Home Tools

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).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

RG-12525, CAS 120128-20-3

Please contact us for prices and availability for the specification of product you are interested at.
Product consultation

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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	PPARγ:60 nM, CYP3A4:0.5 μM (ki), LTC4:2.6 nM(Guinea pig), 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.

Related Products

Related compounds with same targets

Methysticin Lecanoric acid Isocupressic acid Dipterocarpol 8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate 6',7'-Dihydroxybergamottin α-Viniferin RG-12525

Dose Conversion

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

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

RG-12525 120128-20-3 DNA损伤和修复代谢 P450 PPAR RG 12525 NID 525 RG12525 Inhibitor inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.