Tamibarotene (Synonyms: 他米巴羅汀; Am 80)

目錄號(hào): HY-14652 純度: 99.94%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Tamibarotene 是一種具有口服活性的視黃酸受體 α (RARα) 的激動(dòng)劑，比 RARγ 的選擇性高。

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Tamibarotene Chemical Structure

CAS No. : 94497-51-5

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥500	In-stock
1 mg	￥125	In-stock
5 mg	￥250	In-stock
10 mg	￥400	In-stock
50 mg	￥714	In-stock
100 mg		詢(xún)價(jià)
200 mg		詢(xún)價(jià)

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻(xiàn)

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•Pharmacol Res. 2020 Oct;160:105149. [Abstract]
•J Pathol. 2023 Feb 24. [Abstract]
•Phytomedicine. 2020, 153444.
•Int J Mol Sci. 2023, 24(3), 2586.
•Research Square Preprint. 2024 Jan 30.
•Research Square Preprint. 2023 Nov 17.
•IBRO Neuroscience Reports. 2021 Feb 14.

Tamibarotene 相關(guān)產(chǎn)品

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查看 RAR/RXR 亞型特異性產(chǎn)品:

查看所有亞型

RXRα RXRβ RXRγ

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Tamibarotene is an orally active retinoic acid receptor α (RARα) agonist, showing high selectivity over RARγ.

IC₅₀ & Target

RARα/β^[1]

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HL-60	ED₅₀	7.9 x 10^-10 M Compound: Am80 (3)	The ability to induce differentiation of human promyelocytic leukemia cell line HL-60 to mature granulocytes was determined by nitro blue tetrazolium (NBT) reduction assay The ability to induce differentiation of human promyelocytic leukemia cell line HL-60 to mature granulocytes was determined by nitro blue tetrazolium (NBT) reduction assay	[PMID: 8182710]
HL-60	IC₅₀	8.94 μM Compound: AM80	Cytotoxicity against Homo sapiens (human) HL60 cells assessed as growth inhibition after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) HL60 cells assessed as growth inhibition after 48 hr by MTT assay	10.1007/s00044-012-0019-9
HL-60	IC₅₀	8.94 μM Compound: AM80, Tamibarotene	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 22014829]
K562	IC₅₀	42.37 μM Compound: AM80	Cytotoxicity against Homo sapiens (human) K562 cells assessed as growth inhibition after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) K562 cells assessed as growth inhibition after 48 hr by MTT assay	10.1007/s00044-012-0019-9
K562	IC₅₀	42.37 μM Compound: AM80, Tamibarotene	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 22014829]
NB-4	IC₅₀	4.81 μM Compound: AM80	Cytotoxicity against Homo sapiens (human) NB4 cells assessed as growth inhibition after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) NB4 cells assessed as growth inhibition after 48 hr by MTT assay	10.1007/s00044-012-0019-9
NB-4	IC₅₀	4.81 μM Compound: AM80, Tamibarotene	Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay	[PMID: 22014829]

體外研究
(In Vitro)

Tamibarotene (20，40 μM) 下調(diào) T 細(xì)胞淋巴瘤細(xì)胞中細(xì)胞周期基因的表達(dá)。Tamibarotene (5 μM) 在 RARA 過(guò)表達(dá)細(xì)胞中增加 RARE 活性的程度比在 RARAlow 細(xì)胞中高得多。此外，RARAwt 過(guò)表達(dá)增加了由 Tamibarotene 處理引起的 CDK2、CDK4 和 CDK6 抑制的程度^[1]。
Tamibarotene 直接逆轉(zhuǎn)轉(zhuǎn)化生長(zhǎng)因子-β1 處理的真皮成纖維細(xì)胞的促纖維化表型，抑制內(nèi)皮細(xì)胞中 ICAM-1 的表達(dá)，并在體外促進(jìn) M1 巨噬細(xì)胞分化^[2]。
Tamibarotene (4 μM) 在 VSMC 中以劑量依賴(lài)性方式上調(diào) apelin mRNA 和蛋白質(zhì)水平。在 Tamibarotene 刺激下，RARα (視黃酸受體 α) 通過(guò)與預(yù)先結(jié)合到 apelin 啟動(dòng)子的 TCE 位點(diǎn)的 KLF5 和 Sp1 相互作用，被募集到 apelin 啟動(dòng)子，形成轉(zhuǎn)錄激活復(fù)合物，隨后導(dǎo)致 apelin 表達(dá)上調(diào)在 VSMC 中。KLF5 和 Sp1 通過(guò)直接結(jié)合 apelin 啟動(dòng)子上的 TCE 協(xié)同介導(dǎo) Tamibarotene 誘導(dǎo)的 apelin 表達(dá)^[4]。

