Mirogabalin besylate

Research use only, not for human use.

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.

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.

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.

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.

DS-5565 | DS5565

GPCR/G Protein

Calcium Channel

Calcium Channel

Neurological Disease

Pain

1138245-21-2

367.46

C18H25NO5S

>98% (HPLC)

DMSO : 125 mg/mL 340.17 mM;

CCC1=CC2C(C1)CC2(CC(=O)O)CN.C1=CC=C(C=C1)S(=O)(=O)O

2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid compound with benzenesulfonic acid (1:1)

(-20℃)

With Ice Pack

≥ 2 years