Mirogabalin besylate

SKU: orb2655991

Description

Mirogabalin besylate (DS-5565) is a novel potent, selective ligand of the α2δ subunit of voltage-gated calcium channels with Kd of 13.5/22.7/27.0/47.6 nM for huamn α2δ-1, human α2δ-2, rat α2δ-1 and rat α2δ-2 subunits, respectively; exhibits a slower dissociation rate for the α2δ-1 subunit than the α2δ-2 subunit compared to pregabalin; shows more potent and longer lasting analgesic effects in experimental neuropathic pain models, partial sciatic nerve ligation rats and streptozotocin-induced diabetic rats; inhibits rota-rod performance and locomotor activity in rats.Pain Phase 3 Clinical.

Key Properties

• CAS Number: 1138245-21-2
• MW: 367.46
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₅NO₅S
• SMILES: CCC1=CC2C(C1)CC2(CC(=O)O)CN.C1=CC=C(C=C1)S(=O)(=O)O
• Target: Calcium Channel
• Solubility: DMSO : 125 mg/mL 340.17 mM

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DS-5565 | DS5565

Quick Database Links

Gene Symbol

Calcium Channel