| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| 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].
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| 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].
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| References | |
| Additional Infomation |
Olorinab is under investigation in clinical trial NCT03155945 (Tolerability, Pharmacokinetics, and Efficacy of APD371 in Subjects With Crohn's Disease Experiencing Abdominal Pain).
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| Molecular Formula |
C18H23N5O3
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|---|---|
| Molecular Weight |
357.406923532486
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| Exact Mass |
357.18
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| CAS # |
1268881-20-4
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| PubChem CID |
60164925
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| Appearance |
White to off-white solid powder
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| LogP |
0.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
553
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| Defined Atom Stereocenter Count |
3
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| 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
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| InChi Key |
ACSQLTBPYZSGBA-GMXVVIOVSA-N
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| 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
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| 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
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~559.58 mM)
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|---|---|
| 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.
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