| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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T6167923 (T-6167923) is a novel and potent inhibitor of MyD88-dependent signaling pathways with anti-inflammatory activity. It acts by binding to Toll/IL1 receptor (TIR) domain of MyD88 and disrupting the formation of MyD88 homodimer. T6167923 inhibits pro-inflammatory cytocines with IC50s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
| ln Vitro |
In peripheral blood mononuclear cells, T6167923 (0-500 μM; 20 h) suppresses the pro-inflammatory cytokine response to staphylococcal enterotoxin B (SEB) [2]. In HEK 293T cells, T6167923 (10-500 μM; 2 hours) suppresses the production of secreted alkaline phosphatase (SEAP) [2]. T6167923 (100 μM; 16 hours) decreases the inhibitory effect on MyD88 signaling by binding to TIR proteins [2]. T6167923 (1-500 μM; 13 hours) prevents the production of full-length MyD88 homodimers [2].
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| ln Vivo |
When mice are treated with SEB and LPS, T6167923 (0.17 and 1 mg; once intraperitoneally) shields them from toxicity [2].
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| Cell Assay |
Cell viability assay[2]
Cell Types: Peripheral blood mononuclear cells Tested Concentrations: 0-500 μM Incubation Duration: 20 hrs (hours) Experimental Results: SEB response to TNF-α, INF-γ, IL-6 and IL was dose-dependently attenuated - The IC50 of 1β in peripheral blood mononuclear cells were 2.66, 2.7, 2.66 and 2.9 μM, respectively. Cell viability assay [2] Cell Types: HEK 293T cell line Tested Concentrations: 10-500 μM Incubation Duration: 2 hrs (hours) Experimental Results: Dose-dependent inhibition of lipopolysaccharide (LPS)-induced MyD88-mediated NF-kB-driven SEAP in HEK 293T cells Expression IC50 range is 40–50 μM. Cell viability assay [2] Cell Types: HEK 293T cell line Tested Concentrations: 100 μM Incubation Duration: 16 hrs (hours) Experimental Results: TIR protein specifically targets MyD88 and reduces the inhibitory effect of MyD88 signaling in a dose-dependent manner. Western Blot Analysis[2] Cell Types: MyD88 knockout HEK 293-I3A Cell Tested Concentrations: 1-500 μM Incubation Duration: 13 hrs (hours) Experimental Results: Dose-dependent inhibition of TIR domain-mediated inhibition of full-length |
| Animal Protocol |
Animal/Disease Models: 16-20 weeks old BALB/c mouse LPS enhanced model [2]
Doses: 0.17 and 1 mg Route of Administration: intraperitoneal (ip) injection; 0.17 and 1 mg once Experimental Results: The therapeutic effect on SEB poisoning is dose-dependent. |
| References |
| Molecular Formula |
C17N3O3S2BRH20
|
|---|---|
| Molecular Weight |
458.393
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| Exact Mass |
457.012
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| CAS # |
2437475-16-4
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| Related CAS # |
2437475-16-4; 1090528-71-4
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| PubChem CID |
25648555
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| Appearance |
White to off-white solid powder
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| Density |
1.530±0.06 g/cm3(Predicted)
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
591
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H](C1=CC=CS1)NC(=O)N2CCN(CC2)S(=O)(=O)C3=CC(=CC=C3)Br
|
| InChi Key |
PNTQVMBKHCOLQD-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C17H20BrN3O3S2/c1-13(16-6-3-11-25-16)19-17(22)20-7-9-21(10-8-20)26(23,24)15-5-2-4-14(18)12-15/h2-6,11-13H,7-10H2,1H3,(H,19,22)/t13-/m0/s1
|
| Chemical Name |
4-(3-bromophenyl)sulfonyl-N-[(1S)-1-thiophen-2-ylethyl]piperazine-1-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~545.39 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1815 mL | 10.9077 mL | 21.8155 mL | |
| 5 mM | 0.4363 mL | 2.1815 mL | 4.3631 mL | |
| 10 mM | 0.2182 mL | 1.0908 mL | 2.1815 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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