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SC 51089 

Cat. No. M28496
SC 51089  Structure
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Biological Activity

SC 51089 is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 exhibits neuroprotective activity.

Chemical Information
Molecular Weight 459.33
Formula C22H20Cl2N4O3
CAS Number 146033-02-5
Solubility (25°C) DMSO 100 mg/mL (ultrasonic and warming and heat to 60°C)
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alexander V Glushakov, et al. PLoS One. Role of the prostaglandin E2 EP1 receptor in traumatic brain injury

[2] Xianwu Li, et al. J Neuroimmune Pharmacol. Antagonism of neuronal prostaglandin E(2) receptor subtype 1 mitigates amyloid β neurotoxicity in vitro

[3] E A Hallinan, et al. Bioorg Med Chem. 2,4-Disubstituted oxazoles and thiazoles as latent pharmacophores for diacylhydrazine of SC-51089, a potent PGE2 antagonist

[4] E A Hallinan, et al. J Med Chem. Aminoacetyl moiety as a potential surrogate for diacylhydrazine group of SC-51089, a potent PGE2 antagonist, and its analogs

[5] K Lee, et al. Xenobiotica. Comparative metabolism of SC-42867 and SC-51089, two PGE2 antagonists, in rat and human hepatocyte cultures

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  Catalog
Abmole Inhibitor Catalog




Keywords: SC 51089  supplier, Prostaglandin Receptor, inhibitors, activators


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