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Butaprost

Catalog No. T26925 CAS 69685-22-9

Synonyms: Butaprostum, TR-4979, (R)-Butaprost

Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3].

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Butaprost, CAS 69685-22-9

Pack Size	Availability	Price/USD
500 μg	35 days	$ 215.00
1 mg	35 days	$ 423.00
5 mg	35 days	$ 1,570.00
10 mg	35 days	$ 2,720.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3].
In vitro	Butaprost, at concentrations ranging from 1-100 nM over a period of 0.5-24 hours, significantly enhances Nur77 mRNA expression by approximately five-fold in hEP2-HEK293/EBNA cells, showing both dose- and time-dependency. The augmentation of Nur77 gene expression is mediated via the PKC pathway. Additionally, at a concentration of 50 μM for 24 hours, Butaprost mitigates TGF-β-stimulated fibronectin expression, Smad2 phosphorylation, and the epithelial-mesenchymal transition in Madin-Darby Canine Kidney (MDCK) cells. Western Blot analysis of HEK 293/EBNA cells, which stably express the human EP2 receptor, corroborates the five-fold increase in Nur77 mRNA expression after exposure to Butaprost.
In vivo	Butaprost treatment (1-4 mg/kg; intraperitoneal injection; twice daily; for 7 days) effectively attenuates fibrosis development in male C57BL/6 mice (8 weeks of age; 21 g) subjected to unilateral ureteral obstruction surgery. This outcome is evidenced by the decreased gene and protein expression levels of α-smooth muscle actin, fibronectin, and collagen 1A1, indicating a significant mitigation of fibrosis.

Synonyms	Butaprostum, TR-4979, (R)-Butaprost
Molecular Weight	408.57
Formula	C24H40O5
CAS No.	69685-22-9

Storage

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

References and Literature

1. Nilsson SF, Drecoll E, Lütjen-Drecoll E, Toris CB, Krauss AH, Kharlamb A, Nieves A, Guerra T, Woodward DF. The prostanoid EP2 receptor agonist butaprost increases uveoscleral outflow in the cynomolgus monkey. Invest Ophthalmol Vis Sci. 2006 Sep;47(9):4042-9. PubMed PMID: 16936121. 2. Duckworth N, Marshall K, Clayton JK. An investigation of the effect of the prostaglandin EP2 receptor agonist, butaprost, on the human isolated myometrium from pregnant and non-pregnant women. J Endocrinol. 2002 Feb;172(2):263-9. PubMed PMID: 11834444. 3. Liang Y, Li C, Guzman VM, Chang WW, Evinger AJ, Pablo JV, Woodward DF. 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. Br J Pharmacol. 2004 Jun;142(4):737-48. Epub 2004 May 24. PubMed PMID: 15159280; PubMed Central PMCID: PMC1575044. 4. Osborne NN, Li GY, Ji D, Andrade da Costa BL, Fawcett RJ, Kang KD, Rittenhouse KD. Expression of prostaglandin PGE2 receptors under conditions of aging and stress and the protective effect of the EP2 agonist butaprost on retinal ischemia. Invest Ophthalmol Vis Sci. 2009 Jul;50(7):3238-48. doi: 10.1167/iovs.08-3185. Epub 2009 Mar 5. PubMed PMID: 19264896.

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Keywords

Butaprost 69685-22-9 Butaprostum TR-4979 (R)-Butaprost TR 4979 TR4979 inhibitor inhibit

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