| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
Kelatorphan targets enkephalin-degrading enzymes, which are responsible for the breakdown of endogenous enkephalins. It is a full inhibitor of these enzymes. By inhibiting enkephalin degradation, Kelatorphan increases the concentration of intact enkephalins at opioid receptors. This mechanism enhances opioid signaling and has been studied for its analgesic effects and effects on opioid peptide physiology.
|
|---|---|
| ln Vitro |
Kelatorphan is a potent inhibitor of enkephalin-degrading enzymes in vitro. It effectively prevents the breakdown of enkephalins, leading to increased levels of intact enkephalins. The compound's ability to inhibit enkephalin degradation makes it a valuable tool for studying opioid peptide physiology and analgesia mechanisms. Specific in vitro data, including IC50 values, are not extensively provided.
|
| ln Vivo |
Kelatorphan (50 μg) alone resulted in a large increase in intact [3H]enkephalin, corresponding to 80 ± 11% of the total recovered radioactivity [2]. In normally awake rats, Kelatorphan (10±20 mg/kg iv) increases minute ventilation. The increase in ventilation is due to a dose-dependent increase in respiratory rate. In arthritic rats, kelafen (20 mg/kg iv) increased ventilation without significant differences between arthritic and non-arthritic rats. Kelatorphan (20 mg/kg, n=6) also produced a slight (116%) but significant increase in respiration in pentobarbital-anesthetized rats 10±15 minutes after administration. Low-dose naloxone pretreatment (0.2 mg/kg iv, 15 minutes before Kelatorphan) did not antagonize the effects of Kelatorphan, but larger doses (1 mg/kg) significantly antagonized Kelatorphan (20 mg/kg) at 5 hours. Keep the rat awake for 10 minutes [3].
In vivo, Kelatorphan alone (50 µg) results in a strong increase of intact enkephalin levels. This demonstrates the compound's ability to inhibit enkephalin degradation in vivo. By increasing enkephalin levels, Kelatorphan enhances opioid signaling and has been studied for its analgesic effects. Specific in vivo efficacy data, including detailed dosing regimens and animal models, are not extensively provided. |
| Enzyme Assay |
In vitro enzyme assays for Kelatorphan involve measuring enkephalin-degrading enzyme activity. Enzyme preparations (e.g., from brain membranes) are incubated with enkephalin substrates and varying concentrations of Kelatorphan. Enkephalin degradation is quantified by HPLC or by measuring the release of degradation products. IC50 values are calculated from concentration-response curves.
|
| Cell Assay |
For in vitro cell-based assays, neuronal cells or brain slices are cultured and treated with Kelatorphan at various concentrations. Enkephalin levels are measured by ELISA or HPLC. Opioid receptor signaling is assessed by measuring cAMP accumulation or other downstream signaling pathways. Cell viability is assessed using standard assays.
|
| Animal Protocol |
In vivo animal studies for Kelatorphan typically use rodent models to assess analgesia and opioid signaling. The compound is administered intracerebroventricularly or systemically at doses determined from pharmacokinetic studies. Enkephalin levels are measured in brain tissues by HPLC or ELISA. Analgesic effects are assessed using standard pain tests (e.g., tail-flick, hot plate).
|
| ADME/Pharmacokinetics |
Kelatorphan has a molecular formula of C14H18N2O5 and a molecular weight of 294.30. It is a full inhibitor of enkephalin-degrading enzymes. Detailed solubility, stability, and storage conditions are not extensively provided in the available literature. Detailed pharmacokinetic parameters are not extensively characterized.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for Kelatorphan are not extensively provided in the available literature. As an inhibitor of enkephalin degradation, it would be expected to have a safety profile related to enhanced opioid signaling. The compound is for research use only and is not for human or clinical use. Standard toxicology assessments would be required for therapeutic development.
|
| References |
[1]. Waksman G, et al. Kelatorphan: a full inhibitor of enkephalin degrading enzymes. Biochemical and pharmacological properties, regional distribution of enkephalinase in rat brain by use of a tritiated derivative. Neuropeptides. 1985 Feb;5(4-6):529-32.
[2]. Waksman G, et al. In vitro and in vivo effects of kelatorphan on enkephalin metabolism in rodent brain. Eur J Pharmacol. 1985 Nov 5;117(2):233-43. [3]. Boudinot E, et al. Effects of the potent analgesic enkephalin-catabolizing enzyme inhibitors RB101 and kelatorphan on respiration. Pain. 2001 Feb 1;90(1-2):7-13. |
| Additional Infomation |
Kelatorphan is a potent, full inhibitor of enkephalin-degrading enzymes. It effectively prevents the breakdown of endogenous enkephalins, leading to increased levels of intact enkephalins and enhanced opioid signaling. The compound is used as a research tool to study opioid peptide physiology, analgesia mechanisms, and the interaction between opioid signaling pathways. No approved therapeutic status is reported.
|
| Molecular Formula |
C14H18N2O5
|
|---|---|
| Molecular Weight |
294.30312
|
| Exact Mass |
294.122
|
| CAS # |
92175-57-0
|
| PubChem CID |
123982
|
| Appearance |
White to off-white solid powder
|
| Density |
1.301g/cm3
|
| Index of Refraction |
1.567
|
| LogP |
1.111
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
21
|
| Complexity |
380
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O=C(C[C@H](C(N[C@@H](C)C(O)=O)=O)CC1=CC=CC=C1)NO
|
| InChi Key |
OJCFZTVYDSKXNM-GXSJLCMTSA-N
|
| InChi Code |
InChI=1S/C14H18N2O5/c1-9(14(19)20)15-13(18)11(8-12(17)16-21)7-10-5-3-2-4-6-10/h2-6,9,11,21H,7-8H2,1H3,(H,15,18)(H,16,17)(H,19,20)/t9-,11+/m0/s1
|
| Chemical Name |
(2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]propanoic acid
|
| 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 : ~100 mg/mL (~339.79 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.49 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 25.0 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: ≥ 2.5 mg/mL (8.49 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 25.0 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: ≥ 2.5 mg/mL (8.49 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 | 3.3979 mL | 16.9895 mL | 33.9789 mL | |
| 5 mM | 0.6796 mL | 3.3979 mL | 6.7958 mL | |
| 10 mM | 0.3398 mL | 1.6989 mL | 3.3979 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
