| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ADX88178 (30 nM-3 μM) TFA effectively enhanced glutamate-mediated calcium mobilization in HEK293 cells expressing hmGluR4, with an EC50 of 3.5 nM, and did not have intrinsic agonist activity [2]. ADX88178 TFA also enhanced glutamate-mediated calcium mobilization in HEK293 cells expressing rat mGluR4, with an EC50 of 9.1 nM, and did not have intrinsic agonist activity [2]. ADX88178 TFA had different levels of inhibitory effects on cytochrome P450 enzymes, with the strongest inhibitory activity against CYP1A2 (IC50 = 0.46 μM) and the weakest inhibitory activity against CYP2D6 (IC50 > 50 μM) [2]. ADX88178 (1000 ng/mL) TFA has low plasma protein binding rate, with a free fraction of 8.1% in rat plasma and 21.5% in mouse plasma [2].
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|---|---|
| ln Vivo |
ADX88178 (10–30 mg/kg; orally; a single dose 30 minutes before administration of levodopa + benserazide) failed to alleviate established levodopa-induced abnormal involuntary movements (AIMs) in 6-hydroxydopamine-injured rats [1]. ADX88178 (0.1–10 mg/kg; orally) dose-dependently reversed haloperidol-induced rigidity in male Sprague-Dawley rats with an ED50 of 1.1 mg/kg, with significant efficacy observed at doses of 3 mg/kg and 10 mg/kg [2]. ADX88178 (3-30 mg/kg; orally; 10 mg/kg; intraperitoneally; 20-60 minutes before administration of levodopa or its carrier) alone failed to improve forelimb dyskinesia in male Sprague-Dawley rats with 6-OHDA damage, but it dose-dependently enhanced the efficacy of submaximal doses of levodopa and completely reversed the dyskinesia when 30 mg/kg ADX88178 was combined with 6 mg/kg levodopa [2].
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| Animal Protocol |
Animal/Disease Models:Sprague-Dawley mice (male, 270-300 g, 6-hydroxydopamine-induced, with stable AIMs induced beforehand by levodopa + benserazide) [1]
Doses: 10 mg/kg; 30 mg/kg Route of Administration: Oral; a single dose 30 minutes before levodopa + benserazide administration Experimental Results: No significant reduction in total AIMs scores compared to the solvent group. No significant effect on axial, forelimb, or oral AIMs subtypes. Animal/Disease Models:Sprague-Dawley mice (male, 260–450 g, haloperidol-induced ankylosing spondylitis) [2] Doses: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg Route of Administration: Oral Experimental Results: Ankylosing spondylitis was reversible in a dose-dependent manner. At a dose of 3 mg/kg, the latency of ankylosing spondylitis was reduced to 33.4 seconds (62.3% shorter than haloperidol alone). At a dose of 10 mg/kg, the latency of ankylosing spondylitis was reduced to 25.7 seconds (71.0% shorter than haloperidol alone). The ED50 for reversing ankylosing spondylitis was 1.1 mg/kg. The plasma EC50 reached 92 ng/mL (338 nM). Animal/Disease Models:Sprague-Dawley mice (male, 225-300 g, bilateral striatal 6-hydroxydopamine injury) [2] Doses: 3-30 mg/kg (oral); 10 mg/kg (intraperitoneal) Route of Administration: Oral; Intraperitoneal; Experimental Results: Oral administration of 3, 10 or 30 mg/kg alone had no significant effect on forelimb gait scores. Oral administration of 3 mg/kg in combination with 6 mg/kg levodopa increased forelimb steps to approximately 18. Oral administration of 10 mg/kg in combination with 6 mg/kg levodopa increased forelimb steps to approximately 23. Oral administration of 30 mg/kg in combination with 6 mg/kg levodopa completely reversed forelimb gait defects, and steps returned to pre-injury levels (approximately 35). Intraperitoneal injection of 10 mg/kg levodopa can enhance its efficacy, making 60 mg/kg levodopa (compared to 120 mg/kg levodopa alone) able to completely reverse motor inertia. |
| References |
|
| Molecular Formula |
C14H13F3N6O2S
|
|---|---|
| Molecular Weight |
386.35
|
| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CC1=C(C2=CNN=C2)N=C(NC3=NC=CC(C)=N3)S1.OC(C(F)(F)F)=O
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5883 mL | 12.9416 mL | 25.8833 mL | |
| 5 mM | 0.5177 mL | 2.5883 mL | 5.1767 mL | |
| 10 mM | 0.2588 mL | 1.2942 mL | 2.5883 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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