5.30923

Kir6.2/SUR1 Channel Activator, VU0071063

• 동의어(들): Kir6.2/SUR1 Channel Activator, VU0071063, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione, 7-(4-( tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione, 7-(4-(tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener
• 실험식(Hill 표기법): C₁₈H₂₂N₄O₂
• CAS Number: 333415-38-6
• Molecular Weight: 326.39
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC₅₀ = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC₅₀ = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC₅₀ >100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC₅₀ = 65 µM) and Kir2.3 (IC₅₀ = 91 µM) channels. Inhibits glucose-stimulated Ca²⁺ influx into mouse pancreatic β-cells.

A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC₅₀ = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC₅₀ = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC₅₀ >100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC₅₀ = 65 µM) and Kir2.3 (IC₅₀ = 91 µM) channels. Inhibits glucose-stimulated Ca²⁺ influx into mouse pancreatic β-cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

생화학적/생리학적 작용

EC₅₀ = 7 µM for Kir6.2/SUR1 channel activation

Primary Target
SUR1-containing channels

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

기타 정보

Raphemot, R., et al. 2014. Mol. Pharmacol.85, 858.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable