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68047-06-3

68047-06-3 structure
68047-06-3 structure
  • Name: 4-hydroxytamoxifen
  • Chemical Name: afimoxifene
  • CAS Number: 68047-06-3
  • Molecular Formula: C26H29NO2
  • Molecular Weight: 387.514
  • Catalog: API Antibiotics Other antibiotics
  • Create Date: 2018-05-09 08:00:00
  • Modify Date: 2024-01-04 11:35:07
  • 4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
Name afimoxifene
Synonyms MFCD00278780
4-hydroxytamoxifen
4-[(1Z)-1-{4-[2-(Dimethylamino)ethoxy]phenyl}-1-phenyl-1-buten-2-yl]phenol
Phenol, 4-[(1Z)-1-[[4-[2-(dimethylamino)ethoxy]phenyl]phenylmethylene]propyl]-
4-{(1Z)-1-[{4-[2-(dimethylamino)ethoxy]phenyl}(phenyl)methylidene]propyl}phenol
4-{(1Z)-1-[{4-[2-(dimethylamino)ethoxy]phenyl}(phenyl)methylene]propyl}phenol
4-hydroxy-tamoxifen
Description 4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
Related Catalog
Target

Estrogen receptor:3.3 nM (IC50)

CRISPR/Cas9
In Vitro 4-Hydroxytamoxifen (Monohydroxytamoxifen) is a selective oestrogen receptor antagonist, with an IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor. 4-Hydroxytamoxifen (10, 100 nM) enables to inhibit the binding of [3H]oestradiol to the human 8 S oestrogen receptor[1]. 4-Hydroxytamoxifen activates intein-linked inactive Cas9, reduces off-target CRISPR-mediated gene editing. In human cells, conditionally active Cas9s modify target genomic sites with up to 25-fold higher specificity than wild-type Cas9[2].
In Vivo 4-Hydroxytamoxifen (0.2, 1 and 5 μg/day, p.o.) causes a dose-related decrease in uterine wet weight of immature rats[1]. 4-Hydroxytamoxifen (6 μg/0.1 mL sesame oil/day, s.c.) effectively attenuates methamphetamine-induced nigrostriatal dopamine depletions in bothsexes of intact and gonadectomized C57BL/6 J mice. 4-Hydroxytamoxifen does not alter the dopamine content levels in the striatum[3].
Kinase Assay Cytosol (200 μL) is incubated for 30 min at 4°C with different concentrations of oestradiol, tamoxifen and (4-Hydroxytamoxifen) or dihydroxytamoxifen administered in 10 μL methanol. Control tubes are incubated with 10 μL methanol alone and non-specific binding is determined in a parallel incubation of cytosol (200 μL) with methanol (10 μL) containing DES (5 × 106 M). [2,4,6,7-3H]Oestradiol solution (50 μL) in TED buffer is added to each tube to give a final concentration of 2 × 10-9 M. Incubation is continued for 4 h (4°C) and then 400 μL of a suspension of dextran-coated charcoal (250 mg % Norit A, 2.5 mg % dextran) in TED buffer are added and allowed to stand for 20 min. Tubes are centrifuged at 800 g for 10 min (4°C) and 400 μL samples of the supernatant are added to 10 mL tritium scintillator (6 g butyl PBD, 135 mL toluene, 720 ml dioxan, 100 g naphthalene, 45 mL absolute methanol). Samples are counted for 10 min in a liquid scintillation spectrometer. Counting efficiency is determined by external standardization (35-36 %). Results are represented as a percentage of the specifically bound radioactivity (c.p.m.) in the control tubes[1].
Animal Admin Mice[3] Animals of each sex are divided into two groups: one group receives 4-Hydroxytamoxifen [6 μg/0.1 mL sesame oil/day, subcutaneously (s.c.) starting at 06.00 h] injections for three consecutive days, while the other group receives an equivalent amount of sesame oil injection for 3 days. Four hours following the third injection, each group is then subdivided into two groups: one receives four cumulative doses of methamphetamine hydrochloride (10 mg/kg, s.c.), and the other receives a comparable volume of saline at 2-h intervals. Bilateral gonadectomy is performed under pentobarbital anesthesia (50 mg/kg, intraperitoneally). Five weeks after surgery,gonadectomized mice of each sex are randomly divided into six groups. Five groups of each sex receive three daily injections ofvarious concentrations of 4-Hydroxytamoxifen (0, 1.5, 3.0, 6.0, and 12.0 μg/0.1 mL sesame oil/day). Four hours following the third injection, mice receive four doses of methamphetamine (MA, 10 mg/kg) at 2-h intervals. The remaining group of each sex receives sesame oil pretreatment for three consecutive days, followed by saline injections, and serves as the control group[3].
References

[1]. Jordan VC, et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. J Endocrinol. 1977 Nov;75(2):305-16.

[2]. Davis KM, et al. Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat Chem Biol. 2015 May;11(5):316-8.

[3]. Kuo YM, et al. 4-Hydroxytamoxifen attenuates methamphetamine-induced nigrostriatal dopaminergic toxicity in intact and gonadetomized mice. J Neurochem. 2003 Dec;87(6):1436-43.
Density 1.1±0.1 g/cm3
Boiling Point 514.4±50.0 °C at 760 mmHg
Melting Point 105-107ºC
Molecular Formula C26H29NO2
Molecular Weight 387.514
Flash Point 264.9±30.1 °C
Exact Mass 387.219818
PSA 32.70000
LogP 7.34
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.597
Storage condition 2-8°C
Stability Stable. Store cool. Incompatible with strong oxidizing agents.
Water Solubility 95% ethanol: 20 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SL1210000
CHEMICAL NAME :
Phenol, 4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-b utenyl)-, (E)-
CAS REGISTRY NUMBER :
68047-06-3
LAST UPDATED :
199801
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C26-H29-N-O2
MOLECULAR WEIGHT :
387.56

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
50 ug/kg
SEX/DURATION :
female 4 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
TYPE OF TEST :
DNA adduct

MUTATION DATA

TEST SYSTEM :
Rodent - mouse
DOSE/DURATION :
480 umol/kg/4D (Continuous)
REFERENCE :
CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 15,2087,1994
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Warning
Hazard Statements H302-H312-H332-H361
Precautionary Statements P280
Personal Protective Equipment Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
Hazard Codes Xn
Risk Phrases R20/21/22;R63
Safety Phrases S22-S23-S36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS SL1210000

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title: CAS No. 68047-06-3 | Chemsrc address: https://m.chemsrc.com/en/baike/524526.html

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