2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. KCL-286

KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury.

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KCL-286 Chemical Structure

KCL-286 Chemical Structure

CAS No. : 1952276-71-9

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Based on 1 publication(s) in Google Scholar

KCL-286 Related Antibodies

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Description

KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury[1][3].

IC50 & Target

RAR α (EC50 = 26 nM);RAR β (EC50 = 1.9 nM);RAR γ (EC50 = 11 nM)[1]
Cellular Effect
Cell Line Type Value Description References
COS-7 EC50
1.9 nM
Compound: 10
Transactivation of GAL4-fused mouse RARbeta-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
Transactivation of GAL4-fused mouse RARbeta-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
[PMID: 30792038]
COS-7 EC50
13 nM
Compound: 10
Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
[PMID: 30792038]
COS-7 EC50
26 nM
Compound: 10
Transactivation of GAL4-fused mouse RARalpha-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
Transactivation of GAL4-fused mouse RARalpha-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
[PMID: 30792038]
HEK293 EC50
2.05 nM
Compound: 10
Transactivation of GAL4 DBD-fused human RARbeta-LBD expressed in HEK293 cells by beta-lactamase reporter gene based assay
Transactivation of GAL4 DBD-fused human RARbeta-LBD expressed in HEK293 cells by beta-lactamase reporter gene based assay
[PMID: 30792038]
In Vitro

KCL-286 (0.1 μM, 72 h) increases the neurite density and the number of synapses to a significant extent which activates RARβ2[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KCL-286 Related Antibodies
In Vivo

KCL-286 (3 mg/kg, p.o., every other days for 4 weeks) modulates various regenerative pathways as well as restoring ECM levels and cell adhesion molecules in the injured rat model[2].
KCL-286 (3 mg/kg, p.o., every other days for 4 weeks) improves the hind limb locomotor function in moderate thoracic SC contusion rat model[2].
KCL-286 (3 mg/kg, p.o., every other days for 4 weeks) achieves full locomotor and sensory recovery after 3 weeks in C5-T1 dorsal root avulsion rat model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Non-injured or avulsed male Sprague-Dawley rats[2]
Dosage: 3 mg/kg, every other days for 4 weeks
Administration: Oral gavage (p.o.)
Result: Resulted in 82 genes presenting a return to their basal level and 99 genes being strongly upregulated in injured model.
Resulted in 58 genes returning to their basal level after being significantly downregulated under injured conditions.
Significantly modified genes associated with ECM, paths within this signaling complex were both upregulated (those pertaining to the modulation of the cholinergic system, ion transport, and ion channels) or downregulated by the drug after injury.
Highly upregulated the ligand-gated ion channel.
Regulated the G-protein coupled receptor signaling cascades and G-protein coupled receptor protein pathways and chemokine signalling.
Upregulated RARβ in the cell bodies and axons of all neuron subtypes.
Animal Model: Moderate thoracic SC contusion male Sprague-Dawley rat model[2]
Dosage: 3 mg/kg, every other days for 4 weeks
Administration: Oral gavage (p.o.)
Result: Significantly reduced the tissue loss that progressively occurs at sub-acute and chronic stages following the injury.
Significantly reduced gliosis, shown by reduction in OX42 expression and neuronal loss assessed by neuronal nuclear protein (NeuN) levels.
Significantly lowered the expression of reactive astrocytes Glial fibrillary acidic protein and microglia Ionized Calcium Binding Adaptor Molecule 1.
Significantly upregulated decorin expression and lowered CSPGs in contused rats.
Molecular Weight

334.33

Formula

C19H14N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=C(C)C2=C1OC(C3=NC(C4=CC=C(C(O)=O)C=C4)=NO3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (18.69 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9911 mL 14.9553 mL 29.9106 mL
5 mM 0.5982 mL 2.9911 mL 5.9821 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.62 mg/mL (1.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9911 mL 14.9553 mL 29.9106 mL 74.7764 mL
5 mM 0.5982 mL 2.9911 mL 5.9821 mL 14.9553 mL
10 mM 0.2991 mL 1.4955 mL 2.9911 mL 7.4776 mL
15 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9851 mL
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KCL-286 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KCL-2861952276-71-9C286KCL286KCL 286C 286C-286RAR/RXRRetinoic acid receptorsRetinoid X receptorsNeuronsinjuryaxonal regenerationspinalneuroinflammationInhibitorinhibitorinhibit

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