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(E/Z)-4-Hydroxytamoxifen

Cat. No. M7839
(E/Z)-4-Hydroxytamoxifen Structure
Synonym:

Afimoxifene

Size Price Availability Quantity
5mg USD 58  USD58 In stock
10mg USD 85  USD85 In stock
50mg USD 245  USD245 In stock
100mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

(E/Z)-4-Hydroxytamoxifen is the racemate of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen and a modulator of the estrogen receptor (ER).

Chemical Information
Molecular Weight 387.51
Formula C26H29NO2
CAS Number 68392-35-8
Solubility (25°C) Methanol 10 mg/mL
DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alexandra K Knox, et al. Heterodimeric GW7604 Derivatives: Modification of the Pharmacological Profile by Additional Interactions at the Coactivator Binding Site

[2] T E Mrdter, et al. Activity levels of tamoxifen metabolites at the estrogen receptor and the impact of genetic polymorphisms of phase I and II enzymes on their concentration levels in plasma

[3] Anastasia Detsi, et al. Synthesis of (Z)-4-hydroxytamoxifen and (Z)-2-[4-[1-(p-hydroxyphenyl)-2-phenyl]-1butenyl]phenoxyacetic acid

[4] F Zhang, et al. Synthesis and reactivity of a potential carcinogenic metabolite of tamoxifen: 3,4-dihydroxytamoxifen-o-quinone

[5] D N Pathak, et al. Activation of 4-hydroxytamoxifen and the tamoxifen derivative metabolite E by uterine peroxidase to form DNA adducts: comparison with DNA adducts formed in the uterus of Sprague-Dawley rats treated with tamoxifen

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Keywords: (E/Z)-4-Hydroxytamoxifen, Afimoxifene supplier, Estrogen Receptor, inhibitors, activators


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