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  3. Acolbifene hydrochloride

Acolbifene hydrochloride (Synonyms: EM-652 hydrochloride; SCH 57068 hydrochloride)

Cat. No.: HY-16023 Purity: 98.48% ee.: 98.04%
Handling Instructions

Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.

For research use only. We do not sell to patients.

Acolbifene hydrochloride Chemical Structure

Acolbifene hydrochloride Chemical Structure

CAS No. : 252555-01-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 217 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 217 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties[1][2][3][4][5].

IC50 & Target[5]

ERα

2 nM (IC50, E2-induced transcriptional activity)

ERβ

0.4 nM (IC50, E2-induced transcriptional activity)

In Vitro

Acolbifene (ACOL) does not affect pathways of cholesterol synthesis, supporting the involvement of the clearance-related receptors in its hypocholesterolemic action[2].
Acolbifene (EM-652) shows no agonistic activity on ERα and ERβ transcriptional function and blocks the estradiol (E2)-mediated activation of both ERα and ERβ[3].
Acolbifene (EM-652) shows the most potent inhibition of estradiol-stimulated cell proliferation in human breast cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity[4].

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

In Vivo

Acolbifene (ACOL) reduces food intake and strongly decreases cholesterolemia in rats fed a cholesterol-free diet[2].
Acolbifene (ACOL) reduces food intake (16%) and weight gain (45%, mainly fat) similarly in both dietary cohorts[2].

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

Animal Model: Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g[2].
Dosage: 2.5 mg/kg.
Administration: Oral gavage, once daily for 21 d.
Result: Prevents tumor growth in rats.
Clinical Trial
Molecular Weight

494.02

Formula

C₂₉H₃₂ClNO₄

CAS No.
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
Solvent & Solubility
In Vitro: 

DMSO : 180 mg/mL (364.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0242 mL 10.1210 mL 20.2421 mL
5 mM 0.4048 mL 2.0242 mL 4.0484 mL
10 mM 0.2024 mL 1.0121 mL 2.0242 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
Acolbifene hydrochloride
Cat. No.:
HY-16023
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