Cat. No.: HY-N6812

Karacoline

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Based on 1 Customer Validation

Karacoline is an orally active PPARγ activator and ERK/JNK MAPK inhibitor. Karacoline restricts ROS production, maintains mitochondrial membrane potential, and inhibits pulmonary cell apoptosis. Karacoline inhibits NF-κB pathway activation, reduces acetylation levels of p65 and the expression of MMP14 and MMP9, enhances the expression of type II collagen (collagen II) and aggrecan (aggrecan), and suppresses extracellular matrix degradation. In a mouse model of sepsis-induced acute lung injury, Karacoline alleviates lung injury, inhibits the release of IL-1β, IL-6 and TNF-α, increases the Bcl-2/BAX ratio, and reduces caspase 3 expression. Karacoline can be used in research related to acute lung injury and intervertebral disc degeneration.

For research use only. We do not sell to patients.

Purity: 99.58%
CAS No.: 39089-30-0
Formula: C₂₂H₃₅NO₄
Molecular Weight:377.52

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Karacoline Chemical Structure

CAS No.: 39089-30-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]

PPARγ

MMP9

MMP14

IL-1β

IL-6

Caspase 3

TNF-α

All NF-κB Isoforms :

All PPAR Isoforms :

All ERK Isoforms :

All JNK Isoforms :

All p38 MAPK Isoforms :

All MMP Isoforms :

All Interleukin Related Isoforms :

All Bcl-2 Family Isoforms :

All Caspase Isoforms :

All TNF Receptor Isoforms :

In Vitro

Karacoline (1.6 μM; 24 h) inhibits LPS (HY-D1056)-induced apoptosis of MH-S cells by reducing ROS production and maintaining the stability of mitochondrial membrane potential^[1].
Karacoline (1.6 μM; 24 h) upregulates the expression of PPARγ in LPS-stimulated MH-S cells, inhibits the JNK/ERK MAPK signaling pathway (excluding p38), and simultaneously suppresses the expression of MMP9^[1].
Karacoline (0.001-1000.0 μM; 24 h) has an IC₅₀ of 6.444 μM in primary rat nucleus pulposus cells, and Karacoline (1.25 μM; 0-3 days) partially reverses TNF-α-induced cytotoxicity in these cells^[2].
Karacoline (1.25-12.88 μM; 24 h) reverses TNF-α-induced changes in gene expression in primary rat nucleus pulposus cells, downregulates MMP-14 expression and upregulates type II collagen expression, while the 1.25 μM concentration also upregulates aggrecan expression^[2].
Karacoline (1.25-12.88 μM; 48 h) reverses TNF-α-induced extracellular matrix degradation in primary rat nucleus pulposus cells and increases aggrecan secretion; at the concentration of 1.25 μM, it also increases type II collagen secretion and reduces MMP-14 secretion^[2].
Karacoline (1.25-12.88 μM; 4 days) increases the levels of type II collagen and proteoglycan, and decreases the level of MMP-14, in primary rat nucleus pulposus cells treated with TNF-α^[2].
Karacoline (1.25 μM-12.88 μM; 24-48 h) reduces TNF-α-induced MMP-14 protein expression and inhibits the activation of the NF-κB pathway in primary rat nucleus pulposus cells by decreasing the acetylation level of p65^[2].
Karacoline (1.25-12.88 μM; 48 h) reduces TNF-α-induced apoptosis in primary rat nucleus pulposus cells^[2].

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

Apoptosis Analysis^[1]

Cell Line:

LPS-stimulated MH-S murine alveolar macrophages
Concentration:

1.6 μM
Incubation Time:

24 h
Result:

Attenuated LPS-induced apoptosis, as shown by reduced cleaved caspase-3 expression, increased Bcl-2/BAX ratio, and decreased proportion of apoptotic cells.
Reduced LPS-induced intracellular ROS fluorescence intensity.
Reversed LPS-mediated MMP loss (restored red/green fluorescence ratio).

ELISA Assay^[2]

Cell Line:

primary rat nucleus pulposus cells
Concentration:

0, 1.25, 12.88 μM+100 ng/mL TNF-α
Incubation Time:

24 h
Result:

Reduced MMP-14 expression and increased collagen II expression, with 1.25 μM also increasing aggrecan expression.

Western Blot Analysis^[2]

Cell Line:

primary rat nucleus pulposus cells
Concentration:

0, 1.25, 12.88 μM+100 ng/mL TNF-α
Incubation Time:

48 h
Result:

Reduced TNF-α-induced MMP-14 protein expression.

