| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
RG 12525 selectively and more than 8000 times antagonizes the spasmodic actions of LTC4, LTD4, and LTE4 on lung strips (KB value = 3 nM) and competitively inhibits the binding of 3H-LTD4 to lung membranes (Ki = 3.0 +/- 0.3 nM)[1]. RG 12525 (at 2.5 µM or 25 µM) suppresses CYP2C9 and -3A4 microsomal activity, but not CYP1A2, -2A6, -2C19, or -2D6. At 5 and 10 µM midazolam doses, RG 12525 (25 µM) likewise significantly inhibits [2].
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|---|---|
| ln Vivo |
ORAL RG 12525 suppresses bronchoconstriction (ED50 = 0.6 mg/kg), wheal development (ED50 = 5 mg/kg, 9 mg/kg t1/2 = 10 hours), anaphylaxis mortality (ED50 = 2.2 mg)/kg, t1/2 = 7 hours (10 mg/kg), and antigen-induced bronchoconstriction (ED50 = 0.6 mg/kg) [1]. In an anaphylaxis paradigm, RG 12525 decreases antigen-induced mortality; ED50 (95% confidence interval) = 2.2 (0.8-6.4) mg/kg. RG 12525 also reduced LTD4-induced bronchoconstriction with an ED50 = 0.6 (0.4-1.0) mg/kg in a lung function model[3].
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| References |
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| Molecular Formula |
C25H21N5O2
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|---|---|
| Molecular Weight |
423.47
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| Exact Mass |
423.17
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| CAS # |
120128-20-3
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| PubChem CID |
129044
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| Appearance |
White to yellow solid powder
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| Density |
1.308g/cm3
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| Boiling Point |
667ºC at 760 mmHg
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| Flash Point |
227.3ºC
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| Vapour Pressure |
1.17E-17mmHg at 25°C
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| Index of Refraction |
1.681
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| LogP |
4.496
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
559
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JELDFLOBXROBFH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H21N5O2/c1-2-7-20(19(6-1)15-25-27-29-30-28-25)16-31-22-11-13-23(14-12-22)32-17-21-10-9-18-5-3-4-8-24(18)26-21/h1-14H,15-17H2,(H,27,28,29,30)
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| Chemical Name |
2-[[4-[[2-(2H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]quinoline
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| Synonyms |
RG12525; RG-12525; RG 12525
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~59.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.91 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3614 mL | 11.8072 mL | 23.6144 mL | |
| 5 mM | 0.4723 mL | 2.3614 mL | 4.7229 mL | |
| 10 mM | 0.2361 mL | 1.1807 mL | 2.3614 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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