Phenoxybenzamine-d5 (hydrochloride) |
| Katalog-Nr.GC46202 |
Phenoxybenzamin-d5 (Hydrochlorid) ist das mit Deuterium markierte Phenoxybenzamin-Hydrochlorid.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1329838-45-0
Sample solution is provided at 25 µL, 10mM.
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Phenoxybenzamine-d5 is intended for use as an internal standard for the quantification of phenoxybenzamine by GC- or LC-MS. Phenoxybenzamine is an antagonist of α-adrenergic receptors (α-ARs).1,2 It inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing α1-ARs (EC50s = 125.9-316.2 nM), as well as radioligand binding to α2A-, α2B-, and α2C-ARs in CHO cell membranes (Kis = 60, 10, and 60 nM, respectively). Phenoxybenzamine (0.5-5 μM) decreases norepinephrine-, histamine-, and calcium-induced contractions in isolated rabbit aortic strips.3 It also inhibits proliferation of nine cancer cell lines, including lymphoma, breast, and lung cancer cells, with IC50 values ranging from 29.5 to 99.8 μM.4 Phenoxybenzamine (3-1,000 μg/kg) reduces increases in diastolic blood pressure induced by the α-AR agonists cirazoline , St-587, Sgd 101/75, and B-HT 920 in pithed rats.5 It also decreases the time to find the platform in the Morris water maze, indicating restored spatial memory, in a rat model of fluid percussion-induced traumatic brain injury (TBI).6 Formulations containing phenoxybenzamine have been used in the treatment of hypertension and hyperhidrosis associated with pheochromocytomas, an adrenal medullary neuroendocrine tumor.
|1. Minneman, K.P., Theroux, T.L., Hollinger, S., et al. Selectivity of agonists for cloned α1-adrenergic receptor subtypes. Mol. Pharmacol. 46(5), 929-936 (1994).|2. Frang, H., Cockcroft, V., Karskela, T., et al. Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J. Biol. Chem. 276(33), 31279-31284 (2001).|3. McPherson, G.A., Krstew, E., and Malta, E. Effects of phenoxybenzamine on responses to some receptor agonists and calcium in vitro. Clin. Exp. Pharmacol. Physiol. 12(5), 455-464 (1985).|4. Inchiosa, M.A., Jr. Anti-tumor activity of phenoxybenzamine and its inhibition of histone deacetylases. PLoS One 13(6):e0198514, (2018).|5. Timmermans, P.B., Thoolen, M.J., Mathy, M.J., et al. Effects of the irreversible α-adrenoceptor antagonists phenoxybenzamine and benextramine on the effectiveness of nifedipine in inhibiting α1- and α2-adrenoceptor mediated vasoconstriction in pithed rats. Naunyn Schmiedebergs Arch. Pharmacol. 329(4), 404-413 (1985).|6. Rau, T.F., Kothiwal, A., Rova, A., et al. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury. Int. J. Mol. Sci. 15(1), 1402-1417 (2014).
| Cas No. | 1329838-45-0 | SDF | |
| Canonical SMILES | [2H]C1=C(OCC(C)N(CC2=CC=CC=C2)CCCl)C([2H])=C([2H])C([2H])=C1[2H].Cl | ||
| Formula | C18H17ClD5NO • HCl | M.Wt | 345.3 |
| Löslichkeit | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.3 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml | 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. |
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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 | 2.896 mL | 14.4802 mL | 28.9603 mL |
| 5 mM | 0.5792 mL | 2.896 mL | 5.7921 mL |
| 10 mM | 0.2896 mL | 1.448 mL | 2.896 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 31 reference(s) in Google Scholar.)
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