Immunofluorescence^[2]

Cell Line:

primary rat nucleus pulposus cells
Concentration:

0, 1.25, 12.88 μM+100 ng/mL TNF-α
Incubation Time:

4 days
Result:

Increased collagen II and aggrecan levels and reduced MMP-14 levels.

In Vivo

Karacoline (10-40 mg/kg; i.g.) protects against sepsis-induced acute lung injury in male C57BL/6 mice by improving survival, reducing pulmonary edema, barrier dysfunction, inflammation, and apoptosis, via PPARγ-associated inhibition of JNK/ERK MAPK signaling^[1].

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

Animal Model:

C57BL/6 (male, 6-8 weeks old, 20-25 g, sepsis-induced acute lung injury via CLP surgery)^[1]
Dosage:

10 mg/kg (survival monitoring); 20 mg/kg; 40 mg/kg (survival monitoring)
Administration:

i.g. (single dose for survival monitoring); i.g. (1 h before surgery and 12 h after surgery)
Result:

Improved 7-day survival of CLP-induced septic mice at 20 mg/kg and 10 mg/kg (40 mg/kg did not improve survival beyond 20 mg/kg).
Reduced lung wet-to-dry weight ratio at 20 mg/kg.
Decreased total protein and albumin levels in bronchoalveolar lavage fluid (BALF) at 20 mg/kg.
Lowered BALF concentrations of IL-1β, IL-6, and TNF-α at 20 mg/kg.
Reduced lung injury scores at 20 mg/kg.
Mitigated histopathological changes including alveolar disruption, interstitial edema, and inflammatory cell infiltration at 20 mg/kg.
Increased the Bcl-2/BAX ratio in lung tissue at 20 mg/kg.
Decreased cleaved-caspase-3 levels in lung tissue at 20 mg/kg.
Reduced BAX expression in lung tissue at 20 mg/kg.
Increased Bcl-2 expression in lung tissue at 20 mg/kg.
Lowered TUNEL-positive cell counts in lung tissue at 20 mg/kg.
Restored PPARγ mRNA and protein expression in lung tissue at 20 mg/kg.
Suppressed phosphorylation of JNK and ERK in lung tissue at 20 mg/kg.
Reduced MMP9 expression in lung tissue at 20 mg/kg.

Chemical Information

CAS No. 39089-30-0
Appearance Solid
Molecular Weight 377.52
Formula C₂₂H₃₅NO₄
Color White to off-white
SMILES

O[C@@H]1C23C4C([C@]5(O)[C@]6([H])[C@@]3([H])C[C@@]([C@@H](OC)C5)([H])[C@@H]6O)C[C@]2([H])[C@@](CN4CC)(C)CC1
Structure Classification
- Terpenoids
- Diterpenoids
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (66.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6489 mL

13.2443 mL

26.4887 mL

5 mM

0.5298 mL

2.6489 mL

5.2977 mL

10 mM

0.2649 mL

1.3244 mL

2.6489 mL

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lei Z, et al. Karacoline attenuates sepsis-induced acute lung injury by suppressing apoptosis via PPARγ-associated inhibition of JNK/ERK MAPK signaling. Respiratory research. 2026 Jun 15. [Content Brief]

[2]. Zhou X, et al. Karacoline, identified by network pharmacology, reduces degradation of the extracellular matrix in intervertebral disc degeneration via the NF-κB signaling pathway. Journal of pharmaceutical analysis. 2020 Feb;10(1):13-22. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6489 mL	13.2443 mL	26.4887 mL	66.2217 mL
	5 mM	0.5298 mL	2.6489 mL	5.2977 mL	13.2443 mL
	10 mM	0.2649 mL	1.3244 mL	2.6489 mL	6.6222 mL
	15 mM	0.1766 mL	0.8830 mL	1.7659 mL	4.4148 mL
	20 mM	0.1324 mL	0.6622 mL	1.3244 mL	3.3111 mL
	25 mM	0.1060 mL	0.5298 mL	1.0595 mL	2.6489 mL
	30 mM	0.0883 mL	0.4415 mL	0.8830 mL	2.2074 mL
	40 mM	0.0662 mL	0.3311 mL	0.6622 mL	1.6555 mL
	50 mM	0.0530 mL	0.2649 mL	0.5298 mL	1.3244 mL
	60 mM	0.0441 mL	0.2207 mL	0.4415 mL	1.1037 mL

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Karacoline

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

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Anti-Aging Compound Library

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All NF-κB Isoforms

All PPAR Isoforms

All ERK Isoforms

All JNK Isoforms

All p38 MAPK Isoforms

All MMP Isoforms

All Interleukin Related Isoforms

All Bcl-2 Family Isoforms

All Caspase Isoforms

All TNF Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Karacoline Related Classifications

HY-N6812 Related Classifications