Amodiaquine-dihydrochloride-Amodiaquin-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAmodiaquine dihydrochlorideCat. No.: HY-B1322BCAS No.: 69-44-3Synonyms: Amodiaquin dihydrochloride分式: CHClNO分量: 428.78作靶點(diǎn): Parasite; Histone Methyltransferase作通路: Anti-infection; Epigenetics儲(chǔ)存式: 4C, sealed storage, away from moi

2、sture and light* In solvent : -80C, 6 months; -20C, 1 month (sealedstorage, away from moisture and light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (291.52 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.3322 mL 11.6610 mL 23.3220 mL5 mM 0.4664 mL 2.3322 mL 4.6644 mL10 mM 0.2332 mL 1.1661 m

3、L 2.3322 mL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，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄的儲(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，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.85 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10

4、% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.85 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Amodiaquine dihydrochloride (Amodiaquin dihydrochloride)種4-氨喹啉類抗瘧劑，種有效的具有服活性的組胺 N-甲轉(zhuǎn)移酶 (histamine N-methyltransferase) 抑制劑，Ki 值為 18.6 nM。Amodiaquin

5、edihydrochloride 也種 Nurr1 激動(dòng)劑，可特異性結(jié)合 Nurr1 的配體結(jié)合域，EC50 為 20 M。抗炎作。IC50 & Target EC50: 20 M (Nurr1-LBD (ligand binding domain) 1Histamine N-methyltransferase 3體外研究 Amodiaquine (10-20 M; 4 hours) treatment suppresses LPS-induced expression of proinflammatorycytokines (IL-1, interleukin-6, TNF- and iNO

6、S) in a dose-dependent manner 1.Amodiaquine (5 M; 24 hours) significantly inhibits neurotoxin (6-OHDA-induced cell death in primarydopamine cells as examined by the number of TH+ neurons and dopamine uptake. The neuroprotectiveeffect of Amodiaquine is also observed in rat PC12 cells 1.RT-PCR 1Cell L

7、ine: Primary microgliaConcentration: 10 M, 15 M, 20 MIncubation Time: 4 hoursResult: Suppressed LPS-induced expression of proinflammatory cytokines (IL-1, interleukin-6,TNF- and iNOS) in a dose-dependent manner.體內(nèi)研究 Amodiaquine (40 mg/kg; intraperitoneal injection; daily; for 3 days; male ICR mice)

8、treatment diminishesperihematomal activation of microglia/macrophages and astrocytes. Amodiaquine also suppresses ICH-induced mRNA expression of IL-1, CCL2 and CXCL2, and ameliorated motor dysfunction of mice 2.Animal Model: Male ICR mice (8-10weeks of age) induced ntracerebral hemorrhage (ICH) 2Dos

9、age: 40 mg/kgAdministration: Intraperitoneal injection; daily; for 3 daysResult: Diminished perihematomal activation of microglia/macrophages and astrocytes. Biochem Biophys Res Commun. 2019 Dec 2. pii: S0006-291X(19)32185-0.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Chun-

10、Hyung Kim, et al. Nuclear receptor Nurr1 agonists enhance its dual functions and improve behavioral deficits in an animal model2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEof Parkinsons disease. Proc Natl Acad Sci U S A. 2015 Jul 14;112(28):8756-61.2. Keita Kinoshita, et al. A Nurr1 agonist amod

11、iaquine attenuates inflammatory events and neurological deficits in a mouse model ofintracerebral hemorrhage. J Neuroimmunol. 2019 May 15;330:48-54.3. Akira Yokoyama, et al. Effect of amodiaquine, a histamine N-methyltransferase inhibitor, on, Propionibacterium acnes andlipopolysaccharide-induced he

12、patitis in mice. Eur J Pharmacol. 2007 Mar 8;558(1-3):179-84.4. M T HOEKENGA. The treatment of acute malaria with single oral doses of amodiaquin, chloroquine, hydroxychloroquine andpyrimethamine. Am J Trop Med Hyg. 1954 Sep;3(5):833-8.5. John R Horton, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct21;353(2):334-344.McePdfHeightCautio