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RG-12525

Catalog No. T16739 CAS 120128-20-3

Synonyms: NID 525

RG-12525（NID 525） is an orally available, selective and competitive leukotriene D (LTD) antagonist that inhibits LTC4, LTD4 and LTE4-induced contraction of guinea pig thin-walled bands, with IC50 values of 2.6 nM, 2.5 nM, and 7 nM, respectively.RG-12525 inhibits CYP3A4, with a Ki value of 0.5 µM. RG-12525 is a novel and potent PPAR-γ agonist (IC50 value of about 60 nM) with species specificity for the study of asthma.

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RG-12525, CAS 120128-20-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 169.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 478.00
25 mg	5 days	$ 913.00
50 mg	6-8 weeks	$ 1,390.00
1 mL * 10 mM (in DMSO)	In stock	$ 318.00

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Purity: 96.77%

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Description	RG-12525（NID 525） is an orally available, selective and competitive leukotriene D (LTD) antagonist that inhibits LTC4, LTD4 and LTE4-induced contraction of guinea pig thin-walled bands, with IC50 values of 2.6 nM, 2.5 nM, and 7 nM, respectively.RG-12525 inhibits CYP3A4, with a Ki value of 0.5 µM. RG-12525 is a novel and potent PPAR-γ agonist (IC50 value of about 60 nM) with species specificity for the study of asthma.
Targets&IC50	PPARγ:60 nM, LTE4:7 nM (Guinea pig), LTD4:2.5 nM (Guinea pig), 3H-LTD4:3.0nM ( (Ki), LTC4:2.6 nM (Guinea pig), CYP3A4:0.5 μM (Ki)
In vitro	RG-12525 competitively inhibits 3H-LTD4 binding to lung membranes (Ki = 3.0 +/- 0.3 nM) and antagonizes the spasmogenic activity of LTC4, LTD4, and LTE4 on lung strips in a competitive manner (KB values = 3 nM), displaying 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. Additionally, at 25 µM concentration, RG-12525 causes substantial inhibition at the 5 and 10 µM midazolam concentrations[3].
In vivo	Orally, RG-12525 inhibits LTD4-induced wheal formation with an ED50 of 5 mg/kg and a half-life (t1/2) of 10 hours at 9 mg/kg. It also inhibits LTD4-induced bronchoconstriction with an ED50 of 0.6 mg/kg and anaphylactic death with an ED50 of 2.2 mg/kg and a half-life (t1/2) of 7 hours at 10 mg/kg. Additionally, RG-12525 inhibits antigen-induced bronchoconstriction with an ED50 of 0.6 mg/kg[1]. In the systemic anaphylaxis model, RG-12525 inhibits antigen-induced mortality with an ED50 (95% confidence interval) of 2.2 (0.8-6.4) mg/kg. Furthermore, RG-12525 protects against LTD4-induced bronchoconstriction in a model measuring changes in pulmonary function, with an ED50 of 0.6 (0.4-1.0) mg/kg[2].

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

Storage

store at low temperature

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

Solubility Information

DMSO: 10 mg/mL (23.61 mM), Sonication is recommended.

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. 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. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library

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Keywords

RG-12525 120128-20-3 DNA Damage/DNA Repair GPCR/G Protein Metabolism Leukotriene Receptor PPAR RG12525 NID-525 NID 525 NID525 RG 12525 inhibitor inhibit

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