化合物 PLX5622 hemifumarate,PLX5622 hemifumarate

化合物 PLX5622 hemifumarate|T12505|TargetMol

價(jià)格	￥11313
包裝	200mg

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:化合物 PLX5622 hemifumarate	英文名稱:PLX5622 hemifumarate
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): T12505

Product Introduction

Bioactivity

Name	PLX5622 hemifumarate
Description	PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor with an IC 50 of 0.016 μM and Ki of 5.9 nM. PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. In vivo, PLX5622 hemifumarate demonstrates desirable PK properties in varies animals [1] [2].
In vitro	PLX5622 (1-20 μM; 3 days) hemifumarate effectively depletes microglia while not affecting oligodendrocytes or astrocytes in cerebellar slices. PLX5622 (4 μM; 3 days) hemifumarate leads to a 30-40% reduction in NG2+ or PDGFRα+ cells, increasing to 90-95% at 20 μM. No reduction of NG2+ or PDGFRα+ OPCs is observed in slices exposed to 1 μM or 2 μM PLX5622 despite robust (~95%) depletion of the microglial cells [3].
In vivo	Pharmacodynamics of PLX5622 hemifumarate in preclinical studies PLX5622 (1200 ppm; chow; for 3 weeks or 3 days; adult C57/Bl6 wild type mice) hemifumarate causes around 80% of microglia lost after 3 days of treatment and a 99% microglia loss after 3 weeks of treatment. PLX5622 (adult C57/Bl6 wild type mice aged 3 months; diet for 3 weeks) reduces microglia in cortex, striatum, cerebellum and hippocampus [4]. PLX5622 (50 mg/kg; intraperitoneal injection; once (neonatal rat) or twice (adult rat) a day; for a total of 14 days) hemifumarate depletes microglia by 80-90% within 3 days of treatment, which increases to > 90% by 7 days. After 14 days of PLX5622 treatment, microglia is depleted by > 96% in both neonates and adults while preserving baseline astrocyte quantity. (A single daily injection of 0.65% PLX5622 suspended in 5% dimethyl sulfoxide and 20% Kolliphor RH40 in 0.01 M PBS is sufficient for neonatal microglia depletion, adult depletion requires injections twice daily) [5]. PLX5622 (formulated in AIN-76A standard chow at 1200 mg/kg; for 28 days) hemifumarate leads to reduction in microglia throughout the CNS in 14-month-old 5xfAD mice [6]. Pharmacokinetics of PLX5622 hemifumarate in preclinical species [4] Species IV PO (gavage) Dose (mg/kg) AUC 0-∞ (ng hr/mL) CL (mL/min/kg) Vss (L/kg) t 1/2 (hr) Dose (mg/kg) AUC 0-∞ (ng hr/mL) Cmax (ng/mL) F Mouse 1.92 15,500 2.1 0.34 2.6 45 215,000 26,300 59% Rat (male) 1.13 2,630 7.7 1.2 2.3 45 99,600 12,000 95% Rat (female) 1.13 5,110 3.7 1.0 3.9 45 181,000 15,600 89% Dog 1.00 6,230 3.0 2.3 15 45 96,500 3,630 34% Monkey 1.35 2,100 11 1.6 2.2 ND ND ND ND Preparation of gavage dosing suspensions for PLX5622 hemifumarate [4] PLX5622 hemifumarate is dissolved in DMSO at a concentration that is 20x the final dosing solution. The compound stock is protected from light. A fresh stock is made each week. The components of the diluent generally are prepared a day or more in advance because they take time to dissolve completely: a) 2% hydroxypropyl methyl cellulose (HPMC): 2.0 g powder was brought to 100 mL deionized water; b) 25% Polysorbate 80 (PS80): 25 g was brought to 100 mL deionized water. To make 100 mL diluent, add 25 mL of 2% HPMC stock (0.5% final) and 4 mL of 25% PS80 stock (1% final) to 71 mL deionized water to have final 100 mL. Final composition after mixing with compound: 0.5% HPMC, 1% PS80, 5% DMSO. On each dosing day, the compound stock is diluted 20-fold as follows: 19 volumes of diluent are measured into the tube, and 1 volume of the 20x compound/DMSO stock is added. The cap is closed and the content of the tube is mixed by inversion and placed in a sonicating water bath to make a uniform suspension.
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 100 mg/mL (220.53 mM), Sonication is recommended.
Keywords	PLX5622 hemifumarate \| PLX-5622 Hemifumarate \| PLX 5622 \| PLX-5622 \| PLX5622 \| PLX 5622 Hemifumarate \| PLX5622 Hemifumarate \| PLX-5622 hemifumarate
Inhibitors Related	Onatasertib \| Cerdulatinib hydrochloride \| Sotuletinib \| Masitinib \| GW2580 \| c-Fms-IN-1 \| Linifanib \| c-Fms-IN-13 \| Pexidartinib \| PLX5622 \| c-Fms-IN-3 \| Pazopanib Hydrochloride

關(guān)鍵字： PLX5622 hemifumarate|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	589.8595萬(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)	中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,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：589.8595萬(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：抑制劑&激動(dòng)劑，天然產(chǎn)物，重組蛋白，化合物庫(kù)，技術(shù)服務(wù)
公司地址：上海市靜安區(qū)江場(chǎng)三路238號(hào)8樓

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