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RG-12525

Name: RG-12525
Brand: TargetMol
SKU: T16739
Price: 116 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16739Cas No. 120128-20-3

Alias 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.

RG-12525

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Purity: 95.49%

Catalog No. T16739Alias NID 525Cas No. 120128-20-3

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$116	-	In Stock
5 mg	$289	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:95.49%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

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	LTC4:2.6 nM (Guinea pig), CYP3A4:0.5 μM (Ki), LTD4:2.5 nM (Guinea pig), PPARγ:60 nM, LTE4:7 nM (Guinea pig), [3H]-LTD4:3.0nM ( (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

Chemical Properties

Molecular Weight	423.47
Formula	C₂₅H₂₁N₅O₂
Cas No.	120128-20-3
Smiles	N1=NNC(=N1)CC=2C=CC=CC2COC3=CC=C(OCC4=NC=5C=CC=CC5C=C4)C=C3
Relative Density.	1.308 g/cm3 (Predicted)

Storage & Solubility Information

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.

Solubility Information

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.36 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3614 mL	11.8072 mL	23.6144 mL	118.0721 mL
5 mM	0.4723 mL	2.3614 mL	4.7229 mL	23.6144 mL
10 mM	0.2361 mL	1.1807 mL	2.3614 mL	11.8072 mL
20 mM	0.1181 mL	0.5904 mL	1.1807 mL	5.9036 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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