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

體內(nèi)研究
(In Vivo)

Tamibarotene (1 mg/kg/天) 分別顯著減輕博來(lái)霉素 (BLM) 處理的小鼠和緊致皮膚 1 小鼠的真皮和真皮下纖維化。一致地，Tamibarotene 顯著抑制與組織纖維化相關(guān)的多種分子的表達(dá)，包括轉(zhuǎn)化生長(zhǎng)因子-β1、結(jié)締組織生長(zhǎng)因子、IL-4、IL-10、IL-13、IL-17A、腫瘤壞死因子-α、IFN BLM 處理小鼠的損傷皮膚中的-γ 和單核細(xì)胞趨化蛋白 1。此外，Tamibarotene 降低 BLM 處理小鼠引流淋巴結(jié)中 CD4⁺ T 細(xì)胞中效應(yīng) T 細(xì)胞的比例，同時(shí)增加幼稚 T 細(xì)胞的比例^[2]。
與未處理的小鼠相比，Tamibarotene (2.5 mg/kg，po) 不會(huì)導(dǎo)致牙周炎攻擊小鼠的 AST、ALT 或 ALP 血清水平發(fā)生任何顯著變化。Tamibarotene 改善牙槽骨吸收，顯著減少 P 的數(shù)量。gingivalis 誘導(dǎo)的小鼠破骨細(xì)胞。與 EPD 小鼠相比，Tamibarotene 顯著增加 CD4⁺ Foxp3⁺ Treg 細(xì)胞的百分比。Tamibarotene 還可有效降低 P 中 CD4⁺ROR-γt⁺ (Th17) 細(xì)胞的表達(dá)。gingivalis 感染的牙齦組織和 CLNs^[3]。Tamibarotene (1 mg/kg，po) 增加大鼠球囊損傷動(dòng)脈中的 apelin 表達(dá)，這與培養(yǎng)的 VSMCs的結(jié)果一致^[4]。
在老年 SAMP8 小鼠中，海馬 ADAM10 水平在給予 Tamibarotene (1 mg/kg/天) 后得到改善。Tamibarotene 給藥后 Hes5 和 Ki67 得到恢復(fù)，空間工作記憶也得到改善^[5]。

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

Clinical Trial

分子量

351.44

Formula

C₂₂H₂₅NO₃

CAS 號(hào)

94497-51-5

性狀

固體

顏色

White to off-white

中文名稱(chēng)

他米巴羅汀

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	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 25.5 mg/mL (72.56 mM; 超聲加熱助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.8454 mL	14.2272 mL	28.4544 mL
5 mM	0.5691 mL	2.8454 mL	5.6909 mL
10 mM	0.2845 mL	1.4227 mL	2.8454 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)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(qǐng)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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.11 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.11 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.11 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.94%

選擇批次：

Data Sheet (667 KB) SDS (393 KB)

COA (192 KB) LCMS (133 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Wang X, et al. Retinoic acid receptor alpha drives cell cycle progression and is associated with increased sensitivity to retinoids in T-cell lymphoma. Oncotarget. 2017 Apr 18;8(16):26245-26255. [Content Brief]

[2]. Toyama T, et al. Tamibarotene Ameliorates Bleomycin-Induced Dermal Fibrosis by Modulating Phenotypes of Fibroblasts, Endothelial Cells, and Immune Cells. J Invest Dermatol. 2016 Feb;136(2):387-98. [Content Brief]

[3]. Jin Y, et al. Tamibarotene modulates the local immune response in experimental periodontitis. Int Immunopharmacol. 2014 Dec;23(2):537-45. [Content Brief]

[4]. Lv XR, et al. Synthetic retinoid Am80 up-regulates apelin expression by promoting interaction of RARα with KLF5 and Sp1 in vascular smooth muscle cells. Biochem J. 2013 Nov 15;456(1):35-46. [Content Brief]

