| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| Other Sizes |
|
Purity: ≥98%
Zaltoprofen (CN 100; CN-100; CN100), a nonsteroidal anti-inflammatory drug (NSAID), is a potent inhibitor of COX-1 and COX-2 enzymes with potential anti-inflammatory activity. It has been approved for treatment of arthritis. It acts by binding to specific sites on the bradykinin B2 receptor. Zaltoprofen most potently inhibits bradykinin-enhancement of capsaicin-induced Ca2+ uptake into DRG neurons. Zaltoprofen also significantly inhibits bradykinin-induced 12-lipoxygenase (12-LOX) activity and the slow bradykinin-induced onset of substance P release from DRG neurons.
| ln Vitro |
In human platelets, thromboxane B2 generation is inhibited in a dose-dependent manner by Zaltoprofen (0.1-10 μM; 15 min)[1]. Zaltoprofen (0.01-1 μM; 30 min) decreases the synthesis of prostaglandin E2 by synovial cells activated by interleukin-1β[1]. The increase in [Ca2+]i in DRG cells caused by bradykinin is inhibited by zaltoprofen (0.1–1 μM; 5 min)[2].
|
|---|---|
| ln Vivo |
In rats, zaltoprofen (5–20 mg/kg; single po) suppresses nociceptive responses elicited by bradykinin[2]. In mice, acetic acid-induced writhing response is inhibited in a dose-dependent manner by Zaltoprofen (3-30 mg/kg; single po)[2].
|
| Animal Protocol |
Animal/Disease Models: Eightweeks old male Wistar rats were injected Bradykinin every 15 min[2]
Doses: 5, 10, 20 mg/kg Route of Administration: A single po Experimental Results: Inhibited bradykinin-induced nociceptive responses, with an ED50 of 9.7 mg/kg. The duration of analgesic effect was 60-90 min. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Zaltoprofen has known human metabolites that include (2S,3S,4S,5R)-3,4,5-trihydroxy-6-[2-(6-oxo-5H-benzo[b][1]benzothiepin-3-yl)propanoyloxy]oxane-2-carboxylic acid, Zaltoprofen S-oxide, and 10-hydroxy-zaltoprofen. |
| References |
|
| Additional Infomation |
Zaltoprofen is an organic molecular entity.
A non-steroidal anti-inflammatory drug approved for use in Japan in 1993. |
| Molecular Formula |
C17H14O3S
|
|
|---|---|---|
| Molecular Weight |
298.36
|
|
| Exact Mass |
298.066
|
|
| CAS # |
74711-43-6
|
|
| Related CAS # |
Zaltoprofen-13C,d3
|
|
| PubChem CID |
5720
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.3±0.1 g/cm3
|
|
| Boiling Point |
500.5±50.0 °C at 760 mmHg
|
|
| Melting Point |
129-131ºC
|
|
| Flash Point |
256.5±30.1 °C
|
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
|
| Index of Refraction |
1.656
|
|
| LogP |
3.68
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
4
|
|
| Rotatable Bond Count |
2
|
|
| Heavy Atom Count |
21
|
|
| Complexity |
422
|
|
| Defined Atom Stereocenter Count |
0
|
|
| InChi Key |
MUXFZBHBYYYLTH-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8,10H,9H2,1H3,(H,19,20)
|
|
| Chemical Name |
10,11-Dihydro-alpha-methyl-10-oxodibenzo(b,f)thiepin-2-acetic acid
|
|
| Synonyms |
|
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 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 (8.38 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 (8.38 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 | 3.3517 mL | 16.7583 mL | 33.5166 mL | |
| 5 mM | 0.6703 mL | 3.3517 mL | 6.7033 mL | |
| 10 mM | 0.3352 mL | 1.6758 mL | 3.3517 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03355638 | Completed | Drug: Aflibercept Injection [Eylea] Drug: Pranoprofen Eyedrops Drug: Omega-3 Supplementation |
Macular Edema | Università degli Studi di Brescia | January 2016 | Phase 4 |
| NCT01369238 | Unknown † | Device: Bee Venom Acupuncture Therapy
Drug: zaltoprofen |
Whiplash Injuries | Korean Pharmacoacupuncture Institute | June 2011 | Not Applicable |
| NCT03712670 | Completed | Drug: Aflibercept Drug: Pranoprofen Dietary Supplement: Carotenoids |
Retinal Disease | Università degli Studi di Brescia | January 1, 2016 | Not Applicable |
| NCT03013959 | Unknown † | Drug: Pranoprofen | Keratitis, Herpetic | Peking Union Medical College | November 2016 | |
| NCT01205958 | Unknown † | Procedure: acupuncture | Chronic Neck Pain状 | Kyunghee University Medical Center | December 2009 | Not Applicable |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA