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| Targets |
Tedalinab targets the cannabinoid receptor 2 (CB2), a G protein-coupled receptor that is primarily expressed in immune cells and peripheral tissues. It is a potent and selective CB2 agonist with more than 4700-fold selectivity over CB1. By activating CB2 receptors, Tedalinab modulates immune cell function and inflammatory responses. The CB2 receptor is a promising target for anti-inflammatory and analgesic therapies.
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| ln Vitro |
Tedalinab demonstrates potent and selective CB2 agonist activity in vitro. It is more than 4700 times more selective for CB2 than CB1. This high selectivity suggests that Tedalinab may have reduced psychoactive side effects compared to non-selective cannabinoid agonists. Specific in vitro data, including EC50 values and detailed assay conditions, are not extensively provided in the available literature.
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| ln Vivo |
Tedalinab has been investigated for its anti-inflammatory and analgesic properties in vivo. It has potential for treating neuropathic pain and osteoarthritis. As a CB2 agonist, it modulates immune cell function and reduces inflammation. Specific in vivo efficacy data, including dosing regimens, animal models, and detailed results, are not extensively provided in the available literature.
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| Enzyme Assay |
In vitro receptor binding and functional assays for Tedalinab involve measuring affinity and activity at CB2 and CB1 receptors. Membrane preparations from cells expressing human recombinant CB2 or CB1 receptors are incubated with radiolabeled ligands and varying concentrations of Tedalinab. Receptor activation is measured by assessing downstream signaling pathways, such as cAMP accumulation. Ki and EC50 values are calculated.
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| Cell Assay |
For in vitro cell-based assays, cells expressing CB2 receptors are cultured and treated with Tedalinab at various concentrations. Receptor activation is measured by assessing cAMP accumulation or other downstream signaling pathways. Anti-inflammatory effects are assessed by measuring cytokine production in immune cells. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo animal studies for Tedalinab typically use rodent models of pain and inflammation. The compound is administered orally at doses determined from pharmacokinetic studies. Pain behaviors are assessed using standard tests (e.g., mechanical allodynia, thermal hyperalgesia). Inflammatory markers are measured in plasma or tissue homogenates. Histological examination of tissues assesses the extent of inflammation and tissue damage.
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| ADME/Pharmacokinetics |
Tedalinab has a molecular formula of C19H21F2N3O. It is an orally bioactive small molecule. Detailed pharmacokinetic parameters (absorption, distribution, metabolism, excretion, half-life, bioavailability) are not extensively characterized in the available literature. The compound is for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Tedalinab are not extensively provided in the available literature. As a CB2 agonist, it would be expected to have a safety profile related to modulation of the endocannabinoid system. The compound's high selectivity for CB2 over CB1 suggests a reduced risk of central nervous system side effects. Standard toxicology assessments would be required for therapeutic development.
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| References | |
| Additional Infomation |
Tedalinab (GRC-10693) is an effective and selective cannabinoid receptor 2 (CB2) agonist. It is more than 4700 times more selective for CB2 than CB1. It has been investigated for its anti-inflammatory and analgesic properties, with potential for treating neuropathic pain and osteoarthritis. The compound is orally bioactive. No approved therapeutic status is reported.
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| Molecular Formula |
C19H21F2N3O
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|---|---|
| Molecular Weight |
345.3938
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| Exact Mass |
345.165
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| CAS # |
916591-01-0
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| PubChem CID |
67029278
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| Appearance |
White to off-white solid powder
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| LogP |
4.618
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
537
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)(C)NC(=O)C1=NN(C2=C1[C@H]3CC[C@@H]2C3)C4=C(C=C(C=C4)F)F
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| InChi Key |
NTPZXHMTJGOMCJ-WDEREUQCSA-N
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| InChi Code |
InChI=1S/C19H21F2N3O/c1-19(2,3)22-18(25)16-15-10-4-5-11(8-10)17(15)24(23-16)14-7-6-12(20)9-13(14)21/h6-7,9-11H,4-5,8H2,1-3H3,(H,22,25)/t10-,11+/m0/s1
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| Chemical Name |
(1R,7S)-N-tert-butyl-3-(2,4-difluorophenyl)-3,4-diazatricyclo[5.2.1.02,6]deca-2(6),4-diene-5-carboxamide
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| Synonyms |
GRC10693; GRC 10693; GRC-10693
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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 |
| 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 : ~100 mg/mL (~289.53 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8953 mL | 14.4764 mL | 28.9528 mL | |
| 5 mM | 0.5791 mL | 2.8953 mL | 5.7906 mL | |
| 10 mM | 0.2895 mL | 1.4476 mL | 2.8953 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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