Latanoprost-PHXA41-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELatanoprostCat. No.: HY-B0577CAS No.: 130209-82-4Synonyms: PHXA41分式: CHO分量: 432.59作靶點: Prostaglandin Receptor作通路: GPCR/G Protein儲存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL

2、(231.17 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3117 mL 11.5583 mL 23.1166 mL5 mM 0.4623 mL 2.3117 mL 4.6233 mL10 mM 0.2312 mL 1.1558 mL 2.3117 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗

3、結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.78 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.78 mM); Clear solution1/3 Master of Small Molecule

4、s 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.78 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Latanoprost種前列腺素受體 (FP prostanoid receptor) 激動劑，能夠降低眼內(nèi)壓。IC50 & Target FP Receptor體外研究 Benzalkonium chloride latanoprost (BAK-latanoprost) and 0.02% BAK induce significant apo

5、ptosis in theapical layers that correlated with the significant decrease of cell viability. Preservative-free latanoprost (PF-latanoprost) slightly decreases cell viability and few apoptotic cells are found in the superficial layers, withoutreaching statistical significance compared with PBS 1. Lata

6、noprost (0.1 M) significantly increases cellviability as compared with control. Meanwhile, 0.1 M latanoprost results in the obvious promotion of neuriteoutgrowth similar to ciliary neurotrophic factor (CNTF) and simultaneously increases the levels of p-Akt andp-mTOR expression. Latanoprost can promo

7、te neurite outgrowth through an FP receptor-mediatedmodulation of the PI3K-Akt-mTOR signaling pathway 3. Latanoprost (0.03 or 0.3 g/mL) and bimatoprostincrease MMP-9 activity by 75% 27% and 75% 24%, respectively, in human CBSM cells 4.體內(nèi)研究 A single drop of latanoprost results in marked miosis, anter

8、ior bowing of the peripheral iris, narrowing of theiridocorneal angle, and shallowing of the anterior chamber of the beagle dog. Following latanoprost, the pupildiameter, ACA, and AOD (means) decreases 84%, 14%, and 16%, respectively 2.PROTOCOLCell Assay 1 Cellular viability is evaluated in duplicat

9、e at 24 hours with the MTT assay. The 3D-HCEs are transferred to24-well plates containing 300 L of MTT solution diluted at 0.5 mg/mL in the culture medium, and 300 L ofthe same MTT solution is applied on the apical surface of the 3D-HCEs. Reconstituted tissues are incubatedfor 3 hours at 37C. Then t

10、hey are transferred to 24-well plates containing 750-L isopropanol, and 750-Lisopropanol is added to the apical surface of the 3D-HCEs. The plates are agitated for 2 hours at roomtemperature before reading the optical density (OD) at 570 nm versus OD 690 nm. The results are expressedas percentages o

11、f cell viability (mean SD) compared with the negative control (PBS).MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Pauly A, et al. In vitro and in vivo comparative toxicological study of a new preservative-free latanoprost formulation. Inv

12、est OphthalmolVis Sci. 2012 Dec 13;53(13):8172-80.2. Tsai S, et al. The effect of topical latanoprost on anterior segment anatomic relationships in normal dogs. Vet Ophthalmol. 2013Sep;16(5):370-6.3. Zheng J, et al. Latanoprost promotes neurite outgrowth in differentiated RGC-5 cells via the PI3K-Ak

13、t-mTOR signaling pathway. Cell MolNeurobiol. 2011 May;31(4):597-604.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE4. Ooi YH, et al. Effect of bimatoprost, latanoprost, and unoprostone on matrix metalloproteinases and their inhibitors in human ciliary bodysmooth muscle cells. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5259-65.5. BAnn True Gabelt, et al. Prostaglandin Subtype-Selective and Non-Selective IOP-Lowering Comparison in Monkeys.