| Identification | Back Directory | [Name]
RG 12525 | [CAS]
120128-20-3 | [Synonyms]
NID 525
RG 12525
2-[4-[2-(1H-Tetrazol-5-ylmethyl)benzyloxy]phenoxymethyl]quinoline
Quinoline, 2-[[4-[[2-(2H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]- | [Molecular Formula]
C25H21N5O2 | [MDL Number]
MFCD00877828 | [MOL File]
120128-20-3.mol | [Molecular Weight]
423.47 |
| Chemical Properties | Back Directory | [Boiling point ]
667.0±65.0 °C(Predicted) | [density ]
1.308±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
4.72±0.10(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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. | [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]. | [storage]
Store at -20°C | [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. DOI:10.1016/0024-3205(89)90377-9
[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 DOI:10.1177/00912700122010122
[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. DOI:10.1007/BF01972809 |
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