M228

MRS 1220

solid

• 동의어(들): 9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline
• 실험식(Hill 표기법): C₂₁H₁₄ClN₅O₂
• CAS Number: 183721-15-5
• Molecular Weight: 403.82
• MDL number: MFCD01321046
• UNSPSC 코드: 12352209
• PubChem Substance ID: 24896720
• NACRES: NA.77

속성

• 양식: solid
• Quality Level: 100
• 색상: white
• solubility: DMSO: 2 mg/mL; 2-hydroxypropyl-β-cyclodextrin: insoluble; H₂O: insoluble; ethanol: insoluble
• SMILES string: Clc1ccc2nc(NC(=O)Cc3ccccc3)n4nc(nc4c2c1)-c5ccco5
• InChI: 1S/C21H14ClN5O2/c22-14-8-9-16-15(12-14)20-25-19(17-7-4-10-29-17)26-27(20)21(23-16)24-18(28)11-13-5-2-1-3-6-13/h1-10,12H,11H2,(H,23,24,28)
• InChI key: TWWFAXQOKNBUCR-UHFFFAOYSA-N
• 유전자 정보: human ... ADORA3(140) ; rat ... Adora1(29290), Adora2a(25369), Adora3(25370)

설명

생화학적/생리학적 작용

MRS1220 is a putative A3 adenosine receptor antagonist. MRS 1220 was found to be competitive in saturation binding studies using the agonist radioligand ¹²⁵I AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of ³⁵S guanosine 5′-O-(3-thiotriphosphate (³⁵S GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with KB values of 1.7 and 92 nM, respectively, proved to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A3 agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with an IC₅₀ value of 0.3 μM.

특징 및 장점

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable
• 개인 보호 장비: Eyeshields, Gloves, type N95 (US)