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| ln Vitro |
As a strong and targeted positive allosteric modulator of mGluR4, ADX88178 was created. The new radioligand ADX88178 is used to image the metabotropic glutamate receptor subtype 4 (mGluR4). With an EC50 value of 4 nM, ADX88178 increases glutamate-mediated activation of human mGluR4. Other mGluRs (EC50 > 30 μM) are not significantly affected by ADX88178 [1]. A new powerful, specific, and brain-penetrating mGlu4 positive allosteric modulator is ADX88178. After 30 minutes of pretreatment with 1, 10, or 100 nM ADX88178 or 100 nM LAP4, microglia were exposed to LPS during 24 hours. The culture supernatant was then removed for TNFα level determination using ELISA. The pretreatment of ADX88178 and LAP4 both considerably reduced the levels of TNFα generated by LPS. TNFα can be inhibited by ADX88178 at concentrations of only 1 nM, and it works just as well at 10 and 100 nM [2].
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| ln Vivo |
In mice, ADX88178 (1-30 mg/kg po) dose-dependently enhanced the number of open-arm entries. Specifically, the number of open-arm entries rose 5-fold, 7-fold, and almost 13-fold at 3, 10, and 30 mg/kg ADX88178, respectively, compared to vehicle-treated controls. Furthermore, ADX88178 dose-dependently enhanced arm open time. Specifically, the time spent opening the arms increased 8-fold, 12-fold, and 24-fold at 3, 10, and 30 mg/kg ADX88178 compared to vehicle-treated controls. In rats, ADX88178 (10-100 mg/kg po) dose-dependently enhanced the number of open-arm entries in the rat EPM test. Specifically, the number of open-arm entry rose by more than 5-fold, 8-fold, and 10-fold at 10, 30, and 100 mg/kg ADX88178, respectively, compared to vehicle-treated controls. Furthermore, ADX88178 dose-dependently enhanced arm open time. Specifically, arm open time increased 7.5-, 11-, and 13-fold at 10, 30, and 100 mg/kg ADX88178 compared to vehicle-treated controls [3].
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| References |
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| Molecular Formula |
C12H12N6S
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|---|---|
| Molecular Weight |
272.328879356384
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| Exact Mass |
272.084
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| CAS # |
1235318-89-4
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| PubChem CID |
46836872
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| Appearance |
White to off-white solid powder
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| LogP |
2.756
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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 |
3
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| Heavy Atom Count |
19
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| Complexity |
304
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MIQNXKWDQRNHAU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12N6S/c1-7-3-4-13-11(16-7)18-12-17-10(8(2)19-12)9-5-14-15-6-9/h3-6H,1-2H3,(H,14,15)(H,13,16,17,18)
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| Chemical Name |
5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine
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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 : ~16.67 mg/mL (~61.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.13 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 16.7 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6720 mL | 18.3601 mL | 36.7202 mL | |
| 5 mM | 0.7344 mL | 3.6720 mL | 7.3440 mL | |
| 10 mM | 0.3672 mL | 1.8360 mL | 3.6720 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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