[CAS NO. 1268881-20-4] Olorinab
PRODUCTS SPECIFICATIONS [1268881-20-4]
DESCRIPTION [1268881-20-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 357.41 |
| Molecular Formula | C18H23N5O3 |
| SMILES | O=C(C1=NN(C(N=CC=2)=CN2=O)C3=C1C[C@@]4([H])[C@]3([H])C4)N[C@H](CO)C(C)(C)C |
Summary
Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB 2 ) agonist, with an EC 50 of 6.2 nM for hCB 2 .
IC50 & Target
EC50: 6.2 nM (hCB 2 ) [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 CB 2 over CB 1 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 CB 2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED 50 =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 CB 2 receptors [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04655599 | Arena Pharmaceuticals |
Irritable Bowel Syndrome
|
January 29, 2021 | Phase 1 |
| NCT04043455 | Arena Pharmaceuticals |
Irritable Bowel Syndrome
|
July 24, 2019 | Phase 2 |
| NCT03155945 | Arena Pharmaceuticals |
Crohn´s Disease|Abdominal Pain
|
July 19, 2017 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 200 mg/mL ( 559.58 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7979 mL | 13.9895 mL | 27.9791 mL |
| 5 mM | 0.5596 mL | 2.7979 mL | 5.5958 mL |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7979 mL |
Synonyms