Terfenadine (Synonyms: MDL 9918, NSC 665802, (±)-Terfenadine, DL-Terfenadine) |
| Catalog No.GC10978 |
Histamine H1-receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 50679-08-8
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) induces dose and time-dependent apoptosis on A375 melanoma cells. The IC50 after 24 h of TEF treatment in complete medium was 10.4 μM for A375 cells, 9.9 μM for Hs294T cells and 9.6 for HT144 cells[2]. Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity[2]. Terfenadine (10 μM; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms[2].
Terfenadine (p.o.; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate and enhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models[3].
References:
[1]. Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-307.
[2]. Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16(12):1253-67.
[3]. An L, et al. Terfenadine combined with epirubicin impedes the chemo-resistant human non-small cell lung cancer both in vitro and in vivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115.
| Cas No. | 50679-08-8 | SDF | |
| Synonyms | MDL 9918, NSC 665802, (±)-Terfenadine, DL-Terfenadine | ||
| Chemical Name | 1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O | ||
| Formula | C32H41NO2 | M.Wt | 471.67 |
| Solubility | ≥ 18mg/mL in DMSO | 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 | 2.1201 mL | 10.6006 mL | 21.2013 mL |
| 5 mM | 0.424 mL | 2.1201 mL | 4.2403 mL |
| 10 mM | 0.212 mL | 1.0601 mL | 2.1201 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 2 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *