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532583 TLR1/TLR2 Agonist II, CU-T12-9 - CAS 1821387-73-8 - Calbiochem

532583
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1821387-73-8C₁₇H₁₃F₃N₄O₂

Products

RéférenceConditionnement Qté
5325830001 Flacon en verre 10 mg
Description
OverviewA diphenyl substituted imidazole based compound that directly and selectively targets TLR1/2 and induces their dimerization and activates TLR1 & 2 signaling leading to NF-κB and AP-1 activation (KD = 182 and 478 nM, respectively; EC50 = 52.9 nM for TLR2 in HEK-Blue cells over-expressing hTLR2). Does not affect the dimerization of TLR2/TLR6 and exhibits poor affinity towards TLR3, TLR4, TLR5, TLR7 and TLR8. Shown to compete with Pam3CSK4 (Cat. No. 506350; Ki = 45.4 nM) for binding to TLR1/2 interface and enhance heterodimerization. Up-regulates the expression of TLR1, TLR2, TNFα, IL-10, and iNOS in RAW 264.7 macrophages in a time-dependent manner. Shown to be non-toxic up to 100 µM concentration.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number532583
Brand Family Calbiochem®
SynonymsN-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
References
ReferencesCheng, K., et al. 2014. Manuscript in preparation.
Product Information
CAS number1821387-73-8
FormYellow powder
Hill FormulaC₁₇H₁₃F₃N₄O₂
Chemical formulaC₁₇H₁₃F₃N₄O₂
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetTLR1/TLR2
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
5325830001 04055977241266

Documentation

TLR1/TLR2 Agonist II, CU-T12-9 - CAS 1821387-73-8 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Cheng, K., et al. 2014. Manuscript in preparation.

Brochure

Titre
NPI Flyer- Epigenetics and Nuclear Function Feature
New Products - Antibodies, Small Molecule, Inhibitors

Informations techniques

Titre
White Paper: Further considerations of antibody validation and usage.
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision19-December-2014 JSW
SynonymsN-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
DescriptionA 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.
FormYellow powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1821387-73-8
Chemical formulaC₁₇H₁₃F₃N₄O₂
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesCheng, K., et al. 2014. Manuscript in preparation.