RG-12525

Modify Date: 2024-01-14 20:58:19

RG-12525 structure	Common Name	RG-12525
	CAS Number	120128-20-3	Molecular Weight	423.46700
	Density	1.308g/cm3	Boiling Point	667ºC at 760 mmHg
	Molecular Formula	C₂₅H₂₁N₅O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	227.3ºC

Use of RG-12525

RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.

Name	2-[[4-[[2-(2H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]quinoline
Synonym	More Synonyms

Description	RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor Research Areas >> Metabolic Disease
Target	LTD4:2.5 nM (IC50, Guinea pig) LTC4:2.6 nM (IC50, Guinea pig) LTE4:7 nM (IC50, Guinea pig) PPARγ:60 nM (IC50) CYP3A4:0.5 μM (Ki)
In Vitro	RG 12525 competitively inhibits 3H-LTD4 binding to lung membranes (Ki = 3.0 +/- 0.3 nM) and competitively antagonizes the spasmogenic activity of LTC4, LTD4 and LTE4 on lung strips (KB values = 3 nM) with greater than 8000 fold selectivity[1]. RG 12525 (2.5 µM or 25 µM) inhibits the microsomal activity of CYP2C9 and -3A4, but does not significantly inhibit CYP1A2,-2A6, -2C19, or -2D6. RG 12525 (25 µM) also causes a substantial amount of inhibition at the 5 and 10 µM midazolam concentrations[2].
In Vivo	RG 12525 orally inhibits LTD4 induced wheal formation (ED50 = 5 mg/kg with a t1/2 = 10 hrs at 9 mg/kg), LTD4 induces bronchoconstriction (ED50 = 0.6 mg/kg), and anaphylactic death (ED50 = 2.2 mg/kg with a t1/2 = 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED50 = 0.6 mg/kg)[1]. RG 12525 inhibits antigen-induced mortality in the systemic anaphylaxis model with an ED50 (95% confidence interval) = 2.2 (0.8-6.4) mg/kg. RG 12525 also protects against LTD4-induced bronchoconstriction in a model measuring changes in pulmonary function with an ED50 = 0.6 (0.4-1.0) mg/kg[3].
References	[1]. Van Inwegen RG, et al. Antagonism of peptidoleukotrienes and inhibition of systemic anaphylaxis by RG 12525 in guinea pigs. Life Sci. 1989;44(12):799-807. [2]. Fayer JL, et al. Lack of correlation between in vitro inhibition of CYP3A-mediated metabolism by a PPAR-gamma agonist and its effect on the clinical pharmacokinetics of midazolam, an in vivo probe of CYP3A activity. J Clin Pharmacol. 2001 Mar;41(3):305-16. [3]. Carnathan GW, et al. The effect of RG 12525 on leukotriene D4-mediated pulmonary responses in guinea pigs. Agents Actions. 1989 Jun;27(3-4):316-8.

Density	1.308g/cm3
Boiling Point	667ºC at 760 mmHg
Molecular Formula	C₂₅H₂₁N₅O₂
Molecular Weight	423.46700
Flash Point	227.3ºC
Exact Mass	423.17000
PSA	85.81000
LogP	4.49670
Vapour Pressure	1.17E-17mmHg at 25°C
Index of Refraction	1.681
Storage condition	2-8℃

Precursor 6
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DownStream 0