Description
Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo
Product information
CAS Number: 135-23-9
Molecular Weight: 297.85
Formula: C14H20ClN3S
Chemical Name: N-[2-(dimethylamino)ethyl]-N-[(thiophen-2-yl)methyl]pyridin-2-amine hydrochloride
Smiles: Cl.CN(C)CCN(CC1=CC=CS1)C1C=CC=CN=1
InChiKey: BONORRGKLJBGRV-UHFFFAOYSA-N
InChi: InChI=1S/C14H19N3S.ClH/c1-16(2)9-10-17(12-13-6-5-11-18-13)14-7-3-4-8-15-14;/h3-8,11H,9-10,12H2,1-2H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (335.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Methapyrilene hydrochloride (650 μM) results in a down-regulation of TF and up-regulation of FTL, while the level of HMOX1 is not changed. Additionally, the levels of CD44 and SOX9 proteins and the expression of PROM1 (CD133), hepatic stem cell-associated markers are increased. Methapyrilene hydrochloride (650 μM) decreases CYP2E1, CYP3A4, NR1l3, ALB, mRNA expression and increases CD133 expression.
In Vivo:
Methapyrilene hydrochloride (oral gavage; 40 or 80 mg/kg; 5 days per week; 6 weeks) results in changes in the expression of classic hepatotoxicity-related marker genes and iron homeostasis-related genes, especially a prominent, dose-dependent down-regulation of the transferrin (Tf) gene and an up-regulation of the ferritin, light chain (FTL) gene in rats. Methapyrilene hydrochloride (oral gavage; 150 mg/kg; 3 days) causes periportal liver necrosis at high dosage. Methapyrilene is sufficient to induce liver necrosis, or a subtoxic dose of 50 mg/kg/day.
Products are for research use only. Not for human use.
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