Itraconazole-d5 (Synonyms: R51211-d5) |
| Catalog No.GC47474 |
An internal standard for the quantification of itraconazole
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1217510-38-7
Sample solution is provided at 25 µL, 10mM.
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Itraconazole-d5 is intended for use as an internal standard for the quantification of itraconazole by GC- or LC-MS. Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).1,2 It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).1,3 It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.2 It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).4
1.Vanden Bossche, H., Marichal, P., Le Jeune, L., et al.Effects of itraconazole on cytochrome P-450-dependent sterol 14α-demethylation and reduction of 3-ketosteroids in Cryptococcus neoformansAntimicrob. Agents Chemother.37(10)2101-2105(1993) 2.Kim, J., Tang, J.Y., Gong, R., et al.Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growthCancer Cell17(4)388-399(2010) 3.Warrilow, A.G., Melo, N., Martel, C.M., et al.Expression, purification, and characterization of Aspergillus fumigatus sterol 14-a demethylase (CYP51) isoenzymes A and BAntimicrob. Agents Chemother.54(10)4225-4234(2010) 4.Strating, J.R.P.M., van der Linden, L., Albulescu, L., et al.Itraconazole inhibits enterovirus replication by targeting the oxysterol-binding proteinCell Rep.10(4)600-615(2015)
| Cas No. | 1217510-38-7 | SDF | |
| Synonyms | R51211-d5 | ||
| Canonical SMILES | O=C(N(C(C)C([2H])([2H])C([2H])([2H])[2H])N=C1)N1C(C=C2)=CC=C2N3CCN(C4=CC=C(OC[C@]5([H])O[C@](C6=C(Cl)C=C(Cl)C=C6)(CN7N=CN=C7)OC5)C=C4)CC3 | ||
| Formula | C35H33Cl2D5N8O4 | M.Wt | 710.7 |
| Solubility | DMSO : ≥ 0.5 mg/mL (0.70 mM); DMF : ≥ 0.5 mg/mL (0.70 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4071 mL | 7.0353 mL | 14.0706 mL |
| 5 mM | 281.4 μL | 1.4071 mL | 2.8141 mL |
| 10 mM | 140.7 μL | 703.5 μL | 1.4071 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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