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RG-12525

Catalog No. T16739 CAS 120128-20-3

Synonyms: NID 525

RG-12525 is a PPAR-gamma agonist (IC50: appr 60 nM) and a potent inhibitor of CYP3A4 (Ki: 0.5 μM). RG-12525 is a specific and competitive antagonist of the peptidoleukotrienes, LTC4, LTD4, and LTE4, inhibiting LTC4-, LTD4- and LTE4-induced guinea pig parenchymal strips contractions (IC50s: 2.6 nM, 2.5 nM, and 7 nM, respectively).

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RG-12525, CAS 120128-20-3

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Purity: 98%

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Description	RG-12525 is a PPAR-gamma agonist (IC50: appr 60 nM) and a potent inhibitor of CYP3A4 (Ki: 0.5 μM). RG-12525 is a specific and competitive antagonist of the peptidoleukotrienes, LTC4, LTD4, and LTE4, inhibiting LTC4-, LTD4- and LTE4-induced guinea pig parenchymal strips contractions (IC50s: 2.6 nM, 2.5 nM, and 7 nM, respectively).
Targets&IC50	CYP3A4:0.5 μM (ki), LTC4:2.6 nM(Guinea pig), PPARγ:60 nM, LTD4:2.5 nM(Guinea pig), LTE4:7 nM(Guinea pig)
In vitro	RG 12525 competitively suppresses 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. RG 12525 (25 μM) induces a substantial amount of inhibition at the 5 and 10 μM midazolam concentrations. RG 12525 (2.5 μM or 25 μM) suppresses the microsomal activity of CYP2C9 and -3A4, but does not significantly inhibit CYP1A2,-2A6, -2C19, or -2D6 [1][2].
In vivo	RG 12525 inhibits antigen-induced mortality in the systemic anaphylaxis model (ED50 (95% confidence interval) = 2.2 (0.8-6.4) mg/kg). RG 12525 inhibits LTD4 induced wheal formation (ED50 = 5 mg/kg and 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 and a t1/2 = 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED50 = 0.6 mg/kg). RG 12525 also protects against LTD4-induced bronchoconstriction in a model measuring changes in pulmonary function (ED50 = 0.6 (0.4-1.0) mg/kg)[1][3].

Synonyms	NID 525
Molecular Weight	423.47
Formula	C25H21N5O2
CAS No.	120128-20-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RG-12525 120128-20-3 DNA Damage/DNA Repair Metabolism P450 PPAR RG 12525 NID 525 RG12525 Inhibitor inhibitor inhibit

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