추천 제품
분석
≥98% (HPLC)
Quality Level
양식
powder
제조업체/상표
Calbiochem®
저장 조건
OK to freeze
protect from light
색상
yellow
solubility
DMSO: 50 mg/mL
저장 온도
2-8°C
SMILES string
FC(F)(F)c1ccc(cc1)c2nc[n](c2)c3c(ccc(c3)[N+](=O)[O-])NC
InChI
1S/C17H13F3N4O2/c1-21-14-7-6-13(24(25)26)8-16(14)23-9-15(22-10-23)11-2-4-12(5-3-11)17(18,19)20/h2-10,21H,1H3
InChI key
LITXVDAFEYLWQE-UHFFFAOYSA-N
일반 설명
A non-cytotoxic (up to 100 µM) diphenyl-substituted imidazole compound that exhibits high affinity toward both TLR1 & TLR2 (KD = 182 nM & 478 nM, respectively) and induces TLR1/2 heterodimerization, effectively completing against Pam3CSK4 (Cat. No. 506350) for TLR1/2 binding (Ki = 45.4 nM; [Pam3] = 20 mg/mL; [TLR1/2] = 80 nM). Shown to potently induce secreted embryonic alkaline phosphatase (SEAP) production from human TLR2-, but not TLR3-, 4-, 5-, 7-, 8-, transfected HEK293 (EC50 = 52.9 nM) in an NF-κB inhibitor Triptolide-(Cat. No. 645900) blockable manner via selective TLR1/2, but not TLR2/6, heterodimer activation. Reported to induce comparable NF-κB-dependent reporter transcription as 100 ng/mL Pam3CSK4 when administered to human macrophage U937 cultures at 5 µM concentration (24 h) and effectively trigger NO production in both murine Raw 264.7 and primary rat macrophage cultures (ECmax = 1.2 & 0.4 µM, respectively; 24 h), blockable by TLR1/2 antagonist CU-CPT22 (Cat. No. 614305), but not TLR4 antagonist TAK-242 (Cat. No. 614316 & 508336). Likewise, both CU-T12-9 and Pam3CSK4 (1 µM & 50 ng/mL, respectively) are demonstrated to induce similar time-dependent induction of TLR1, TLR2, TNF-α, iNOS, IL-10 mRNA in Raw 264.7 cells.
생화학적/생리학적 작용
Primary Target
TLR1/TLR2
TLR1/TLR2
Reversible: yes
경고
Toxicity: Standard Handling (A)
재구성
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
기타 정보
Cheng, K., et al. 2014. Manuscript in preparation.
법적 정보
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
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