Nimodipine_HNMR_25290_MedChemExpress

Inhibitors, Agonists, Screening Data SheetBIOLOGICAL ACTIVITY: Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti–analgesic.In Vitro: Nociceptin (1 μg/mL) significantly prevents LPS (10 ng/mL)–stimulated cell migration whereas it is ineffective when addedalone. Nociceptin (1 nM–10 μM) elicits a concentration–dependent blockade of LPS–mediated cell migration, with a maximal effectat 1 and 10 μM. Nociceptin counteracts LPS–induced elevation of IL–1β mRNA levels. Nociceptin (1 μM) and NNC 55–0396 induceapoptotic cell death in U87 cells. Nociceptin (1 μM) counteracts LPS–induced [Ca2+]i increase in U87 cells via β–arrestin 2.Nociceptin counteracts the LPS–induced phosphorylation of PKC and ERK in U87 cells. Nociceptin inhibits the LPS–mediatedtranscriptional activation of NF–kB and AP–1 reporter genes[1].PROTOCOL (Extracted from published papers and Only for reference) Cell Assay:[1]Cell proliferation assay is carried out in the assay. U87 cells are plated on 12–well plate and treated for 24 hmaintained in cell culture medium containing 10% fetal bovine serum. Five hours before the end of the treatments, [methyl–3H]Thymidine (50 nM final concentration) is added to serum–free cell culture medium and the plate is incubated at 37°C. Thereafter,medium is removed and cells are washed twice with PBS. 200 μL of PBS is added to each well, the cells are scraped off and centrifugedat 13,000g for 3 min at 4°C; supernatants are then discarded, pellets resuspended in 500 μL of cold trichloroacetic acid (10% w/v),incubated on ice for 20 min and centrifuged at 13,000g for 3 min at 4°C. The obtained supernatant is then discarded, pellet suspendedin 500 μL of cold methanol and centrifuged at 3 min for 13,000g at 4°C. After that, the pellet is suspended in 200 μL of NaOH 1 N andheated at 55°C for 10 min. Samples are then neutralized with 200 μL of HCl 1 N and 350 μL of the labeled DNA incubated in countingvials with 4 mL of Filter Count scintillation liquid. Vials are vortexed and incubated overnight at room temperature and theradioactivity is determined by liquid scintillation spectrometry.References: [1]. Bedini A, et al. Nociceptin/orphanin FQ antagonizes lipopolysaccharide–stimulated proliferation, migration and inflammatory signaling in humanglioblastoma U87 cells. Biochem Pharmacol. 2017 Sep 15;140:89–104.Product Name:NociceptinCat. No.:HY-P0183CAS No.:170713-75-4Molecular Formula:C79H129N27O22Molecular Weight:1809.04Target:Opioid Receptor; Opioid ReceptorPathway:GPCR/G Protein; Neuronal SignalingSolubility:DMSO

File ..170619 2017-06-19 09-04-59\WW4359-003-1_1.D Tgt Mass (CHM): Injection Date : 19 Jun 17 11:17 am +0800 Seq. Line : 27 Sample Name : WW4359-003-1_1 Location : P2-A-02 Acq. Operator : CLJ_701 Inj : 1 Spec. Reported : MS Integration Inj Volume : 0.5 ul

Acq. Method : D:\chem32\1\DATA\20170619\20170619 2017-06-19 09-04-59\1-POS-3MIN.M

Analysis Method : D:\CHEM32\1\DATA\20170619\20170619 2017-06-19 09-04-59\1-POS-3MIN.M

Catalog No : HY-16973 Batch#25003 A-RP-186

Method Info : Mobile Phase: A: water(0.01%TFA) B:ACN(0.01%TFA)

Gradient: 5% to 95%B within 1.3 min

Flow Rate :1.8ml/min

Column :SunFire C18, 4.6*50mm,3.5um A-RP-186

Oven Temperature : 45C

min0.511.522.5mAU

05001000 DAD1 B, Sig=214,4 Ref=off

1.586

1.7472.084

min0.511.522.5mAU

0200400600 DAD1 C, Sig=254,4 Ref=off

1.455

1.482

1.7412.084

min0.511.522.5050000100000 MSD1 TIC, MS File ES-API, Pos, Scan, Frag: 70

Inhibitors, Agonists, Screening Data SheetBIOLOGICAL ACTIVITY: Imidazole is a planar 5–membered ring. Imidazole is a highly polar compound. Imidazole has been used extensively as a corrosioninhibitor.Imidazole is incorporated into many important biological molecules. The most pervasive is the amino acid histidine, which has animidazole side–chain. Imidazole is useful as a buffer in the pH range of 6.2–7.8 One of the applications of imidazole is in thepurification of His–tagged proteins in immobilised metal affinity chromatography(IMAC). Imidazole is used to elute tagged proteinsbound to Ni ions attached to the surface of beads in the chromatography column. An excess of imidazole is passed through thecolumn, which displaces the His–tag from nickel co–ordination, freeing the His–tagged proteins. Imidazole has become an importantpart of many pharmaceuticals. Synthetic imidazoles are present in many fungicides and antifungal, antiprotozoal, and antihypertensivemedications. Imidazole is part of the theophylline molecule, found in tea leaves and coffee beans, which stimulates the central nervoussystem. It is present in the anticancer medication mercaptopurine, which combats leukemia by interfering with DNA activities.Product Name:ImidazoleCat. No.:HY-D0837CAS No.:288-32-4Molecular Formula:C3H4N2Molecular Weight:68.08Solubility:H2O: ≥ 100 mg/mLCaution: 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,

Inhibitors, Agonists, Screening

Safety Data SheetRevision Date:Oct.-06-2018Print Date:Oct.-06-2018

1. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :(R)-GNE-140

Catalog No. :HY-100742A

CAS No. :2003234-63-51.2 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 USA

Tel:609-228-6898

Fax:609-228-5909

E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-6898

2. 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.