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Clonixin

Alias: Deltar; lysine clonixinate; CLONIXIN; 17737-65-4; Clonixic acid; Clonixine; Clonixino; ...Clonixin
Cat No.:V18533 Purity: ≥98%
Clonixin (SCH-10304) is an orally bioactive NSAID.
Clonixin
Clonixin Chemical Structure CAS No.: 17737-65-4
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Clonixin (SCH-10304) is an orally bioactive NSAID.
Clonixin is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory properties. It is a potent inhibitor of cyclooxygenase (COX) enzymes, which are responsible for the production of prostaglandins. Clonixin is indicated for use in the management of chronic arthritic conditions and certain soft tissue disorders associated with pain and inflammation. It has been reported to block inward calcium currents. It has a molecular formula of C13H11ClN2O2 and a molecular weight of 262.69.
Biological Activity I Assay Protocols (From Reference)
Targets
Clonixin targets cyclooxygenase (COX) enzymes, which are responsible for the production of prostaglandins. It acts as an inhibitor, blocking the activity of COX enzymes. By inhibiting COX, it reduces the synthesis of prostaglandins, which are mediators of pain and inflammation. It also blocks inward calcium currents.
ln Vitro
In vitro, Clonixin is a potent inhibitor of COX enzymes. It blocks prostaglandin synthesis. It also blocks inward calcium currents. Its activity can be measured in enzyme assays using purified COX enzymes.
ln Vivo
In vivo, Clonixin is indicated for use in the management of chronic arthritic conditions and certain soft tissue disorders associated with pain and inflammation. It exhibits analgesic and anti-inflammatory properties. It is a non-steroidal anti-inflammatory drug.
Enzyme Assay
Clonixin is evaluated in cell-free enzymatic assays using purified COX-1 and COX-2 enzymes. The compound is incubated with the enzyme and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of COX inhibition.
Cell Assay
Clonixin is assessed in cell-based assays using immune cells or other cell types. Cells are treated with Clonixin, and the production of prostaglandins and other inflammatory mediators is measured. Its effects on cell viability and function are evaluated.
Animal Protocol
Clonixin is administered orally in animal models and in clinical settings to treat pain and inflammation. It is used in the management of chronic arthritic conditions and soft tissue disorders. Efficacy is assessed by measuring pain and inflammation.
ADME/Pharmacokinetics
Clonixin has a molecular weight of 262.69 and a molecular formula of C13H11ClN2O2. It has a CAS number of 17737-65-4. The compound is a solid. It should be stored under recommended conditions.
Toxicity/Toxicokinetics
No detailed toxicity data is available for Clonixin beyond its known use as an NSAID. It can cause gastrointestinal side effects. The compound is a therapeutic agent and is available by prescription only.
References

[1]. Anti-nociceptive Activity of Clonixin in Rhesus Monkeys. Jpn J Pharmacol. 1972 Dec;22(6):749-53.

[2]. Clonixin: A Clinical Evaluation of a New Oral Analgesic. J Clin Pharmacol New Drugs. Sep-Oct 1971;11(5):371-7.

Additional Infomation
Clonixin is a pyridine monocarboxylic acid, a compound in which nicotinic acid is substituted at the 2-position with a (2-methyl-3-chlorophenyl)amino group. It (in the form of a lysine salt) is used to treat renal colic, muscle pain, and moderate migraine attacks. It has a variety of pharmacological effects, including nonsteroidal anti-inflammatory drug (NSAID), nonnarcotic analgesic, antipyretic, platelet aggregation inhibitor, vasodilator, EC 1.14.99.1 (prostaglandin intraperoxidase) inhibitor, and lipoxygenase inhibitor. It is a pyridine monocarboxylic acid, an aminopyridine compound, and an organochlorine compound whose function is related to nicotinic acid. It is the conjugate acid of Clonixin (1-). Clonixin is a nonsteroidal anti-inflammatory drug. It is an anti-inflammatory analgesic. Drug Indications It is indicated for the treatment of chronic arthritis and certain soft tissue disorders associated with pain and inflammation. Mechanism of Action The mechanism of action of Clonixin appears not to have been studied at the molecular level. It is speculated that its mechanism of action is similar to other nonsteroidal anti-inflammatory drugs (NSAIDs), reducing prostaglandin production by inhibiting cyclooxygenases 1 and 2.
Pharmacodynamics
Clonicoxin is a nonsteroidal anti-inflammatory drug (NSAID) with a structure similar to [DB00586]. It has vasodilatory and analgesic effects.
Clonixin is also known as Clonixic acid and Chlonixin. It is a non-steroidal anti-inflammatory drug. The compound is a therapeutic agent.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H11CLN2O2
Molecular Weight
262.69
Exact Mass
262.05
CAS #
17737-65-4
PubChem CID
28718
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
410.2±45.0 °C at 760 mmHg
Melting Point
242 °C
Flash Point
201.9±28.7 °C
Vapour Pressure
0.0±1.0 mmHg at 25°C
Index of Refraction
1.665
LogP
5.09
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
3
Heavy Atom Count
18
Complexity
301
Defined Atom Stereocenter Count
0
SMILES
CC1=C(C=CC=C1Cl)NC2=C(C=CC=N2)C(=O)O
InChi Key
CLOMYZFHNHFSIQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H11ClN2O2/c1-8-10(14)5-2-6-11(8)16-12-9(13(17)18)4-3-7-15-12/h2-7H,1H3,(H,15,16)(H,17,18)
Chemical Name
2-(3-chloro-2-methylanilino)pyridine-3-carboxylic acid
Synonyms
Deltar; lysine clonixinate; CLONIXIN; 17737-65-4; Clonixic acid; Clonixine; Clonixino; ...Clonixin
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 Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~380.68 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.8068 mL 19.0338 mL 38.0677 mL
5 mM 0.7614 mL 3.8068 mL 7.6135 mL
10 mM 0.3807 mL 1.9034 mL 3.8068 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
Randomized Clinical Trial: Comparison of Lysine Clonixinate, Ketorolac and Metamizole Sodium in Poisoning by Scorpion Stings
CTID: NCT03943199
Phase: Not Applicable
Status: Completed
Date: 2019-07-20
A Comparative Study Between Lysine Clonixinate+Cyclobenzaprine and Caffeine+Carisoprodol+Sodium Diclofenac+Paracetamol
CTID: NCT01421433
Phase: Phase 3
Status: Unknown
Date: 2011-08-22
Intravenous Lysine Clonixinate for the Acute Treatment of Severe Migraine Attacks: A Double-Blind, Randomized, Placebo-Controlled Study
CTID: Not Applicable
Phase: Not Applicable
Status: Completed
Date: 2003-07-01
Treatment of Pain Associated to Knee Osteoarthritis in the Elderly: A Randomized Double-Blind Clinical Trial With Lysine Clonixinate
CTID: Not Applicable
Phase: Not Applicable
Status: Completed
Date: 2011-03-01
Analgesic Efficacy of Lysine Clonixinate, Paracetamol and Dipyrone in Lower Third Molar Extraction: A Randomized Controlled Trial
CTID: Not Applicable
Phase: Not Applicable
Status: Completed
Date: 2009-08-01
Comparison of the Effect of Lysine Clonixinate (Dolamin®) and Ibuprofen (Advil®) in Reducing Acute Pain Related to Tendinopathy in Patients
CTID: Not Applicable
Phase: Phase 4
Status: Completed
Date: 2014-09-16
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