Acolbifene hydrochloride

Modify Date: 2024-01-07 12:48:10

Acolbifene hydrochloride structure	Common Name	Acolbifene hydrochloride
	CAS Number	252555-01-4	Molecular Weight	494.02200
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₉H₃₂ClNO₄	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Acolbifene hydrochloride

Acolbifene (EM-652) hydrochloride, the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) hydrochloride possesses potent and pure anticarcinogenic properties[1][2].

Name	(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2H-chromen-7-ol,hydrochloride
Synonym	More Synonyms

Description	Acolbifene (EM-652) hydrochloride, the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) hydrochloride possesses potent and pure anticarcinogenic properties[1][2].
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
Target	Estrogen receptor:0.110 nM (IC50, in T-47D cells.)
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].
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]. 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.
References	[1]. Wang T, et al. Recent advances in selective estrogen receptor modulators for breast cancer. Mini Rev Med Chem. 2009 Sep;9(10):1191-201. [2]. Christian Lemieux, et al. The selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats. J Nutr. 2005 Sep;135(9):2225-9. [3]. A Tremblay, et al. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 1998 Jan;139(1):111-8. [4]. Sylvain Gauthier, et al. Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution. J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77.

Molecular Formula	C₂₉H₃₂ClNO₄
Molecular Weight	494.02200
Exact Mass	493.20200
PSA	62.16000
LogP	6.76680
Vapour Pressure	1.42E-17mmHg at 25°C

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Acolbifene hydrochloride (USAN)

Acolbifene Hydrochloride

EM 652.Hydrochloride

Acolbifene HCl

DC Chemicals Limited
China
Product Name: Acolbifene hydrochloride
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: ￥2170/10 mM * 1 mL in DMSO

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