Elabela(19-32) TFA
目录号 : GC60800
Elabela(19-32)TFA是一种有效的apelin受体(APJ)内源性激动剂，Ki值为0.93nM。Elabela(19-32)TFA激活Gαi1和β-arrestin-2信号通路，EC50分别为8.6nM和166nM。Elabela(19-32)TFA诱导受体内在化，降低动脉压，对心脏产生正性肌力作用。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Elabela(19-32) TFA is a potent apelin receptor (APJ) endogenous agonist with a Ki of 0.93 nM. Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart[1][2].
Elabela(19-32) TFA (analogue 3) has an EC50 of 36 nM in HEK293 cells transiently expressing the HA-hAPJ receptor. Elabela(19-32) TFA is slightly less potent than apelin-13 and ELA to elicit receptor internalization[1]. Elabela(19-32) TFA (0.001 to 0.3 nM) has an EC50 of 1.5 pM in inducing changes in left ventricular developed pressure (LVDP) on the Langendorff perfused isolated rat heart[1].
Elabela(19-32) TFA (analogue 3) is rapidly metabolized in rat plasma (t1/2<2 min)[1].
[1]. Peiran Yang, et al. Elabela/Toddler Is an Endogenous Agonist of the Apelin APJ Receptor in the Adult Cardiovascular System, and Exogenous Administration of the Peptide Compensates for the Downregulation of Its Expression in Pulmonary Arterial Hypertension. Circulation. 2017 Mar 21;135(12):1160-1173. [2]. Alexandre Murza, et al. Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA That Modulates Vascular and Cardiac Functions. J Med Chem. 2016 Apr 14;59(7):2962-72.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.5491 mL | 2.7457 mL | 5.4913 mL |
| 5 mM | 0.1098 mL | 0.5491 mL | 1.0983 mL |
| 10 mM | 0.0549 mL | 0.2746 mL | 0.5491 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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