| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| ln Vitro |
4-Hydroxytamoxifen, also known as Monohydroxytamoxifen, functions as a selective antagonist of estrogen receptors. It binds to [3H]oestradiol with an IC50 of 3.3 nM. The human 8S estrogen receptor is inhibited from binding [3H]oestradiol by 4-hydroxytamoxifen (10, 100 nM) [1]. 4-Hydroxytamoxifen decreases off-target CRISPR-mediated gene editing and activates intein-linked inactive Cas9. Conditionally activated Cas9 is 25 times more selective than wild-type Cas9 at altering target genomic locations in human cells [2].
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| ln Vivo |
In immature rats, 4-Hydroxytamoxifen (0.2, 1, and 5 μg/d) reduces uterine wet weight in a dose-related manner [1]. 4-The methamphetamine-induced nigrostriatal dopamine depletion in both sexes of intact and gonadectomized C57BL/6 J mice is significantly attenuated by hydroxytamoxifen (6 μg/0.1 mL sesame oil, once daily subcutaneous injection). 4-The striatum's dopamine levels are unaffected by 4-hydroxytamoxifen [3].
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| Enzyme Assay |
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| References |
[1]. Jordan VC, et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. J Endocrinol. 1977 Nov;75(2):305-16.
[2]. Davis KM, et al. Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat Chem Biol. 2015 May;11(5):316-8. [3]. Kuo YM, et al. 4-Hydroxytamoxifen attenuates methamphetamine-induced nigrostriatal dopaminergic toxicity in intact and gonadetomized mice. J Neurochem. 2003 Dec;87(6):1436-43. [4]. Zhang J, et al. Drug Inducible CRISPR/Cas Systems. Comput Struct Biotechnol J. 2019;17:1171-1177 |
| Molecular Formula |
C26H29NO2
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|---|---|
| Molecular Weight |
387.52
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| Exact Mass |
387.2198
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| CAS # |
68047-06-3
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| Related CAS # |
(E/Z)-4-Hydroxytamoxifen;68392-35-8;(E)-4-Hydroxytamoxifen;174592-47-3
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| SMILES |
O(C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])/C(/C1C([H])=C([H])C(=C([H])C=1[H])O[H])=C(\C1C([H])=C([H])C([H])=C([H])C=1[H])/C([H])([H])C([H])([H])[H]
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| Synonyms |
ICI 79280 trans-4-Hydroxytamoxifen (Z)-4-Hydroxytamoxifen
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~129.03 mM)
Ethanol : ~20 mg/mL (~51.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (12.90 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5805 mL | 12.9026 mL | 25.8051 mL | |
| 5 mM | 0.5161 mL | 2.5805 mL | 5.1610 mL | |
| 10 mM | 0.2581 mL | 1.2903 mL | 2.5805 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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