| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
Lobenzarit is associated with multiple human targets including the estrogen receptor (ESR1), glucocorticoid receptor (NR3C1), progesterone receptor (PGR), and various adrenergic, serotonin, dopamine, and histamine receptors, suggesting a complex polypharmacological profile. Its immunomodulatory effects are mediated through actions on T lymphocyte subsets, particularly regulatory and helper T cells.
|
|---|---|
| ln Vitro |
Lobenzarit demonstrates antioxidant properties by inhibiting chemiluminescence generated by reactive oxygen species. The disodium salt form (Lobenzarit sodium) has an IC50 of 1.6 μM for inhibiting peroxide-induced chemiluminescence. These in vitro activities contribute to its anti-inflammatory and immunomodulatory effects observed in cellular systems.
|
| ln Vivo |
In animal models, Lobenzarit prevents autoimmune kidney disease in hybrid mice. In Sprague-Dawley rats, administration via intraperitoneal injection at doses of 10 and 50 mg/kg once daily for 7 days demonstrated anti-arthritic effects; however, no therapeutic effect was observed in T lymphocyte-depleted arthritic rats, confirming its immunomodulatory mechanism depends on functional T cells.
|
| Enzyme Assay |
Typical non-cell-based binding assays for Lobenzarit involve radioligand displacement studies using membrane preparations from cells expressing specific receptors (e.g., estrogen receptor, glucocorticoid receptor). Test compounds are incubated with receptor-containing membranes and a known radiolabeled ligand; binding affinity is determined by measuring the concentration required to displace 50% of the bound radioligand (IC50). Assays are performed in buffer systems at physiological pH, with incubation times optimized for equilibrium binding, followed by filtration or centrifugation to separate bound from free ligand.
|
| Cell Assay |
In vitro cellular assays for Lobenzarit typically utilize immune cell lines or primary lymphocytes to assess immunomodulatory activity. Cells are cultured in RPMI-1640 medium supplemented with fetal bovine serum and antibiotics. Following treatment with Lobenzarit at various concentrations (typically 0.3-300 μM) for specified durations, endpoints such as cytokine production, T cell proliferation, or reactive oxygen species generation are measured. Chemiluminescence assays are commonly employed to quantify antioxidant activity in activated phagocytes or cell-free systems.
|
| Animal Protocol |
The primary in vivo animal model for Lobenzarit is the adjuvant-induced arthritis model in Sprague-Dawley rats. Animals are immunized with an appropriate adjuvant to induce arthritis, then treated with Lobenzarit via intraperitoneal injection at doses of 10-50 mg/kg once daily for 7 days. Disease severity is assessed by measuring paw swelling, joint inflammation scores, and histopathological examination of joint tissues. T lymphocyte depletion studies are performed to confirm the mechanism of action.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Lobenzarit are typical of small-molecule immunomodulators. The compound has a molecular weight of 291.68 g/mol for the free acid form and is administered via oral or intraperitoneal routes in preclinical studies. LogP is 5.1, indicating moderate lipophilicity. The disodium salt form has improved aqueous solubility, with a melting point of 388°C (dec.) and boiling point of 481°C. Detailed PK parameters such as half-life, bioavailability, and volume of distribution are not extensively reported in the available literature.
|
| Toxicity/Toxicokinetics |
Toxicological data for Lobenzarit are primarily derived from preclinical animal studies. The compound is supplied as a high-purity research reagent (>98%) for laboratory use only. In animal models, it is generally well-tolerated at therapeutic doses, though no specific LD50 values or detailed toxicity profiles are provided in the available sources. Standard safety pharmacology assessments would include evaluation of hematological parameters, hepatic and renal function, and histopathological examination of major organs.
|
| Additional Infomation |
Lobenzarit is an aminobenzoic acid.
Lobenzarit has an International Nonproprietary Name (INN) and is also known as Lobenzaritum. It is supplied as a research reagent for in vitro and in vivo studies investigating immunomodulation and anti-arthritic effects. The compound is structurally an aminobenzoic acid derivative with the molecular formula C14H10ClNO4. Its disodium salt (CAS 64808-48-6) is the form commonly used in research applications. |
| Molecular Formula |
C14H10NO4CL
|
|---|---|
| Molecular Weight |
291.6865
|
| Exact Mass |
291.029
|
| CAS # |
63329-53-3
|
| Related CAS # |
63329-53-3 (free);64808-48-6 (sodium);
|
| PubChem CID |
3946
|
| Appearance |
Light yellow to green yellow solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
481.0±45.0 °C at 760 mmHg
|
| Melting Point |
64-66 °C(lit.)
|
| Flash Point |
244.7±28.7 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.700
|
| LogP |
6.91
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
20
|
| Complexity |
376
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1C=C(C(O)=O)C(NC2C=C(Cl)C=CC=2C(O)=O)=CC=1
|
| InChi Key |
UGDPYGKWIHHBMB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H10ClNO4/c15-8-5-6-10(14(19)20)12(7-8)16-11-4-2-1-3-9(11)13(17)18/h1-7,16H,(H,17,18)(H,19,20)
|
| Chemical Name |
2-(2-carboxyanilino)-4-chlorobenzoic 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 (~342.83 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4283 mL | 17.1415 mL | 34.2830 mL | |
| 5 mM | 0.6857 mL | 3.4283 mL | 6.8566 mL | |
| 10 mM | 0.3428 mL | 1.7141 mL | 3.4283 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
