STING-IN-5
Based on 1 Customer Validation
STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.89%
- CAS. Nr.: 2920064-17-9
- Formel: C47H67NO9S2
- Molecular Weight:854.17
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
In Vitro
STING-IN-5 (compound 30) (40 μM; 24 h) exhibits less effect on RAW264.7 cell viability[1].
STING-IN-5 (2.5 and 5 μM; 2 h) inhibits NO production in LPS-stimulated RAW264.7 with inhibition rate of 69.28 ± 2.36 and 78.66 ± 2.73 at 2.5 and 5 μM, respectively, and exhibits IC50 of 1.15 ± 0.15 μM[1].
STING-IN-5 (0.5-2 μM; 2 h) suppresses STING, as well as TBK1/IRF3/NF-κB activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7
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Concentration:40 μM
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Incubation Time:24 h
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Result:Exhibited less effect on RAW264.7 cell viability of 91.08 ± 1.09%
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Cell Line:RAW264.7 (stimulated by LPS for 6 h)
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Concentration:0.5, 1 and 2 μM
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Incubation Time:2 h
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Result:Significantly inhibited the protein expression of STING and the phosphorylation of the downstream targets TBK1, IRF3, p65, and IκB in a concentration-dependent manner.
In Vivo
Pharmacokinetic Parameters of STING-IN-5 in male Sprague-Dawley rats[1].
| Tmax (h) | Cmax (ng/mL) | AUC0-t (ng/mL·h) | AUC0-∞ (ng/mL·h) | T1/2 (h) | MRT0-t (h) | MRT0-∞ (h) |
| 1 | 66.52 | 81.08 | 135.7 | 1.11 | 0.99 | 2.02 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (6-8 weeks; acute liver injury induced by injection of 10 mg/kg LPS)[1]
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Dosage:1.25, 2.5, 5 mg/kg
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Administration:i.g.; once daily; for 3 days
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Result:Significantly improved pathological changes including disorderly arranged liver cells, blurred boundaries, congested hepatic sinusoids, swollen hepatocytes, a small number of hepatocytes were necrotic, and inflammatory cells infiltrated local areas.
Significantly reduced the levels of AST, ALT, and ALP (liver function specific indicators).
Chemical Information
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CAS. Nr. 2920064-17-9
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Appearance Solid
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Molecular Weight 854.17
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Formel C47H67NO9S2
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Color White to off-white
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SMILES
C[C@H]([C@H](OC(CCSSCCC(NOCC=C)=O)=O)CC[C@@]1([C@@]2([C@@H](C[C@]3(/C4=C(CC/C=C(C)/C)\C(OCC5=CC=CC=C5)=O)[H])O)[H])C)[C@@]1(CC[C@]2(C)[C@@]3(C)C[C@@H]4OC(C)=O)[H]
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (117.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1707 mL | 5.8536 mL | 11.7073 mL | 29.2682 mL |
| 5 mM | 0.2341 mL | 1.1707 mL | 2.3415 mL | 5.8536 mL | |
| 10 mM | 0.1171 mL | 0.5854 mL | 1.1707 mL | 2.9268 mL | |
| 15 mM | 0.0780 mL | 0.3902 mL | 0.7805 mL | 1.9512 mL | |
| 20 mM | 0.0585 mL | 0.2927 mL | 0.5854 mL | 1.4634 mL | |
| 25 mM | 0.0468 mL | 0.2341 mL | 0.4683 mL | 1.1707 mL | |
| 30 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9756 mL | |
| 40 mM | 0.0293 mL | 0.1463 mL | 0.2927 mL | 0.7317 mL | |
| 50 mM | 0.0234 mL | 0.1171 mL | 0.2341 mL | 0.5854 mL | |
| 60 mM | 0.0195 mL | 0.0976 mL | 0.1951 mL | 0.4878 mL | |
| 80 mM | 0.0146 mL | 0.0732 mL | 0.1463 mL | 0.3659 mL | |
| 100 mM | 0.0117 mL | 0.0585 mL | 0.1171 mL | 0.2927 mL |