| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Olorinab targets the cannabinoid receptor type 2 (CB2). It is a highly potent and selective CB2 agonist. It exhibits consistent single-digit nanomolar potency and full intrinsic efficacy across multiple species, with strong selectivity for CB2 over CB1 in both binding and functional assays. Olorinab also induces robust CB2 receptor internalization, supporting agonist-driven receptor recycling. By activating CB2, it modulates immune cell signaling and inflammatory responses.
|
|---|---|
| ln Vitro |
Comprehensive in vitro investigation of Olorinab (APD 371) (6) shows that Olorinab (APD 371) is selective for CB2 in terms of binding and functioning Higher than CB1 test, and that single-digit nanomolar potency and full intrinsic efficacy are maintained across all species evaluated. Additionally, in CHO cells expressing HA-tagged rat CB2, lorinab (APD 371) caused effective receptor internalization (about 106% compared to the CB1/2 agonist CP55,940), indicating that it may be able to drive agonist-driven receptor recycling as hypothesised [1].
In vitro, Olorinab is a highly potent, selective, and fully efficacious CB2 agonist with an EC₅₀ of 6.2 nM for hCB2. Profiling demonstrates consistent single-digit nanomolar potency and full intrinsic efficacy across multiple species, with strong selectivity for CB2 over CB1. It induces robust CB2 receptor internalization. Its effects on immune cell signaling and inflammatory responses have been characterized in cell-based assays. |
| ln Vivo |
At doses ≥3 mg/kg PO, olorinab (APD 371) considerably raises the paw withdrawal threshold (ED50=2.3 mg/kg). A single dosage of Olorinab (APD 371) (10 mg/kg PO) lowered the paw withdrawal threshold for up to 4 hours following delivery in a different experiment. Furthermore, it is possible that CB2 receptor activity mediates Olorinab's (APD 371) analgesic action [1].
In vivo, oral administration of Olorinab produces significant, sustained analgesic effects, increasing paw withdrawal thresholds in a CB2-dependent manner. It reduces chronic pain and inflammation-related symptoms without typical CB1-mediated psychoactive effects. Olorinab has been investigated for the treatment of chronic pain. Its efficacy in pain models highlights its value for pain and inflammation research. |
| Enzyme Assay |
The activity of Olorinab can be assessed using cell-based functional assays. Cells expressing human CB2 receptors are treated with varying concentrations of Olorinab, and the activation of downstream signaling (e.g., inhibition of cAMP production, activation of MAPK pathways) is measured. The EC₅₀ for receptor activation is determined from dose-response curves. Binding affinity and selectivity for CB2 over CB1 are assessed using radioligand binding assays.
|
| Cell Assay |
To evaluate the cellular effects of Olorinab, immune cells (e.g., macrophages, T cells) are treated with the compound. The modulation of cytokine production, chemotaxis, and other immune functions is assessed. CB2 receptor internalization is measured using fluorescently labeled receptor constructs or by flow cytometry. The compound's effects on cell signaling pathways are analyzed by Western blotting.
|
| Animal Protocol |
In vivo studies with Olorinab typically involve administration to animal models via oral routes. In models of chronic pain (e.g., neuropathic pain, inflammatory pain), the compound's analgesic effects are assessed by measuring paw withdrawal thresholds or other pain-related behaviors. Its effects on inflammation are evaluated by measuring inflammatory markers in tissues. Pharmacokinetic parameters, such as oral bioavailability and half-life, are also characterized.
|
| ADME/Pharmacokinetics |
Olorinab has a molecular formula of C₁₈H₂₃N₅O₃ and a molecular weight of 357.41 g/mol. Its CAS number is 1268881-20-4. The purity is typically ≥95%. It is a small molecule agonist of the CB2 receptor. It should be stored according to the manufacturer's instructions.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for Olorinab are not extensively detailed in the available literature. However, as a selective CB2 agonist, it is designed to avoid the psychoactive effects associated with CB1 receptor activation, which may contribute to a more favorable safety profile. As with all research compounds, standard safety precautions should be taken when handling Olorinab.
|
| References | |
| Additional Infomation |
Olorinab is being investigated in the clinical trial NCT03155945 (APD371: tolerability, pharmacokinetics, and efficacy in subjects with Crohn's disease and abdominal pain).
Olorinab (APD 371) is a highly potent, selective, and fully efficacious cannabinoid receptor type 2 (CB2) agonist. It is being investigated for the treatment of chronic pain and inflammation. Olorinab activates CB2 receptors to modulate immune cell signaling and inflammatory responses without typical CB1-mediated psychoactive effects. It is a research tool for studying the CB2 receptor and developing novel pain therapeutics. |
| Molecular Formula |
C18H23N5O3
|
|---|---|
| Molecular Weight |
357.406923532486
|
| Exact Mass |
357.18
|
| CAS # |
1268881-20-4
|
| PubChem CID |
60164925
|
| Appearance |
White to off-white solid powder
|
| LogP |
0.3
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
553
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
O=C(C1C2=C([C@H]3C[C@H]3C2)N(C2C=[N+](C=CN=2)[O-])N=1)N[C@H](CO)C(C)(C)C
|
| InChi Key |
ACSQLTBPYZSGBA-GMXVVIOVSA-N
|
| InChi Code |
InChI=1S/C18H23N5O3/c1-18(2,3)13(9-24)20-17(25)15-12-7-10-6-11(10)16(12)23(21-15)14-8-22(26)5-4-19-14/h4-5,8,10-11,13,24H,6-7,9H2,1-3H3,(H,20,25)/t10-,11-,13+/m0/s1
|
| Chemical Name |
(2S,4S)-N-[(2S)-1-hydroxy-3,3-dimethylbutan-2-yl]-9-(4-oxidopyrazin-4-ium-2-yl)-8,9-diazatricyclo[4.3.0.02,4]nona-1(6),7-diene-7-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~559.58 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (13.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (13.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (13.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
