| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Laquinimod-d5 targets the immune system as an immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. The parent compound Laquinimod reduces astrocyte NF-κB activation. As a carboxamide derivative, it modulates immune responses and has neuroprotective effects. The deuterated form is used as a labeled compound for pharmacokinetic and metabolic studies.
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| ln Vitro |
In vitro studies demonstrate that Laquinimod-d5 is the deuterium-labeled form of Laquinimod, which is a potent immunomodulator that prevents neurodegeneration and inflammation. Laquinimod reduces astrocyte NF-κB activation. The compound modulates immune responses in the central nervous system. Detailed in vitro activity data for the deuterated form are expected to be similar to the parent compound.
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| ln Vivo |
In vivo activity of Laquinimod-d5 is inferred from the parent compound Laquinimod, which is an orally available immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocyte NF-κB activation. The deuterated form is used for pharmacokinetic and metabolic studies. Detailed in vivo data for the deuterated form are not extensively documented.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Laquinimod-d5 is not applicable in the traditional sense, as the compound is an immunomodulator rather than a classical enzyme inhibitor. Binding studies may be performed to assess its interaction with immune cell receptors or signaling molecules. NF-κB activation assays in astrocytes can be used to evaluate the compound's immunomodulatory activity. Standard protocols include appropriate positive controls and vehicle controls.
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| Cell Assay |
In vitro cell-based assays for Laquinimod-d5 are conducted using immune cells or astrocytes to evaluate its immunomodulatory effects. Cells are treated with the compound at various concentrations, and NF-κB activation is measured using reporter assays or Western blot. Cytokine production is assessed by ELISA. Standard protocols include appropriate positive controls and vehicle controls.
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| Animal Protocol |
In vivo animal studies for Laquinimod-d5 would typically be conducted using mouse models of neurodegeneration or inflammation. Animals would be administered the compound orally, and efficacy would be evaluated by measuring inflammatory markers, neurodegeneration, and behavioral outcomes. The deuterated form is used for pharmacokinetic studies. Detailed in vivo protocols and efficacy data are not available from the search results.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Laquinimod-d5 include its use as a deuterium-labeled compound for research applications. The parent compound Laquinimod is orally available. The deuterated form has CAS number 1214267-09-0. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively documented. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicity information for Laquinimod-d5 is limited. As a research-use compound, standard safety precautions for handling should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
Laquinimod-d5 (ABR-215062-d5) is the deuterium-labeled form of Laquinimod, an orally available immunomodulator that prevents neurodegeneration and inflammation in the CNS. Laquinimod reduces astrocyte NF-κB activation. CAS 1214267-09-0. It is intended for research use only.
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| Exact Mass |
361.124
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|---|---|
| CAS # |
1214267-09-0
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| PubChem CID |
58046980
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
571
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1=C(C(=C(C(=C1[2H])[2H])N(CC)C(=O)C2=C(C3=C(C=CC=C3Cl)N(C2=O)C)O)[2H])[2H]
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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 (~276.37 mM; with sonication)
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| 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.) |
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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