M7571

MK-571 sodium salt hydrate

≥95% (HPLC), powder, leukotriene D4 antagonist

• 동의어(들): 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate, L-660711
• 실험식(Hill 표기법): C₂₆H₂₆ClN₂NaO₃S₂ · xH₂O
• CAS Number: 115103-85-0
• Molecular Weight: 537.07 (anhydrous basis)
• MDL number: MFCD11114392
• UNSPSC 코드: 51111800
• PubChem Substance ID: 329817910
• NACRES: NA.77

속성

• Product Name: MK-571 sodium salt hydrate, ≥95% (HPLC)
• Quality Level: 100
• 분석: ≥95% (HPLC)
• 양식: powder
• 저장 조건: desiccated
• 색상: white to beige
• solubility: H₂O: 15 mg/mL, clear
• 주관자: Merck & Co., Inc., Kenilworth, NJ, U.S.
• 배송 상태: wet ice
• 저장 온도: −20°C
• SMILES string: O.[Na+].CN(C)C(=O)CCSC(SCCC([O-])=O)c1cccc(\C=C\c2ccc3ccc(Cl)cc3n2)c1
• InChI: 1S/C26H27ClN2O3S2.Na.H2O/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22;;/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32);;1H2/q;+1;/p-1/b10-6+;;
• InChI key: MSHRPLRGSQECLY-DOLBFOAYSA-M

설명

애플리케이션

MK-571 sodium salt hydrate has been used:

• as an efflux inhibitor for monitoring multidrug resistance protein (MRP)-function and to avoid redundancy of other transporters
• to assess its effect on cell proliferation and 2D-migration in vitro in various cell lines of glioblastoma multiforme (GBM)
• as multidrug resistance (MDR) transporter inhibitor to study its effects in ovarian cancer cells
• as specific inhibitors of ABCC1/2 to investigate transport, toxicity, flow cytometry and arsenic efflux

생화학적/생리학적 작용

MK 571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK 571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK 571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors. It potentially inhibits MRP1 and has been shown to overcome acquired arsenic tolerance.

MK-571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor.

특징 및 장점

This compound is featured on the Leukotriene Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

안전성 정보

• 픽토그램: GHS07
• 신호어: Warning
• 유해 및 위험 성명서: H315,H319,H335
• 예방조치 성명서: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• 표적 기관: Respiratory system
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable
• 개인 보호 장비: dust mask type N95 (US), Eyeshields, Gloves