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Butaprost

Cat. No. M10803
Butaprost Structure
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1mg USD 480  USD480 1-2 Weeks
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Biological Activity

Butaprost is a selective prostaglandin E receptor (EP2) agonist for murine EP2 receptors EC50 The value is 33 nM,Ki The value is 2.4 μM. Butaprost is less active against rodents EP1, EP3 and EP4 receptors. Butaprost mitigates fibrosis by obstructing TGF-β/Smad2 signaling.

Chemical Information
Molecular Weight 408.57
Formula C24H40O5
CAS Number 69685-22-9
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Jong Hoon Shin, et al. Int J Ophthalmol. Anti-scarring effects of butaprost on human subconjunctival Tenon's fibroblasts

[2] Neville N Osborne, et al. Invest Ophthalmol Vis Sci. Expression of prostaglandin PGE2 receptors under conditions of aging and stress and the protective effect of the EP2 agonist butaprost on retinal ischemia

[3] Siv F E Nilsson, et al. Invest Ophthalmol Vis Sci. The prostanoid EP2 receptor agonist butaprost increases uveoscleral outflow in the cynomolgus monkey

[4] Yanbin Liang, et al. Br J Pharmacol. Upregulation of orphan nuclear receptor Nur77 following PGF(2alpha), Bimatoprost, and Butaprost treatments. Essential role of a protein kinase C pathway involved in EP(2) receptor activated Nur77 gene transcription

[5] N Duckworth, et al. J Endocrinol. An investigation of the effect of the prostaglandin EP2 receptor agonist, butaprost, on the human isolated myometrium from pregnant and non-pregnant women

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