[5]. Kitaoka K, et al. The retinoic acid receptor agonist Am80 increases hippocampal ADAM10 in aged SAMP8 mice. Neuropharmacology. 2013 Sep;72:58-65. [Content Brief]

Cell Assay ^[1]	The CellTiter Aqueous Non-Radioactive Cell Proliferation Assay Kit is used to assess cell growth. Briefly, 10,000 cells per well are seeded in a 96-well plate and cultured in RPMI containing 2% charcoal-stripped FBS and indicated retinoid concentrations for 72 hours. At the end of the treatment period, the MTS reagent is added, cells are incubated an additional 2-4 hours, and absorbance is measured at 490 nanometers. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	For the infection, mice are given sulfamethoxazole and trimethoprim in an oral suspension at 10 mL of deionized water ad libitum for 10 days to reduce the native flora and to support colonization of P. gingivalis W83. Four days after the antibiotic therapy finishes, periodontal infection is established through oral inoculation using 1010 colony-forming units of P. gingivalis suspended in 100 μL 4% carboxymethyl cellulose (CMC) for 7 days. The mice are euthanized 4 weeks after the first oral inoculation. Tamibarotene (2.5 mg/kg) is suspended in a 0.5% carboxymethyl cellulose solution. The drug is orally gavaged into the esophagus daily in a volume of 0.1 mL/10 g body weight. Tamibarotene is administered 1 h before the induction of periodontitis and then given daily per the protocol until day 28. Control mice with periodontal disease receive the same volume of 0.5% carboxymethyl cellulose solution. The body weight of each mouse is measured every 3 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)	[1]. Wang X, et al. Retinoic acid receptor alpha drives cell cycle progression and is associated with increased sensitivity to retinoids in T-cell lymphoma. Oncotarget. 2017 Apr 18;8(16):26245-26255. [Content Brief] [2]. Toyama T, et al. Tamibarotene Ameliorates Bleomycin-Induced Dermal Fibrosis by Modulating Phenotypes of Fibroblasts, Endothelial Cells, and Immune Cells. J Invest Dermatol. 2016 Feb;136(2):387-98. [Content Brief] [3]. Jin Y, et al. Tamibarotene modulates the local immune response in experimental periodontitis. Int Immunopharmacol. 2014 Dec;23(2):537-45. [Content Brief] [4]. Lv XR, et al. Synthetic retinoid Am80 up-regulates apelin expression by promoting interaction of RARα with KLF5 and Sp1 in vascular smooth muscle cells. Biochem J. 2013 Nov 15;456(1):35-46. [Content Brief] [5]. Kitaoka K, et al. The retinoic acid receptor agonist Am80 increases hippocampal ADAM10 in aged SAMP8 mice. Neuropharmacology. 2013 Sep;72:58-65. [Content Brief]

Tamibarotene 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8454 mL	14.2272 mL	28.4544 mL	71.1359 mL
	5 mM	0.5691 mL	2.8454 mL	5.6909 mL	14.2272 mL
	10 mM	0.2845 mL	1.4227 mL	2.8454 mL	7.1136 mL
	15 mM	0.1897 mL	0.9485 mL	1.8970 mL	4.7424 mL
	20 mM	0.1423 mL	0.7114 mL	1.4227 mL	3.5568 mL
	25 mM	0.1138 mL	0.5691 mL	1.1382 mL	2.8454 mL
	30 mM	0.0948 mL	0.4742 mL	0.9485 mL	2.3712 mL
	40 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7784 mL
	50 mM	0.0569 mL	0.2845 mL	0.5691 mL	1.4227 mL
	60 mM	0.0474 mL	0.2371 mL	0.4742 mL	1.1856 mL

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:

Tamibarotene94497-51-5Am 80他米巴羅汀Am80Am-80RAR/RXRAutophagyApoptosisRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的用途提供醫(yī)藥研發(fā)服務(wù)，不為任何個(gè)人或者非科研性質(zhì)的、非用于藥證申報(bào)使用等其他用途提供服務(wù)。

站點(diǎn)地圖隱私聲明

滬ICP備15051369號(hào)-4

上海工商

滬公網(wǎng)安備31011502019417

滬(浦)應(yīng)急管危經(jīng)許[2021]201709(QFYS)

營(yíng)業(yè)執(zhí)照（三證合一）

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Tamibarotene (Synonyms: 他米巴羅汀; Am 80)

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MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻(xiàn)