Latanoprost-PHXA41-DataSheet-生命科学试剂-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作靶点: Prostaglandin Receptor作通路: GPCR/G Protein储存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL

2、(231.17 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验

3、结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.78 mM); Clear solution2. 请依序添加每种溶剂： 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 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.78 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Latanoprost种前列腺素受体 (FP prostanoid receptor) 激动剂，能够降低眼内压。IC50 & Target FP Receptor体外研究 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.体内研究 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 您边的抑制剂师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.