Iloprost
Iloprost is a second generation synthetic analog of prostacyclin derived from carbacyclin, exhibiting approximately 10-fold greater potency than the first generation stable analogs of prostacyclin, represented by carbacyclin. Iloprost binds with high affinity to the prostanoid receptors, with Ki values being 11, 11 and 56 nM for the human recombinant IP, EP1 and EP3 receptors, respectively. Prostacyclin is a prostaglandin member of the eicosanoid family of lipid molecules, which inhibits platelet activation and dilates blood vessels through interaction with G-protein-coupled prostanoid receptors.
References:
1. Schrör K, Darius H, Matzky R, et al. The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK 36 374)--equipotent to PGI2 in vitro. Naunyn-Schmiedeberg's Archives of Pharmacology, 1981, 316(3): 252-255.
2. Abramovitz M, Adam M, Boie Y, et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochimica et Biophysica Acta, 2000, 1483(2): 285-293.
| Physical Appearance | A solution in methyl acetate |
| Storage | Desiccate at -20°C |
| M.Wt | 360.49 |
| Cas No. | 78919-13-8 |
| Formula | C22H32O4 |
| Solubility | Soluble in methyl acetate |
| Chemical Name | (E)-5-((3aS,4R,5R,6aS)-5-hydroxy-4-((3S,4R,E)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)hexahydropentalen-2(1H)-ylidene)pentanoic acid |
| SDF | Download SDF |
| Canonical SMILES | O[C@H]1[C@H](/C=C/[C@H]([C@H](C)CC#CC)O)[C@@H](C/C2=C/CCCC(O)=O)[C@@H](C2)C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Human whole blood |
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Reaction Conditions |
13 nM iloprost |
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Applications |
Iloprost inhibited ADP, thrombin and collagen-induced aggregation of human platelets, with an ED50 value of about 13 nM. Iloprost was equipotent to PGI2 which showed a similar IC50 value of 11 nM in this system. |
| Animal experiment:[1] | |
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Animal models |
Cats subjected to acute myocardial ischemia by ligation of the left anterior descending coronary artery |
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Dosage form |
0.18 ~ 1.79 μg/kg x min Intravenous infusion, started 30 min after ligation and maintained for 4.5 h |
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Applications |
Iloprost did not influence the arterial blood pressure during continuous infusion for 4.5 h up to doses of 1.19 μg/kg x min. Only at 1.79 μg/kg x min there was a significant fall in blood pressure. In contrast, the decrease in peripheral platelet count induced by ligation of the coronary artery was already abolished at a dose of 0.18 μg/kg x min. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Schrör K, Darius H, Matzky R, et al. The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK 36 374)--equipotent to PGI2 in vitro. Naunyn-Schmiedeberg's Archives of Pharmacology, 1981, 316(3): 252-255. 2. Abramovitz M, Adam M, Boie Y, et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochimica et Biophysica Acta, 2000, 1483(2): 285-293. |
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Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
