| 规格 | 价格 | 库存 | 数量 |
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| 10mg |
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| 25mg |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| 靶点 |
Acts as a less effective agonist at the AT₁ receptor compared to Angiotensin II (AII) or Angiotensin III (AIII). The study found no evidence for interaction with a novel, losartan-insensitive receptor as previously suggested. [1]
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| 体内研究 (In Vivo) |
麻醉下的大鼠在暴露于人血管紧张素 II 时表现出内皮依赖性肾皮质血管舒张 (3-8)。在剂量为 1.25 和 12.5 nmol/kg 时,人血管紧张素 II (3-8) 会导致肾功能损害和平均动脉血压呈剂量依赖性升高,但在剂量高达 125 pmol/kg 时不会对心血管产生影响。血流量和血管电导率因肠系膜血压而降低[1]。
在清醒的Long Evans大鼠中,静脉推注Angiotensin II (3-8), human可引起剂量依赖性平均动脉血压升高。[1] 这种升压效应伴随着肾脏和肠系膜血流量及血管传导性的剂量依赖性降低。在肾脏血管床中,剂量效应关系尤为陡峭。[1] Angiotensin II (3-8), human的心血管效应可被AT₁受体拮抗剂氯沙坦完全阻断。[1] L-精氨酸预处理未能一致性地改变Angiotensin II (3-8), human的血流动力学反应。[1] Angiotensin II (3-8), human的升压和血管收缩效应模式与AII和AIII相似,但其效力大约低100倍,且作用持续时间显著缩短。[1] |
| 动物实验 |
Surgical Preparation: Male Long Evans rats (350-450 g) were anesthetized. Pulsed Doppler flow probes were implanted around the left renal artery, superior mesenteric artery, and distal abdominal aorta to measure regional blood flow. After a 7-14 day recovery, catheters were implanted in the distal abdominal aorta (for blood pressure measurement) and the right jugular vein (for drug administration). [1]
Drug Administration and Hemodynamic Measurement: On experimental days, conscious, freely moving rats received intravenous bolus injections of Angiotensin II (3-8), human (dissolved in sterile isotonic saline containing 1% bovine serum albumin) at doses of 0.125, 1.25, and 12.5 nmol/kg (in a volume of 100 μL, flushed with 100 μL saline). Injections were separated by at least 20 minutes. Continuous recordings of heart rate, mean arterial blood pressure, and regional Doppler shift signals (converted to flow and vascular conductance) were made. Data were analyzed over specific time periods following administration. [1] Pharmacological Intervention Studies: In separate experiments, responses to Angiotensin II (3-8), human (12.5 nmol/kg) were assessed before and 5 minutes after an intravenous bolus of losartan (20 μmol/kg). In another set, responses were assessed before and 5 minutes after the start of a primed infusion of L-arginine (1.4 mmol/kg bolus followed by 1.4 mmol/kg/h infusion). [1] |
| 参考文献 | |
| 其他信息 |
Angiotensin IV is an organic molecular entity.
Angiotensin II (3-8), human (H2N-Val-Tyr-Ile-His-Pro-Phe-OH), also known as Angiotensin IV, is a degradation product of Angiotensin II. [1] This study in conscious rats found no evidence for the vasodilator effect of Angiotensin II (3-8), human in renal or mesenteric vascular beds as reported by others in anesthetized models. Instead, it elicited AT₁ receptor-mediated vasoconstriction. [1] The results suggest that Angiotensin II (3-8), human acts as a weak, short-acting agonist at the AT₁ receptor, providing no functional support for the existence of a unique, losartan-insensitive "Angiotensin IV" receptor under these experimental conditions. [1] |
| 分子式 |
C40H54N8O8
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|---|---|
| 分子量 |
774.90556
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| 精确质量 |
774.406
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| CAS号 |
12676-15-2
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| 相关CAS号 |
Angiotensin II (3-8), human TFA
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| PubChem CID |
123814
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| 外观&性状 |
Typically exists as solid at room temperature
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| LogP |
3.389
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| tPSA |
248.94
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| 氢键供体(HBD)数目 |
8
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| 氢键受体(HBA)数目 |
10
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| 可旋转键数目(RBC) |
19
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| 重原子数目 |
56
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| 分子复杂度/Complexity |
1340
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| 定义原子立体中心数目 |
7
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| SMILES |
CC[C@@H]([C@@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@@H](CC1C=CC=CC=1)C(=O)O)=O)=O)CC1=CNC=N1)=O)NC([C@H](CC1C=CC(O)=CC=1)NC([C@H](C(C)C)N)=O)=O)C
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| InChi Key |
QSBGWDDCOJYQGY-KOQODJNWSA-N
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| InChi Code |
InChI=1S/C40H54N8O8/c1-5-24(4)34(47-35(50)29(44-37(52)33(41)23(2)3)18-26-13-15-28(49)16-14-26)38(53)45-30(20-27-21-42-22-43-27)39(54)48-17-9-12-32(48)36(51)46-31(40(55)56)19-25-10-7-6-8-11-25/h6-8,10-11,13-16,21-24,29-34,49H,5,9,12,17-20,41H2,1-4H3,(H,42,43)(H,44,52)(H,45,53)(H,46,51)(H,47,50)(H,55,56)/t24-,29-,30-,31-,32-,33-,34-/m0/s1
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| 化学名 |
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。 注射用配方 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2905 mL | 6.4524 mL | 12.9047 mL | |
| 5 mM | 0.2581 mL | 1.2905 mL | 2.5809 mL | |
| 10 mM | 0.1290 mL | 0.6452 mL | 1.2905 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。