Motolimod
Motolimod Basic information
- Product Name:
- Motolimod
- Synonyms:
-
- Estradiol 3-sulfamate
- BLE 00084
- E2MATE
- ES-J 995
- Estra-1,3,5(10)-triene-3,17-diol (17β)-, 3-sulfamate
- Estradiol Sulfamate
- E2MATE|||BLE 00084|||ES-J 995
- ZK-190628
- CAS:
- 172377-52-5
- MF:
- C18H25NO4S
- MW:
- 351.46
- Mol File:
- 172377-52-5.mol
Motolimod Chemical Properties
- Melting point:
- 202-204 °C(Solv: methanol (67-56-1))
- Boiling point:
- 531.1±60.0 °C(Predicted)
- Density
- 1.319±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 62.5 mg/mL (177.83 mM)
- pka
- 8.88±0.70(Predicted)
- form
- Solid
- color
- White to off-white
Motolimod Usage And Synthesis
Uses
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM.
in vivo
Estradiol 3-sulfamate is readily transformed and absorbed in the gut into its oxidative metabolite, EMATE, and both compounds have already been shown to be potent, long-acting, and orally active STS inhibitors[2].
References
[1] Numazawa M, et al. Inhibition of estrone sulfatase by aromatase inhibitor-based estrogen 3-sulfamates. Steroids. 2006 May;71(5):371-9. DOI:10.1016/j.steroids.2005.12.004
[2] Pohl O, et al. Synergistic effects of E2MATE and norethindrone acetate on steroid sulfatase inhibition: a randomized phase I proof-of-principle clinical study in women of reproductive age. Reprod Sci. 2014 Oct;21(10):1256-65. DOI:10.1177/1933719114522526
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