Methapyrilene (hydrochloride) |
| Catalog No.GC48805 |
An H1 receptor antagonist and non-genotoxic carcinogen
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 135-23-9
Sample solution is provided at 25 µL, 10mM.
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Methapyrilene is a histamine H1 receptor antagonist (Ki = 4.5 nM) and non-genotoxic carcinogen.1,2 Dietary administration of methapyrilene (0.1%) induces liver tumors in rats, with greater than 50% of rats incurring distant metastases.3 It decreases the acetylation of histone 3 lysine 9 (H3K9) and H3K56, as well as the di- and trimethylation of H3K4 and H4K20, respectively, in rat liver when administered at 40 mg/kg per day for six weeks.2 Methapyrilene also increases 4-hydroxy nonenal (4-NHE) protein adducts in rat liver. Formulations containing methapyrilene were previously used as sleep aids.
1.Tran, V.T., Chang, R.S.L., and Snyder, S.H.Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramineProc. Natl. Acad. Sci. U.S.A.75(12)6290-6294(1978) 2.Shpyleva, S., Dreval, K., de Conti, A., et al.Editor's highlight: Organ-specific epigenetic changes induced by the nongenotoxic liver carcinogen methapyrilene in fischer 344 ratsToxicol. Sci.156(1)190-198(2017) 3.Lijinsky, W., Reuber, M.D., and Blackwell, B.N.Liver tumors induced in rats by oral administration of the antihistaminic methapyrilene hydrochlorideScience209(4458)817-819(1980)
| Cas No. | 135-23-9 | SDF | |
| Canonical SMILES | CN(C)CCN(CC1=CC=CS1)C2=NC=CC=C2.Cl | ||
| Formula | C14H19N3S•HCl | M.Wt | 297.8 |
| Solubility | DMF: 15 mg/ml,DMSO: 10 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 1 mg/ml | Storage | -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. |
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| 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 | 3.358 mL | 16.7898 mL | 33.5796 mL |
| 5 mM | 0.6716 mL | 3.358 mL | 6.7159 mL |
| 10 mM | 0.3358 mL | 1.679 mL | 3.358 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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