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Octimibate

Catalog No. T24567 CAS 89838-96-0

Synonyms: Octimibato

Octimibate (Octimibato) is a non-prostaglandin platelet aggregation inhibitor and cyclic prostaglandin agonist.Octimibate is used in the treatment of cardiovascular disease and can be used to study atherosclerosis and thrombosis.

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Octimibate, CAS 89838-96-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 143.00
5 mg	In stock	$ 360.00
10 mg	In stock	$ 530.00
25 mg	In stock	$ 859.00
50 mg	In stock	$ 1,180.00
100 mg	In stock	$ 1,590.00
500 mg	In stock	$ 3,190.00

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Purity: 99.49%

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Description

In vitro

In suspensions of washed (plasma-free) human platelets, octimibate is a potent inhibitor of aggregation; its IC50 is approx 10 nM for inhibition of aggregation is stimulated by several different agonists, including U46619 and ADP. The inhibitory effects of octimibate on aggregation are not competitive with the stimulatory agonist; the maximal response is suppressed but there is no obvious shift in potency of the agonist. In platelet-rich plasma, octimibate inhibits agonist-stimulated aggregation with an IC50 of approx 200 nM.[2]
Octimibate increases cyclic AMP concentrations in platelets and increases the cyclic AMP-dependent protein kinase activity ratio. Octimibate stimulates adenylyl cyclase activity in human platelet membranes, with an EC50 of 200 nM. The maximal achievable activation of adenylyl cyclase by intimidate is 60% of that obtainable with iloprost. Octimibate has no effect on the cyclic GMP-inhibited phosphodiesterase (phosphodiesterase-ITI), which is the major cyclic AMP-degrading enzyme in human platelets.[2]

Synonyms	Octimibato
Molecular Weight	454.56
Formula	C29H30N2O3
CAS No.	89838-96-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Merritt JE, et al. Primate vascular responses to octimibate, a non-prostanoid agonist at the prostacyclin receptor. Br J Pharmacol. 1991;102(1):260-266. 2. Merritt JE, et al. Octimibate, a potent non-prostanoid inhibitor of platelet aggregation, acts via the prostacyclin receptor. Br J Pharmacol. 1991;102(1):251-259. 3. Seiler S, et al. Octimibate inhibition of platelet aggregation: stimulation of adenylate cyclase through prostacyclin receptor activation. J Pharmacol Exp Ther. 1990;255(3):1021-1026. 4. Kowala MC, et al. Prostacyclin agonists reduce early atherosclerosis in hyperlipidemic hamsters. Octimibate and BMY 42393 suppress monocyte chemotaxis, macrophage cholesteryl ester accumulation, scavenger receptor activity, and tumor necrosis factor production. Arterioscler Thromb. 1993;13(3):435-44

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Membrane Protein-targeted Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Octimibate 89838-96-0 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor Octimibato inhibitor inhibit

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