| Size | Price | Stock | Qty |
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| ln Vitro |
MS7710 inhibited the firing frequency and burst activity of dopamine neurons in the ventral tegmental area (VTA) in brain slice electrophysiological experiments [1].
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| ln Vivo |
MS7710 (1–10 mg/kg; intraperitoneal injection; single dose) significantly reduced the hyperactive firing rate and burst firing activity of dopaminergic neurons in the ventral tegmental region of male chronically socially frustrated mice [2]. MS7710 (1 mg/kg; intraperitoneal injection; single dose) significantly reduced the hyperactive firing rate and burst firing activity of dopaminergic neurons in the ventral tegmental region of female chronically socially frustrated mice [2]. MS7710 (5 mg/kg; intraperitoneal injection; single dose) improved social interaction deficits and reward-related cognitive rigidity in both male and female chronically socially frustrated mice over a prolonged period (14 days) [2]. MS7710 (20 mg/kg; intraperitoneal injection; single dose) achieved a brain/plasma partition coefficient of 0.42 in unstressed male mice and 0.21 in unstressed female mice, indicating that its blood-brain barrier permeability is superior to that of silobrazine [2].
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| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 8 weeks old, susceptible model induced by chronic social frustration stress) [2]
Doses: 1 mg/kg; 10 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: Compared with baseline, the firing frequency and burst activity of dopaminergic neurons in the ventral tegmental area were significantly reduced in the 1 mg/kg dose group. Compared with baseline, the firing frequency and burst activity of dopaminergic neurons in the ventral tegmental area were also significantly reduced in the 10 mg/kg dose group. Animal/Disease Models:C57BL/6J (female, 8 weeks old, susceptible to chronic social frustration) [2] Doses: 1 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: Compared with baseline, the firing rate and burst activity of dopamine neurons in the ventral tegmental area were significantly reduced. Animal/Disease Models:C57BL/6J (male and female, 8 weeks old, susceptible mice induced by chronic social frustration stress) [2] Doses: 5 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: 14 days after injection, the social interaction rate of male susceptible mice increased significantly, and their performance on the probabilistic reversal reward learning task was also improved: compared with the saline control group, fewer training sessions were required to re-establish preference for the new 80% reward bar, and they showed a higher correct selection rate during the reversal phase. 14 days after injection, the social interaction rate of female susceptible mice increased significantly, and their performance on the probabilistic reversal reward learning task was also improved: compared with the saline control group, fewer training sessions were required to re-establish preference for the new 80% reward bar, and they showed a higher correct selection rate during the reversal phase. Animal/Disease Models:C57BL/6J (male and female, 8 weeks old, unstressed) [2] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: The brain/plasma partition coefficient (Kp) reached 0.42 in male mice and 0.21 in female mice, indicating that the blood-brain barrier permeability was significantly improved compared with the parent compound silobeladin. |
| References |
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| Molecular Formula |
C27H36N2O5
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|---|---|
| Molecular Weight |
468.59
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| CAS # |
3095336-10-7
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| Appearance |
Off-white to light yellow oil
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| SMILES |
COC1=CC=CC(OCCN2CCC[C@H](CN3C(CC(C=C(OC)C(OC)=C4)=C4CC3)=O)C2)=C1
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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 (~213.41 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 canAdd 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (10.67 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 canAdd 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. 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 | 2.1341 mL | 10.6703 mL | 21.3406 mL | |
| 5 mM | 0.4268 mL | 2.1341 mL | 4.2681 mL | |
| 10 mM | 0.2134 mL | 1.0670 mL | 2.1341 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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