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UNC-9995 is a novel and potent Dopamine D2 Receptor/Drd2 agonist. It inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration.
| ln Vitro |
After induction with IL-6 (300 ng/mL; 24 hours), UNC9995 (10 μM; 1 hour) restores primary astrocyte astrocytes and improves the binding of STAT3 and β-arrestin2. Additionally, it suppresses STING UNC9995 (1, 5, 10, and 20 μM; 1 hour), which when activated with IL-6 (300 ng/mL; 24 hours) can completely eradicate cellular inflammation as well as WT and Arrb2, TBK1, JAK [1].
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| ln Vivo |
In mice and rats, UNC9995 (2 mg/kg/day, i.p., for two weeks) ameliorates depressive-like behavioral phenotypes in the chronic unpredictable indoor (CUMS) and chronic social defeat daytime (CSDS) models.
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| Cell Assay |
Western Blot analysis [1]
Cell Types: primary astrocytes Tested Concentrations: 10 μM Incubation Duration: pre-incubation 1 h; -/− post-astrocytes [1]. Results of using 300 ng/mL IL-6: Enhanced interaction between STAT3 and β-arrestin2. Eliminate the activation of cGAS-STING and JAK/STAT3 pathways stimulated by IL-6, and reduce the levels of p-STING, p-TBK1, and p-JAK. |
| Animal Protocol |
Animal/Disease Models: Chronic Unpredictable Mild Stress (CUMS) Mouse Model[1]
Doses: 2 mg/kg/d Route of Administration: IP; improves the loss of star-shaped astrocytes in the hippocampus[1]. 2-week Experimental Results: Depressive-like symptoms of the CUMS mouse model were improved in WT mice but not in Arrb2−/− mice. |
| References |
| Molecular Formula |
C20H21CL2N3OS
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|---|---|
| Molecular Weight |
422.3712413311
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| Exact Mass |
421.078
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| CAS # |
1354030-52-6
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| PubChem CID |
56599143
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| Appearance |
White to off-white solid powder
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
467
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VBHBKXBUHHJVBZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21Cl2N3OS/c21-16-3-1-4-18(20(16)22)25-10-8-24(9-11-25)7-2-12-26-15-5-6-19-17(13-15)23-14-27-19/h1,3-6,13-14H,2,7-12H2
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| Chemical Name |
5-[3-[4-(2,3-dichlorophenyl)piperazin-1-yl]propoxy]-1,3-benzothiazole
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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 : ~50 mg/mL (~118.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.96 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 12.5 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 | 2.3676 mL | 11.8380 mL | 23.6759 mL | |
| 5 mM | 0.4735 mL | 2.3676 mL | 4.7352 mL | |
| 10 mM | 0.2368 mL | 1.1838 mL | 2.3676 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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