MK-6892_LCMS_09617_MedChemExpress

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MK2-IN-1_hydrochloride_SDS_MedChemExpress

Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jul.-24-2017Print Date:Jul.-24-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :MK2-IN-1 (hydrochloride)Catalog No. :HY-12834ACAS No. :1314118-94-91.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:MK2 InhibitorFormula:C27H26Cl2N4O2Molecular Weight:509.43CAS No. :1314118-94-94. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance Pink to red (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

MK-6892_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:MK–6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A . K i and GTPγS EC 50 of MK–6892 on the Human GPR109A is 4 nM and 16 nM, respectively.IC50 & Target: Ki: 4 nM (GPR109A)[1]EC50: 16 nM (GPR109A)[1]In Vitro: MK–6892 evokes a potent internalization of GPR109A in U2OS β–arrestin2–RrGFP cells.MK–6892 shows an EC 50 value of 74nM on calcium mobilization assay [2].In Vivo: MK–6892 is orally administered to WT or nicotinic acid (NA) receptor null mice on the same C57Bl/6 genetic background.After 15 min of 100 mg/kg dosing of MK–6892 to fed WT or NA receptor null mice, the blood levels of MK–6892 at 15 min are 229μM (~950–fold greater than the in vitro EC 50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148μM (~620–fold greater than the in vitro EC 50) in NA receptor null mice. MK–6892 effectively suppresses plasma FFA in the WT but not in the NA receptor null animals, indicating that the FFA reduction of MK–6892 is NA receptor–dependent. MK–6892 is selected for the studies because of its good PK and activity profiles in these two species (EC 50=4.6 μM in the GTPγS assay for the rat NA receptor and 1.3 μM in the GTPγS assay for the dog NA receptor). Despite the significant weaker activity of MK–6892 in rat and dog with respect to that in human, MK–6892 shows good activity in reducing FFA in rat and dog models [1].PROTOCOL (Extracted from published papers and Only for reference)Animal administration [1]MK–6892 was orally administered to WT or NA receptor null mice on the same C57Bl/6 genetic background. After 15 min of 100 mpk dosing of NA or 1e to fed WT or NA receptor null mice, the blood levels of MK–6892 at 15 min were 229 μM (950–fold greater than the in vitro EC50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148 μM (620–fold greater than the in vitro EC50) in NA receptor null mice.References:[1]. Shen HC, et al. Discovery of a biaryl cyclohexene carboxylic acid (MK–6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. J Med Chem. 2010 Mar 25;53(6):2666–70.[2]. Kim HY, et al. Discovery of 4–(phenyl)thio–1H–pyrazole derivatives as agonists of GPR109A, a high affinity niacin receptor. Arch Pharm Res. 2015 Jun;38(6):1019–32.Product Name:MK–6892Cat. No.:HY-10680CAS No.:917910-45-3Molecular Formula:C 19H 22N 4O 5Molecular Weight:386.40Target:GPR109A Pathway:GPCR/G Protein Solubility:10 mM in DMSOCaution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

依达拉奉右莰醇通过铁死亡-脂质过氧化通路对脑出血大鼠神经保护的作用机制

实验研究依达拉奉右莰醇通过铁死亡-脂质过氧化通路对脑出血大鼠神经保护的作用机制毛权西，李作孝△摘要：目的探讨依达拉奉右莰醇对脑出血大鼠的神经保护作用及血肿周围脑组织脂质过氧化的影响。

方法将128只SD大鼠随机分为假手术组、脑出血组、依达拉奉组和依达拉奉右莰醇组，每组32只。

除假手术组外，其余组大鼠构建急性脑出血模型，依达拉奉组、依达拉奉右莰醇组于造模后分别腹腔注射依达拉奉6mg/kg、依达拉奉右莰醇7.5mg/kg，每12h注射1次，假手术组和脑出血组腹腔注射等量生理盐水。

术后1d、3d、7d和14d按Garcia评分标准进行神经功能评分，HE染色观察血肿周围脑组织病理变化，化学荧光法检测血肿周围脑组织活性氧（ROS）含量，微量酶标法检测血肿周围脑组织还原型谷胱甘肽（GSH）含量，蛋白免疫印迹法检测血肿周围脑组织谷胱甘肽过氧化物酶4（GPX4）、长链脂酰辅酶A合成酶4（ACSL4）和磷脂胆碱酰基转移酶3（LPCAT3）表达。

结果与假手术组比较，脑出血组大鼠神经功能评分降低，血肿周围脑组织出现大量炎性细胞浸润及神经细胞变性，ROS含量、ACSL4和LPCAT3蛋白表达水平升高，GSH含量、GPX4蛋白表达水平降低（P＜0.05）；与脑出血组比较，依达拉奉组和依达拉奉右莰醇组大鼠神经功能评分升高，血肿周围脑组织病理损伤明显减轻，ROS含量、ACSL4和LPCAT3蛋白表达水平降低，GSH含量、GPX4蛋白表达水平增加（P＜0.05）；依达拉奉右莰醇组干预效果优于依达拉奉组（P＜0.05）；除假手术组外，其余各组均在术后3d时变化最明显，术后7d、14d逐渐恢复（P＜0.05）。

