| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
KNT-127 targets the delta-opioid receptor (DOR), a G protein-coupled receptor that is a member of the opioid receptor family. It has selectivity for the delta receptor, with Ki values of 21.3 nM for the mu receptor, 0.16 nM for the delta receptor, and 153 nM for the kappa receptor. By binding to and activating DOR, KNT-127 modulates various physiological processes, including pain perception, mood, and neuroprotection.
|
|---|---|
| ln Vitro |
In vitro, KNT-127 is a potent and selective agonist of the delta-opioid receptor. Its activity is typically measured using receptor binding and functional assays. Receptor binding assays determine the compound's affinity (Ki) for DOR. Functional assays measure the activation of DOR-mediated signaling, such as the inhibition of cAMP accumulation or the activation of G protein-coupled inwardly rectifying potassium channels (GIRKs). These in vitro studies confirm KNT-127's potent and selective DOR agonist activity.
|
| ln Vivo |
In vivo, KNT-127 works effectively through systemic administration. As a selective DOR agonist, it has potential applications in studying pain, mood disorders, and neuroprotection. Unlike traditional opioids, KNT-127 may offer a different side-effect profile. However, specific in vivo protocols and results are not detailed in standard product descriptions.
|
| Enzyme Assay |
In vitro receptor binding assays for KNT-127 measure its affinity for the delta-opioid receptor. Membranes from cells expressing DOR are incubated with a radiolabeled DOR ligand and varying concentrations of KNT-127. The Ki is determined from competition binding curves. Selectivity is assessed by testing the compound against mu and kappa opioid receptors.
|
| Cell Assay |
In vitro cell-based assays for KNT-127 are used to study its effects on DOR-mediated signaling. Cells expressing DOR are treated with KNT-127, and the inhibition of cAMP accumulation is measured. The EC50 is determined from dose-response curves. These assays confirm the compound's agonist activity at the DOR.
|
| Animal Protocol |
In vivo animal experiments for KNT-127 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a DOR agonist would involve its administration to animal models of pain or mood disorders. However, specific protocols for KNT-127 are not detailed.
|
| ADME/Pharmacokinetics |
KNT-127 has a molecular weight of 372.46 g/mol and a molecular formula of C24H24N2O2. It has a CAS number of 1256921-89-7. It is a solid compound with a predicted density of 1.38 g/cm3. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized.
|
| Toxicity/Toxicokinetics |
Detailed toxicity data for KNT-127 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. KNT-127 is a selective DOR agonist, and its toxicity would be related to its effects on DOR-mediated signaling in normal tissues. As with all research chemicals, standard laboratory safety precautions should be followed.
|
| References |
|
| Additional Infomation |
KNT-127 is a research compound and is not approved for any clinical or therapeutic use. It is a potent, selective agonist of the delta-opioid receptor (DOR). It has selectivity for the delta receptor, with Ki values of 21.3 nM for mu, 0.16 nM for delta, and 153 nM for kappa opioid receptors. KNT-127 is a valuable research tool for studying the role of DOR in modulating pain, mood, and neuroprotection.
|
| Molecular Formula |
C24H24N2O2
|
|---|---|
| Molecular Weight |
372.459566116333
|
| Exact Mass |
372.1838
|
| CAS # |
1256921-89-7
|
| PubChem CID |
52942137
|
| Appearance |
Off-white to light yellow solid powder
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
28
|
| Complexity |
628
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
O[C@@]12CC3=CC4C=CC=CC=4N=C3C[C@@]31C1C=C(C=CC=1C[C@H]2N(C)CC3)O
|
| Synonyms |
KNT-127 KNT127 KNT 127
|
| 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 |
| 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 : ~25 mg/mL (~67.12 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.36 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 12.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6849 mL | 13.4243 mL | 26.8485 mL | |
| 5 mM | 0.5370 mL | 2.6849 mL | 5.3697 mL | |
| 10 mM | 0.2685 mL | 1.3424 mL | 2.6849 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
