2. Metabolic Enzyme/Protease Anti-infection
  3. UGT Bacterial
  4. 16-Epiestriol

16-Epiestriol  (Synonyms: 16-epi-Estriol; 16β,17β-Estriol)

Cat. No.: HY-130046
COA
SDS
Handling Instructions Technical Support

16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases.

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16-Epiestriol

16-Epiestriol Chemical Structure

CAS No. : 547-81-9

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16-Epiestriol Related Antibodies

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Description

16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases[1][2].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

16-Epiestriol (200 μM; 15-60 min) is targeted by recombinant human UGT1A1, UGT1A7, UGT1A8, UGT2B15, UGT1A3, UGT2A1, UGT2B4, and UGT2B17 which exhibit low-level glucuronidation activity towards it, with regioselectivity for the 3-OH or 16-OH[1].
16-Epiestriol (0.2-300 μM; 15-60 min) is targeted by pooled human intestine microsomes which preferentially catalyze its 3-OH glucuronidation with a Vmax of 4111 ± 94 pmol/min/mg and Km of 50 ± 3 μM, with secondary activity at the 16-OH and 17-OH[1].
16-Epiestriol (200 μM, 0.2-300 μM; 15-60 min) is targeted by recombinant human UGT2B7 which exhibits high activity towards it, catalyzing 16-OH glucuronidation with a Vmax of 3866 ± 788 pmol/min/mg, Km of 38.4 ± 11.4 μM, and substrate inhibition with a Ki of 162 ± 86.4 μM[1].
16-Epiestriol (0.2-300 μM; 15-60 min) is targeted by recombinant human UGT1A10-F93G which catalyzes its 3-OH glucuronidation with a Vmax of 2249 ± 201 pmol/min/mg and Km of 186 ± 28.0 μM, exhibiting lower turnover and higher Km than wild-type UGT1A10[1].
16-Epiestriol (0.2-300 μM; 15-60 min) is targeted by pooled human liver microsomes which preferentially catalyze its 16-OH glucuronidation with a Vmax of 8011 ± 106 pmol/min/mg and Km of 33 ± 1 μM, with far lower activity at the 3-OH and 17-OH[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

16-Epiestriol Related Antibodies
In Vivo

16-Epiestriol (10-20 mg/kg; i.p.) exhibits potent anti-inflammatory activity in rats. At the dose of 20 mg/kg, it reduces carrageenan-induced paw swelling by 58% at 5 h, and its equimolar potency is more than twice that of Hydrocortisone (HY-N0583)[2].
16-Epiestriol (60 μg/rat; s.c.; administered at 0, 2, 4, and 6 h) exhibits no significant glycogenic activity in adrenalectomized rats, as it does not alter plasma or hepatic glucose concentrations compared with untreated control groups[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, mean body weight ~200 g)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose
Result: Reduced paw volume change to 0.22 mL (±0.05 SEM) at 1 h, 0.59 mL (±0.05 SEM) at 2 h, 0.71 mL (±0.05 SEM) at 3 h, and 0.50 mL (±0.06 SEM) at 5 h at 10 mg/kg.
Reduced paw volume change to 0.17 mL (±0.03 SEM) at 1 h, 0.44 mL (±0.05 SEM) at 2 h, 0.65 mL (±0.04 SEM) at 3 h, and 0.48 mL (±0.05 SEM) at 5 h at 20 mg/kg.
Reduced edema by 58% at 5 h compared to untreated controls at 20 mg/kg.
Reduced edema by 56% at 5 h on an equimolar basis, which is more than twice the efficacy of hydrocortisone.
Showed statistically significantly less edema at 5 h compared to untreated and hydrocortisone-treated groups (p < 0.001 by Student’s t-test) at 20 mg/kg.
Animal Model: Sprague-Dawley (adrenalectomized male, average body weight 185 g)[2]
Dosage: 60 μg/rat per dose; total cumulative dose 240 μg/rat (0.832 μmol/rat)
Administration: s.c.; four doses at 0, 2, 4, and 6 h
Result: Resulted in median plasma glucose concentration of 79.0 mg/dL and median liver glucose concentration of 93.9 μg/g of liver.
Showed no statistically significant differences in median plasma or liver glucose concentrations relative to untreated control groups.
Molecular Weight

288.38

Formula

C18H24O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@@H](O)[C@@H](O)C[C@@]1([H])[C@]3([H])CCC4=C(C=CC(O)=C4)[C@@]3([H])CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.04%

SDS (419 KB)

COA (249 KB)

Handling Instructions (2659 KB)
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16-Epiestriol Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

16-Epiestriol547-81-916-epi-Estriol 16β,17β-EstriolUGTBacterialUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseUGT2B17UGT1A10UGT2B7UGT1A7UGT1A3UGT1A8UGT1A1UGT2B4UGT2A1UGT2B15Inhibitorinhibitorinhibit

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