结论依达拉奉右莰醇可能通过调节脑出血大鼠神经细胞铁死亡相关蛋白的表达，减少脑组织脂质过氧化，抑制神经细胞铁死亡，从而发挥脑保护作用。

关键词：依达拉奉右莰醇；依达拉奉；脑出血；铁死亡；脂质过氧化中图分类号：R743.34文献标志码：A DOI：10.11958/20221777Neuroprotective mechanism of edaravone dexborneol in rats with cerebral hemorrhage throughferroptosis-lipid peroxidation pathwayMAO Quanxi,LI Zuoxiao△Department of Neurology,the Affiliated Hospital of Southwest Medical University,Luzhou646000,China△Corresponding Author E-mail:Abstract:Objective To investigate the neuroprotective effect of edaravone dexborneol on cerebral hemorrhage in rats and the effect of lipid peroxidation on perihematomal brain tissue.Methods A total of128SD rats were randomly divided into the sham-operated group,the cerebral hemorrhage group,the edaravone group and the edaravone dexborneol group, with32rats in each group.The acute cerebral hemorrhage model was constructed in all groups except for the sham-operated group.The edaravone group and edaravone dexamphene group were injected intraperitoneally with6mg/kg of edaravone and edaravone dexamphene7.5mg/kg,one injection every12hours.The sham-operated group and the cerebral hemorrhage group were injected intraperitoneally with equal amounts of saline.The neurological function was scored according to Garcia score at1d,3d,7d,and14d after surgery.Brain tissue around hematoma was stained with HE staining.Chemo fluorescence assay was used to observe pathological changes and reactive oxygen species(ROS)content of brain tissue around hematoma.Micro enzyme labeling assay was used to detect glutathione(GSH)content of brain tissue around hematoma.The expression levels of glutathione peroxidase4(GPX4),long-chain lipid acyl-coenzyme A synthase4(ACSL4) and phospholipid choline acyltransferase3(LPCAT3)in brain tissue around hematoma were detected by protein immunoblotting.Results Compared with the sham-operated group,neurological function scores were decreased in the cerebral hemorrhage group.Massive inflammatory cell infiltration and neuronal degeneration in brain tissue around hematoma were found,and ROS content,ACSL4and LPCAT3protein expression level increased.GSH content and GPX4 protein expression level decreased in the cerebral hemorrhage group(P＜0.05).Compared with the cerebral hemorrhage group,neurological function scores were increased,histopathological damage around the hematoma was significantly基金项目：泸州市人民政府-西南医科大学科技战略合作基金项目（2018LZXNYD-ZK17）作者单位：西南医科大学附属医院神经内科（邮编646000）作者简介：毛权西（1990），男，硕士在读，主要从事神经免疫方向研究。

龙葵正丁醇提取物体外抗肿瘤活性的研究

学试剂有限公司（号：０８５２；洲茄胺：ｉ批２００２）澳Ｓｇｍａ公司（批号：９０）００３；薯蓣皂苷元：中国药品生物制品检定所（号：４批１３— ００１；５９２００）乙醇、油醚、石乙酸乙酯、仿、丁醇、氯正氨水硝
作用并探讨其可能的物质基础方法：用酸溶碱沉法从龙葵正丁醇总浸膏中分离出生物碱．孔吸附树脂及丙酮沉淀法采大
分离出皂苷。Ｍ１以ｒｒ法考察龙葵正丁醇不同提取物对人肝癌细胞株ＳＭＭＣ７２、ｐ２和人胃癌细胞株ＭＣ８３增殖一７１ＨｅＧＧ一０
１。霪． Biblioteka … ； ¨ ｊｉ
龙葵正丁醇提取物体外抗肿瘤活性的研究
高思国李冠业丁霞（南京农业大学理学院，江苏南京２０９）１０５
摘
要目的：研究龙葵正丁醇提取物对人肝癌细胞株ＳＭＭＣ７２、ｅＧ一７１Ｈｐ２和人胃癌细胞株ＭＧ一０Ｃ８３增殖的抑制
的抑制作用，并采用倒置显微镜观察药物对上述３细胞株细胞形态的影响。果：葵正丁醇各提取物对ＳＣ７２、种结龙ＭＭ一７１Ｈｐ２ＭＧ一０ｅＧ、Ｃ８３细胞均有比较显著的细胞增殖抑制作用，呈剂量依赖关系且并且可使上述肿瘤细胞株的细胞形态发生显著变化，引起细胞株的凋亡或坏死结论：葵正丁醇部位是龙葵抗肿瘤活性部位．龙生物碱及皂苷是其可能的物质基础关键词肿瘤细胞株中图分类号龙葵植物提取物细胞抑制率文献标识码Ａ病理学体外实验Ｒ８．１２２７文章编号１７ — ９Ｘ（００ｌ－０６０６２３７２１）１０７ — ３

高效液相色谱法测定盐酸苯海拉明注射液中苯甲醇含量

高效液相色谱法测定盐酸苯海拉明注射液中苯甲醇含量
陈莉
【期刊名称】《海峡药学》
【年(卷),期】2013(25)12
【摘要】目的采用高效液相色谱法建立测定盐酸苯海拉明注射液中苯甲醇的方法.方法色谱柱Agilent氰基柱(250mm×4.6mm,5μm),流动相为乙腈-20mM乙酸铵(用甲酸调pH值至6.5)(50:50),检测波长为257nm.结果苯甲醇浓度在0.625～3.75μL·mL-1范围内与峰面积呈良好的线性关系,r为1.000;苯甲醇加样回收率的平均值为100.3%,RSD=1.4%.结论本方法简便、准确可靠,适用于盐酸苯海拉明注射液中苯甲醇的质量控制.
【总页数】3页(P121-123)
【作者】陈莉
【作者单位】福建省南平市第一医院制剂室,南平,353000
【正文语种】中文
【中图分类】R927.2
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