general health is maintained during periods of treatments. At the end of treatments periods, animals are placed fasting in metabolic cages for 16?hr and urine samples are collected and frozen at ?70°C. Then, the blood samples are collected by cardiac puncture under ketamine?+?xylazine anesthesia and serum samples are obtain by centrifugation at 4000 RPM to. Animals are then sacrificed by decapitation and the uterine tissues and femoral bones are removed and cleaned. Uterine tissues are cleaned from fats and the wet weights are determined directly and expressed as g/100?g body weight. In each rat, both femurs are removed and cleaned from soft tissues. The left femoral bone samples are frozen at ?70°C until analyzed, while the right femoral bones are kept in 10% formalin for mico-CT and minerals analysis.

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

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1455 mL 5.7276 mL 11.4551 mL 28.6379 mL
5 mM 0.2291 mL 1.1455 mL 2.2910 mL 5.7276 mL
10 mM 0.1146 mL 0.5728 mL 1.1455 mL 2.8638 mL
15 mM 0.0764 mL 0.3818 mL 0.7637 mL 1.9092 mL
20 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4319 mL
Help & FAQs
  • 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.

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產(chǎn)品名稱:
A 779
目錄號:
HY-P0216
需求量: