| Size | Price | Stock | Qty |
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| 1mg |
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ST-2825 is novel, potent and specific MyD88 dimerization inhibitor which is neuroprotective after experimental traumatic brain injury in mice. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity. It significantly inhibited the proliferation of and promoted the apoptosis of HCC cells. Moreover, ST2825 significantly decreased bcl-2 expression, increased cleaved caspase-3 expression (P < 0.05), and reduced p65 nuclear expression (P < 0.05) in a dose-dependent manner. ST2825 inhibits the proliferation of and promotes the apoptosis of HCC cells, thereby suggesting that ST2825 may be a new drug for HCC treatment.
| ln Vitro |
IL-1R/TLR signaling is inhibited by ST2825 through disruption of MyD88 homodimerization. The inhibition of dimerization by ST2825 is concentration-dependent, with an estimated 40% inhibition at 5 μM and an approximate 80% inhibition at 10 μM [1].
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| ln Vivo |
ST2825 significantly inhibits IL-1β-stimulated IL-6 production at concentrations of 100 and 200 mg/kg [1]. After oral administration, ST2825 dose-dependently inhibited IL-1β-induced IL-6 production in treated mice. Animals were dosed orally with appropriate vehicle or ST2825 at doses of 50 to 200 mg/kg 5 min before intraperitoneal injection of 20 μg/kg IL-1β.
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| References |
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| Molecular Formula |
C27H28CL2N4O5S
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|---|---|
| Molecular Weight |
591.504
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| Exact Mass |
590.116
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| CAS # |
894787-30-5
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| Related CAS # |
894787-30-5;
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| PubChem CID |
24808138
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| Appearance |
White to off-white solid powder
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| LogP |
4.562
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
39
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| Complexity |
967
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C[C@]2(C[C@@H]3N(C2=O)[C@H](CCS3)C(=O)N)N(C1)C(=O)CC4=CC=C(C=C4)NC(=O)COC5=C(C=C(C=C5)Cl)Cl
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| InChi Key |
HBLHLJXFIPCEMW-ZJSFPPFMSA-N
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| InChi Code |
InChI=1S/C27H28Cl2N4O5S/c28-17-4-7-21(19(29)13-17)38-15-22(34)31-18-5-2-16(3-6-18)12-23(35)32-10-1-9-27(32)14-24-33(26(27)37)20(25(30)36)8-11-39-24/h2-7,13,20,24H,1,8-12,14-15H2,(H2,30,36)(H,31,34)/t20-,24-,27-/m1/s1
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| Chemical Name |
(4R,7R,8aR)-1'-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]-6-oxospiro[3,4,8,8a-tetrahydro-2H-pyrrolo[2,1-b][1,3]thiazine-7,2'-pyrrolidine]-4-carboxamide
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| Synonyms |
ST-2825 ST 2825 ST2825.
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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 : ~100 mg/mL (~169.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.23 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 25.0 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: ≥ 2.5 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6906 mL | 8.4531 mL | 16.9062 mL | |
| 5 mM | 0.3381 mL | 1.6906 mL | 3.3812 mL | |
| 10 mM | 0.1691 mL | 0.8453 mL | 1.6906 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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