AL 8810
目录号 : GC16895A potent, selective FP receptor antagonist
Cas No.:246246-19-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
AL-8810 is a novel prostaglandin F2α analog that acts as a selective antagonist of prostaglandin F2α (FP) receptor.
Prostaglandin receptors are a group of g-protein coupled receptor that exhibited a variety of functions in regulation of blood pressure and renal function; smooth muscle contraction; inhibition of plate aggregation; immune response etc.
AL-8810 has a EC50 of 261 ± 44 nM against FP receptor in the A7r5 rat thoracic aorta smooth muscle cells and a EC50 of 186 ± 63 nM in Swiss mouse 3T3 fibroblasts. In addition, AL-8810 antagonizes the response to 100 nM fluprostenol (Ki = 426 ± 63 nM) in a concentration- dependent manner in A7r5 cells. [1]
In the h-TM cells, AL-8810 antagonizes the (±) fluprostenol-induced PI turn over responses concentration dependently (Ki=2.56 ± 0.62 μm). AL-8810 also antagonizes bimatoprost, travoprost acid, latanoprost acid and travoprost acid. [2] In HCM cells, 1 μm AL-8810 blocks the 85% PGF2-induced MMP-2 secretion and 66% PGF2α-induced activation of ERK1/2. [3]
References:
1. Griffin BW, Klimko P, Crider JY, Sharif NA. AL-8810: a novel prostaglandin F2 alpha analog with selective antagonist effects at the prostaglandin F2 alpha (FP) receptor. J Pharmacol Exp Ther. 1999 Sep;290(3):1278-84.
2. Husain S, Jafri F, Crosson CE. Acute effects of PGF2alpha on MMP-2 secretion from human ciliary muscle cells: a PKC- and ERK-dependent process. Invest Ophthalmol Vis Sci. 2005 May;46(5):1706-13.
3. Sharif NA, Kelly CR, Crider JY. Human trabecular meshwork cell responses induced by bimatoprost, travoprost, unoprostone, and other FP prostaglandin receptor agonist analogues. Invest Ophthalmol Vis Sci. 2003 Feb;44(2):715-21.
| Cas No. | 246246-19-5 | SDF | |
| 化学名 | (Z)-7-((1R,2R,3S,5S)-2-((R,E)-3-(2,3-dihydro-1H-inden-2-yl)-3-hydroxyprop-1-en-1-yl)-3-fluoro-5-hydroxycyclopentyl)hept-5-enoic acid | ||
| Canonical SMILES | F[C@H]1C[C@H](O)[C@H](C/C=C\CCCC(O)=O)[C@H]1/C=C/[C@H](O)C2CC3=CC=CC=C3C2 | ||
| 分子式 | C24H31FO4 | 分子量 | 402.50 |
| 溶解度 | 25mg/mL in DMSO, 20mg/mL in DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4845 mL | 12.4224 mL | 24.8447 mL |
| 5 mM | 0.4969 mL | 2.4845 mL | 4.9689 mL |
| 10 mM | 0.2484 mL | 1.2422 mL | 2.4845 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet