| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| 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].
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| 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. |
| Molecular Formula |
C14H18N2O5
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|---|---|
| Molecular Weight |
294.30312
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| Exact Mass |
294.122
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| CAS # |
92175-57-0
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| PubChem CID |
123982
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| Appearance |
White to off-white solid powder
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| Density |
1.301g/cm3
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| Index of Refraction |
1.567
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| LogP |
1.111
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
21
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| Complexity |
380
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(C[C@H](C(N[C@@H](C)C(O)=O)=O)CC1=CC=CC=C1)NO
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| InChi Key |
OJCFZTVYDSKXNM-GXSJLCMTSA-N
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| 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
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| Chemical Name |
(2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]propanoic acid
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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 (~339.79 mM)
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| 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.
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