Mirogabalin besylate (DS 5565 besylate)
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1250 | Check With Us |
500mg | $1750 | Check With Us |
1g | $2625 | Check With Us |
Cat #: V25560 CAS #: 1138245-21-2 Purity ≥ 98%
Description: Mirogabalin besylate (DS-5565) is a potent, selective and orally bioavailable α2δ-1 ligand under development for treating pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia.
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Molecular Weight (MW) | 367.46 |
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Molecular Formula | C18H25NO5S |
CAS No. | 1138245-21-2 |
Synonyms | DS-5565; DS 5565; DS5565; A-2000700; A2000700; A 2000700 |
Protocol | In Vitro | Mirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively. Mirogabalin shows binding affinity for the gabapentin binding site in rat cortical brain homogenates with the IC50 value of 16.0 nM. Mirogabalin has no effect on any other receptors, channels, transporters, or enzymes at 50 μM |
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In Vivo | Mirogabalin besylate (3 and 10 mg/kg) markedly increases AUC0-8 hours values in a dose-dependent manner in partial sciatic nerve ligation model rats. Mirogabalin (2.5, 5, and 10 mg/kg) causes significant and dose-dependent increase in AUC0-12 hours values and enhances analgesic effects, with estimated ED50 of 4.4, 3.1, and <2.5 mg/kg on day 1, day 3, and day 5, respectively. Moreover, Mirogabalin besylate shows no obvious effect on rota-rod performance and locomotor activity at 3 and 10 mg/kg via oral administration, exhibits significant inhibition on rota-rod performance at 10, 30, and 100 mg/kg, and decreases locomotor activity at 30 and 100 mg/kg in rats |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.7214 mL | 13.6069 mL | 27.2138 mL | 54.4277 mL |
5mM | 0.5443 mL | 2.7214 mL | 5.4428 mL | 10.8855 mL |
10mM | 0.2721 mL | 1.3607 mL | 2.7214 mL | 5.4428 mL |
20mM | 0.1361 mL | 0.6803 mL | 1.3607 mL | 2.7214 mL |
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Method for preparing in vivo formulation:
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