AH 23848 (calcium salt)
目录号 : GC17224Dual antagonist of TP and EP4 receptors
Cas No.:81496-19-7
Sample solution is provided at 25 µL, 10mM.
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AH 23848 (calcium salt) is a dual antagonist of TP1 and EP4 receptors [1][2].
The thromboxane receptor (TP), also known as the prostanoid TP receptor, is activated by thromboxane A2 (TXA2). TXA2 is an exceptionally potent inducer of platelet aggregation and of contraction of vascular and respiratory smooth muscle [1]. Prostaglandin E2 (PGE2) subtype receptors (EP) are involved in cellular proliferation and tumor development. Prostaglandin E2 (PGE2) activates four EP receptors, EP1-4. The EP4 receptor is coupled to Gs and mediates increases in cAMP concentration by activation of adenylyl cyclase [4].
AH 23848 (calcium salt) is a dual antagonist of TP1 and EP4 receptors. AH 23848 is an orally active, potent and specific thromboxane receptor-blocking drug that has a long duration of action. AH 23848 inhibited TXA2-induced platelet aggregation and antagonized the contraction of human bronchial smooth muscle induced by the TP agonist U-46619 with pA2 of 8.3 [1][3]. In 3T6 fibroblasts, AH-23848B induced accumulation of cells in early S phase and lowered cyclin A levels [4].
In syngeneic BALB/cByJ female mice injected with line 66.1 or 410.4 tumor cells, AH23848 inhibited the metastasis of line 66.1 and 410.4 cells [5].
References:
[1]. Brittain RT, Boutal L, Carter MC, et al. AH23848: a thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A2. Circulation. 1985 Dec;72(6):1208-18.
[2]. Coleman RA, Grix SP, Head SA, et al. A novel inhibitory prostanoid receptor in piglet saphenous vein. Prostaglandins. 1994 Feb;47(2):151-68.
[3]. Coleman RA, Sheldrick RL. Prostanoid-induced contraction of human bronchial smooth muscle is mediated by TP-receptors. Br J Pharmacol. 1989 Mar;96(3):688-92.
[4]. Sanchez, T., and Moreno, J.J. Role of EP1 and EP4 PGE2 subtype receptors in serum-induced 3T6 fibroblast cycle progression and proliferation. American Journal of Physiology.Cell Physiology 282, C280-C288 (2002).
[5]. Ma X, Kundu N, Rifat S, et al. Prostaglandin E receptor EP4 antagonism inhibits breast cancer metastasis. Cancer Res. 2006 Mar 15;66(6):2923-7.
| Cas No. | 81496-19-7 | SDF | |
| 化学名 | (4Z)-rel-7-[(1R,2R,5S)-5-([1,1'-biphenyl]-4-ylmethoxy)-2-(4-morpholinyl)-3-oxocyclopentyl]-4-heptenoic acid, hemicalcium salt | ||
| Canonical SMILES | O=C1C[C@H](OCC2=CC=C(C3=CC=CC=C3)C=C2)[C@H](CC/C=C\CCC([O-])=O)[C@H]1N4CCOCC4.O=C5C[C@H](OCC6=CC=C(C7=CC=CC=C7)C=C6)[C@H](CC/C=C\CCC([O-])=O)[C@H]5N8CCOCC8.[Ca+2] | ||
| 分子式 | C29H34NO5 • 1/2Ca | 分子量 | 496.6 |
| 溶解度 | ≤5mg/ml in DMSO | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0137 mL | 10.0685 mL | 20.1369 mL |
| 5 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL |
| 10 mM | 0.2014 mL | 1.0068 mL | 2.0137 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