1. GPCR/G Protein
  2. Cannabinoid Receptor

Olorinab (Synonyms: APD 371)

Cat. No.: HY-111110
Handling Instructions

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.

For research use only. We do not sell to patients.

Olorinab Chemical Structure

Olorinab Chemical Structure

CAS No. : 1268881-20-4

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.

IC50 & Target

EC50: 6.2 nM (hCB2)[1].

In Vitro

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[1].

In Vivo

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[1].

Clinical Trial
References
Molecular Weight

357.41

Formula

C₁₈H₂₃N₅O₃

CAS No.

1268881-20-4

SMILES

O=C(C1=NN(C(N=CC=2)=CN2=O)C3=C1C[[email protected]@]4([H])[[email protected]]3([H])C4)N[[email protected]](CO)C(C)(C)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Olorinab

Cat. No.: HY-111110