鹽酸阿米洛利作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetAmiloride hydrochlorideCat. No.: HY-B0285ACAS No.: 2016-88-8分式: CHClNO分量: 266.09作靶點(diǎn): Sodium Channel; TRP Channel; Apoptosis作通路: Membrane Transporter/Ion Channel; Neuronal Signaling; Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100

2、mg/mL (375.81 mM)H2O : 7.14 mg/mL (26.83 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.7581 mL 18.7906 mL 37.5813 mL5 mM 0.7516 mL 3.7581 mL 7.5163 mL10 mM 0.3758 mL 1.8791 mL 3.7581 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)

3、品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。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?。以下溶解案都?qǐng)先按照 In Vitro 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 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)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；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/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-

4、80 45% salineSolubility: 2.5 mg/mL (9.40 mM); Clear solution此案可獲得 2.5 mg/mL (9.40 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.40 mM); Clear s

5、olutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (9.40 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.40 mM); Clear solution此案可獲得 2.5 mg/mL (9.40 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100

6、 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Amiloride hydrochloride (MK-870 hydrochloride)上鈉通道 (ENaC1) 和尿激酶型纖溶酶原激活物受體 (uTPA2) 的抑制劑。Amiloride hydrochloride是polycystin-2 (PC2; TRPP23) 通道阻斷劑。IC & Target ENaC1; uTPA2; polycystin-2(TRPP2)3體外研究 Amiloride blocks channels with an IC50 o

7、f 2.6 M. The Ki of amiloride for ENaC is 26-fold that of channels (0.1 M for ENaC). Amiloride blockade of ENaC is much more voltage dependent compared withthe channel. The Ki of amiloride for channels is 920 and 13.7 M at 120 and +80 mV, respectively, whichsignificantly differs from that of both and

8、 channels1. Amiloride is a relatively selective inhibitor of theepithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel)in the concentration range of 0.1 to 0.5 M. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger(NHE) wi

9、th an IC50 as low as 3 M in the presence of a low external Na+ but as high as 1 mM in the presence of ahigh Na+. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride(1 M) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, i

10、nhibit the myogenicvasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloridecompletely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 M) in vascular smooth musclecells (VSMC)2.體內(nèi)研究 Amiloride (1 mg/kg/day) subcutaneousl

11、y is found to reverse the initial increases in collagen deposition and preventany further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brainand kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP)

12、 comparedwith controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renaltissues in animals with salt-dependent forms of hypertension2.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) J Am Chem Soc. 2018 Dec 12;140(49):17234-17240. Theranostics. 2019 May 31;9(13):3732-3753. Br J Pha

13、rmacol. 2020 Apr 15. Cell Physiol Biochem. 2018;51(6):2564-2574. J Nanobiotechnology. 2020 Jan 31;18(1):26.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCESPage 2 of 3 www.MedChemE1. Ji, H.L., et al. delta ENaC: a novel divergent amiloride-inhibitable sodium channel. Am

14、J Physiol Lung Cell Mol Physiol, 2012. 303(12): p. L1013-26.2. Teiwes J, et al. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17.3. Giamarchi A, et al. A polycystin-2 (TRPP2) dimerization domain essential for the function of heteromeric polycystin complexes. EMBO J. 2010 Apr7;29(7):1176-91.McePdfHe