4-Hydroxytamoxifen (4-羥基他莫昔芬）

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 是一種口服有效，選擇性的雌激su受體調(diào)節(jié)劑 (SERM)。4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 基于 ER 介導(dǎo)的細(xì)胞核易位誘導(dǎo) CRISPR/Cas9 系統(tǒng)。

貨號：HY-16950
CAS：68047-06-3

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-16950

起訂量：1

規(guī)格:：10mg

價(jià)格:：￥950

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產(chǎn)品詳情

4-Hydroxytamoxifen (Synonyms: 4-羥基他莫昔芬）

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 是一種口服有效，選擇性的雌激su受體調(diào)節(jié)劑 (SERM)。4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 基于 ER 介導(dǎo)的細(xì)胞核易位誘導(dǎo) CRISPR/Cas9 系統(tǒng)。

生物活性

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]^[2]

Estrogen receptor 3.3 nM (IC₅₀)

CRISPR/Cas9

體外研究(In Vitro)

4-Hydroxytamoxifen (Monohydroxytamoxifen) is a selective ostrogen 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].

體內(nèi)研究(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].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00084344	Northwestern University\|National Cancer Institute (NCI)	Breast Cancer	April 2003	Not Applicable

分子量：387.51

Formula：C₂₆H₂₉NO₂

CAS 號：68047-06-3

中文名稱：4-羥基他莫昔芬

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 50 mg/mL (129.03 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 20 mg/mL (51.61 mM; Need ultrasonic)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5806 mL	12.9029 mL	25.8058 mL
5 mM	0.5161 mL	2.5806 mL	5.1612 mL
10 mM	0.2581 mL	1.2903 mL	2.5806 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

參考文獻(xiàn)

[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.

[4]. Zhang J, et al. Drug Inducible CRISPR/Cas Systems. Comput Struct Biotechnol J. 2019;17:1171-1177.

4-Hydroxytamoxifen (4-羥基他莫昔芬）

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 是一種口服有效，選擇性的雌激su受體調(diào)節(jié)劑 (SERM)。4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 基于 ER 介導(dǎo)的細(xì)胞核易位誘導(dǎo) CRISPR/Cas9 系統(tǒng)。

貨號：HY-16950
CAS：68047-06-3

品牌：MCE

型號：HY-16950

起訂量：1

規(guī)格:：10mg

價(jià)格:：￥950

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產(chǎn)品詳情

4-Hydroxytamoxifen (Synonyms: 4-羥基他莫昔芬）

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 是一種口服有效，選擇性的雌激su受體調(diào)節(jié)劑 (SERM)。4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) 基于 ER 介導(dǎo)的細(xì)胞核易位誘導(dǎo) CRISPR/Cas9 系統(tǒng)。

生物活性

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]^[2]

Estrogen receptor 3.3 nM (IC₅₀)

CRISPR/Cas9

體外研究(In Vitro)

4-Hydroxytamoxifen (Monohydroxytamoxifen) is a selective ostrogen 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].

體內(nèi)研究(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].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00084344	Northwestern University\|National Cancer Institute (NCI)	Breast Cancer	April 2003	Not Applicable

分子量：387.51

Formula：C₂₆H₂₉NO₂

CAS 號：68047-06-3

中文名稱：4-羥基他莫昔芬

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 50 mg/mL (129.03 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 20 mg/mL (51.61 mM; Need ultrasonic)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5806 mL	12.9029 mL	25.8058 mL
5 mM	0.5161 mL	2.5806 mL	5.1612 mL
10 mM	0.2581 mL	1.2903 mL	2.5806 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

參考文獻(xiàn)

[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.

[4]. Zhang J, et al. Drug Inducible CRISPR/Cas Systems. Comput Struct Biotechnol J. 2019;17:1171-1177.

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4-Hydroxytamoxifen (4-羥基他莫昔芬）

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4-Hydroxytamoxifen (Synonyms: 4-羥基他莫昔芬）

4-Hydroxytamoxifen (4-羥基他莫昔芬）

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4-Hydroxytamoxifen (Synonyms: 4-羥基他莫昔芬）