APD-371

Research use only, not for human use.

APD-371 (APD371, Olorinab)?is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM).

APD-371 (APD371, Olorinab)?is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.Pain Phase 2 Clinical.

A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed, and that Olorinab (APD 371) is highly selective for CB2 over CB1 in both binding and functional assays. Furthermore, Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling.

Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration. Seperately, the analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB2 receptors.

Olorinab | APD371 | APD 371

GPCR/G Protein

Cannabinoid Receptor

Cannabinoid Receptor

Neurological Disease

Pain

1268881-20-4

357.414

C18H23N5O3

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (559.58 mM)

O=C(C1=NN(C2=C[N+]([O-])=CC=N2)C3=C1C[C@@]4([H])[C@]3([H])C4)N[C@H](CO)C(C)(C)C

3-((4aS,5aS)-3-(((S)-1-hydroxy-3,3-dimethylbutan-2-yl)carbamoyl)-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazol-1-yl)pyrazine 1-oxide

(-20℃)

With Ice Pack

≥ 2 years