RG-12525

SKU: orb1706723

Description

RG-12525 is a potent, orally active antagonist of cysteinyl leukotriene receptors and an agonist of PPAR-γ, with species-specific utility for asthma research. It demonstrates nanomolar potency in inhibiting ligand-induced contractions in vitro and also modulates CYP3A4 activity.

Research Area

Metabolism Research, Molecular Biology, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	120128-20-3
MW	423.47
Purity	95.49%
Formula	C₂₅H₂₁N₅O₂
SMILES	N1=NNC(=N1)CC=2C=CC=CC2COC3=CC=C(OCC4=NC=5C=CC=CC5C=C4)C=C3
Target	Cytochromes P450,Leukotriene Receptor,PPAR
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.36 mM);DMSO:10 mg/mL (23.61 mM)

Bioactivity

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Target IC50	[3H]-LTD4:3.0nM ( (Ki)\|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 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. 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. Read more...
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. 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. Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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LTE4, LTC4, LTD4, NID 525, NID525, NID-525, LeukotrieneReceptor, leukotriene D (LTD), Leukotriene Receptor, CYP3A4, PPARγ, RG12525, RG-12525, RG 12525

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Compound Identifiers

PubChem CID

129044 ↗

Key Properties

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No computed properties available.

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RG-12525

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

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Protocol Information

RG-12525 (orb1706723)

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