苯磺酸貝托司汀|T6405|TargetMol

價(jià)格	￥118	￥178	￥247
包裝	10mg	25mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:苯磺酸貝托司汀	英文名稱:Bepotastine Besilate
CAS:190786-44-8	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.90%	產(chǎn)品類別: 抑制劑
貨號(hào): T6405

Product Introduction

Bioactivity

名稱	Bepotastine Besilate
描述	Bepotastine Besilate (TAU 284) is a non-sedating and selective H1 receptor antagonist (pIC50: 5.7).
激酶實(shí)驗(yàn)	Isothermal Titration Calorimetry (ITC) of Nucelotide Binding: The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.
體外活性	The flux ratios of [14C]Bepotastine (5 μM) in LLC-GA5-COL150 cells are significantly greater than those in LLC-PK1, showing that the B-to-A flux exceeds those in the other direction in LLC-GA5-COL150 cells. Bepotastine stimulates P-gp-mediated ATP hydrolysis with Km, Vmax, and Vmax/Km values of 1.25 mM, 108 nmol/min/mg protein, and 0.087 mL/min/mg protein, respectively. [2] Bepotastine besilate (100 mM) suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured dorsal root ganglion neurons and cultured neutrophils. [3] Bepotastine (100 μM) dose-dependently inhibits chemotaxis of cultured guinea pig peritoneal eosinophils induced by LTB4. Bepotastine (1 mM) significantly reduces A23187-induced histamine release of cultured rat peritoneal mast cells. [4]
體內(nèi)活性	Bepotastine (0.8 mg/kg) administrated in WT and P-gp KO mice results in the plasma total concentrations 580 ng/mL and 467 ng/mL at 6 min after dosing, respectively, and the plasma protein binding with 41.1% and 45.9%. The absorption of [14C]Bepotastine from the proximal region in the presence and absence of verapamil is 63.0% and 72.4%, respectively, and that from the distal region is 10.9% and 62.7%, respectively. [2] Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site). Bepotastine besilate (1 mg/kg-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B(4) (0.03 nmol/site). [3] Bepotastine besilate significantly inhibits conjunctival vascular hyperpermeability in a dose-dependent manner in guinea pig allergic conjunctivitis models with maximal effect for Bepotastine besilate 1.5%. [4] Bepotastine (3 mg/kg and 10 mg/kg) effectively inhibits the compound 48/80-induced scratching behavior of BALB/c mice 1 hour after oral administration. Bepotastine (10 mg/kg) also significantly inhibits the scratching behavior and suppresses the serum LTB(4) levels in atopic dermatitis model NC/Nga mice. [5]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 101 mg/mL (184.6 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	Inhibitor \| TAU-284 \| Bepotastine \| inhibit \| pruritus \| TAU284 \| Histamine Receptor \| urticaria \| atopic dermatitis \| conjunctivitis \| LTB 4 \| Bepotastine Besilate
相關(guān)產(chǎn)品	Famotidine \| Meclizine dihydrochloride \| Nizatidine \| Lidocaine \| Sodium butanoate \| Alginic acid \| Mirtazapine \| Amitriptyline hydrochloride \| Trazodone hydrochloride \| Mianserin hydrochloride \| Doxepin hydrochloride \| Chlorphenesin
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌上市藥物庫(kù) \| 已知活性化合物庫(kù) \| FDA 上市藥物庫(kù) \| GPCR靶點(diǎn)分子庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 疼痛相關(guān)化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：苯磺酸貝托司汀|||TAU 284|||Talion|||Bepreve|||Bepotastine Beslilate|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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