| Identification | Back Directory | [Name]
Motolimod | [CAS]
172377-52-5 | [Synonyms]
E2MATE
ES-J 995
BLE 00084
Estradiol 3-sulfamate
Estra-1,3,5(10)-triene-3,17-diol (17β)-, 3-sulfamate | [Molecular Formula]
C18H25NO4S | [MDL Number]
MFCD00947822 | [MOL File]
172377-52-5.mol | [Molecular Weight]
351.46 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
8.88±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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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