化合物 JAK3-IN-11|T9811|TargetMol

價(jià)格	￥10600	￥17500	￥13800
包裝	25mg	100mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 JAK3-IN-11	英文名稱:JAK3-IN-11
CAS:2412734-00-8	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.
產(chǎn)品類別: 抑制劑
貨號(hào): T9811

Product Introduction

Bioactivity

Name	JAK3-IN-11
Description	JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].
In vitro	JAK3-IN-11 (Compound 12) (10 μM, 72 h) has no obvious cytotoxicity at a concentration of 10 μM [1]. JAK3-IN-11 (Compound 12) (72 h) shows strong inhibition for T cell proliferation with IC 50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation) [1]. JAK3-IN-11 (Compound 12) (0-10 μM, 1h) abrogates IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner [1]. JAK3-IN-11 (Compound 12) covalently binds to JAK3 and irreversibly inhibits JAK3 [1]. Cell Proliferation Assay [1] Cell Line: Mouse T cells in complete RPMI1640 medium then exposed to anti-CD3/anti-CD28 or IL-2. Concentration: Incubation Time: 72 h. Result: Displayed strong inhibition for T cell proliferation with an IC 50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation), showed obvious significant immunosuppressive activity under selective inhibition of JAK3. Western Blot Analysis [1] Cell Line: Purified T cells were pre-activated coated with anti-CD3 and anti-CD28 for 72 h, then cultured with IL-2 (50 U/mL) for 36 h, then, cultured without IL-2 for 36 h Concentration: 0.01, 0.1, 1, 10 μM. Incubation Time: 1 h. Result: Abrogated IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner.
In vivo	JAK3-IN-11 (Compound 12) (Oxazolone (OXZ)-induced DTH Balb/c mice; 0-30 mg/kg; PO, prior to and during the challenge phase, 6 days) inhibits oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner [1]. Animal Model: Oxazolone (OXZ)-induced DTH Balb/c mice model [1]. Dosage: 30, 10, and 3 mg/kg. Administration: PO, prior to and during the challenge phase, 6 days. Result: Dose-dependently inhibited oxazolone (OXZ)-induced delayed-type hypersensitivity (DTH) responses. Animal Model: Male ICR mice [1]. Dosage: 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration. Administration: Pharmacokinetic Analysis Result: Preliminary pharmacokinetic data of JAK3-IN-11 (Compound 12) in male ICR Mice [1] Male ICR mice, 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration [1]. Compound 12 iv (10 mg/kg) po (30 mg/kg) AUC(0-t) (mg/Lh) a 1244.41 ± 77.83 889.42 ± 48.32 AUC(0-∞) (mg/Lh) 1274.41 ± 57.18 897.12 ± 56.72 MRT (0-∞) (h) b 0.73 ± 0.08 1.42 ± 0.38 Vz (L/kg) c 8.36 ± 1.83 220.42 ± 24.71 CLz (L/h/kg) d 8.15 ± 1.21 97.14 ± 20.87 t 1/2 (h) e 0.47 ± 0.06 1.52 ± 0.34 C max (mg/L) f 8763.23 ± 324.65 2008.21 ± 189.44 Bioavailability(%) g 23.82% a Area under the concentration time curve. b Mean residence time. c Volume in steady state. d Plasma clearance. e Terminal half-life. f Peak plasma concentrations. g Bioavailability = AUC 0-t (po)/AUC 0-t × 100%.
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Keywords	JAK-3-IN-11 \| JAK3-IN-11 \| JAK3IN11 \| JAK3 IN 11

關(guān)鍵字： JAK3-IN-11|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.265100萬(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)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營(yíng)模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.265100萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
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