| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
RAR β2[1]
KCL-286 targets the retinoic acid receptor beta-2 (RARβ2), functioning as a potent and selective agonist. It has a reported EC₅₀ of 1.9 nM for RARβ2. Retinoic acid receptors are nuclear receptors that play important roles in development, differentiation, and neuroprotection. RARβ2 is a subtype of RAR that is particularly relevant in the central nervous system. By activating RARβ2, KCL-286 may promote neuroprotective and regenerative processes, making it a candidate for spinal cord injury research. |
|---|---|
| ln Vitro |
In vitro, KCL-286 demonstrates potent and selective RARβ2 agonist activity with an EC₅₀ of 1.9 nM. The compound's activity is assessed in cell-based reporter assays using RAR response element (RARE)-luciferase constructs. Its selectivity for RARβ2 over other RAR subtypes is confirmed through parallel assays. The compound's ability to activate RARβ2-mediated transcription and modulate the expression of RAR target genes is evaluated. KCL-286's potency and selectivity make it a valuable tool for studying RARβ2 biology.
|
| ln Vivo |
Specific in vivo activity data for KCL-286 are limited in the publicly available literature. As an orally active and brain-penetrant RARβ2 agonist, the compound has been investigated for the amelioration of spinal cord injury (SCI). Its ability to cross the blood-brain barrier makes it suitable for central nervous system applications. The compound may promote neuroprotection and functional recovery in SCI models. Further in vivo studies are needed to fully characterize its efficacy, safety, and therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for KCL-286 typically involve competitive binding experiments using RARβ2 protein and radiolabeled or fluorescently labeled retinoic acid as tracer. The compound's binding affinity to RARβ2 is assessed, with EC₅₀ values determined through dose-response experiments. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. The compound's agonist activity is confirmed through functional assays measuring RARE-mediated transcriptional activation.
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| Cell Assay |
In vitro cell-based assays for KCL-286 utilize cell lines expressing RARβ2 to assess its agonist activity. Cells are treated with varying concentrations of the compound for 24-48 hours. RARβ2-mediated transcriptional activity is evaluated using reporter gene assays with RARE-luciferase constructs. The expression of RAR target genes is measured by qPCR. Selectivity for RARβ2 over other RAR subtypes is confirmed through parallel assays. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
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| Animal Protocol |
In vivo animal studies with KCL-286 typically involve administration of the compound to rodent models of spinal cord injury (SCI). The compound is administered orally, leveraging its oral bioavailability. Endpoints include assessment of functional recovery using motor function scores, evaluation of neuroprotection and axonal regeneration, measurement of RAR target gene expression in spinal cord tissue, and pharmacokinetic profiling. The compound's brain-penetrant properties support its evaluation in CNS applications. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
KCL-286 is orally active and brain-penetrant. It has a molecular weight of 334.33 g/mol and a molecular formula of C₁₉H₁₄N₂O₄. Its chemical name is 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid. As a small molecule with favorable physicochemical properties, it has suitable characteristics for oral bioavailability and blood-brain barrier penetration. The compound is typically stored under conditions recommended for research chemicals.
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| Toxicity/Toxicokinetics |
KCL-286 is intended for research use only and is not approved for human therapeutic applications. As a research chemical, comprehensive toxicological data are not extensively documented in the publicly accessible literature. Standard safety precautions should be observed when handling this compound, including the use of appropriate personal protective equipment. As with all research chemicals, comprehensive toxicological profiling would be required before any consideration for clinical development.
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| References | |
| Additional Infomation |
Unii-N8lrs5gbb6 is an organic molecular entity.
KCL-286 (CAS#: 1952276-71-9) has a molecular formula of C₁₉H₁₄N₂O₄ and a molecular weight of 334.33 g/mol. Its chemical name is 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid. It is a potent, selective RARβ2 agonist with an EC₅₀ of 1.9 nM. The compound is orally active and brain-penetrant. It is used for the amelioration of spinal cord injury (SCI). This compound is not a drug and has not undergone clinical trials. |
| Exact Mass |
334.095
|
|---|---|
| CAS # |
1952276-71-9
|
| PubChem CID |
121414283
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
494
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C2C=C(OC2=C(C=C1)C)C3=NC(=NO3)C4=CC=C(C=C4)C(=O)O
|
| InChi Key |
AVCXUODHLRZJJP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H14N2O4/c1-10-3-4-11(2)16-14(10)9-15(24-16)18-20-17(21-25-18)12-5-7-13(8-6-12)19(22)23/h3-9H,1-2H3,(H,22,23)
|
| Chemical Name |
4-[5-(4,7-dimethyl-1-benzofuran-2-yl)-1,2,4-oxadiazol-3-yl]benzoic 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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