2. Metabolic Enzyme/Protease NF-κB PI3K/Akt/mTOR
  3. Endogenous Metabolite NF-κB Keap1-Nrf2 mTOR HIF/HIF Prolyl-Hydroxylase
  4. Cryptochlorogenic acid

Cryptochlorogenic acid  (Synonyms: 4-Caffeoylquinic acid; 4-O-Caffeoylquinic acid)

Cat. No.: HY-N0787 Purity: 99.87%
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Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response.

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

Cryptochlorogenic acid Chemical Structure

Cryptochlorogenic acid Chemical Structure

CAS No. : 905-99-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Cryptochlorogenic acid:

Cryptochlorogenic acid Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Cryptochlorogenic acid

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HIF-1α HIF

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response[1][2][3].

IC50 & Target

HIF-1α

 

In Vitro

Cryptochlorogenic acid (0-150 μM, 12, 24 or 48 h) shows low toxicity to RAW264.7 cells and does not significantly affect the viability of RAW264.7 cells at specific concentrations[2].
Cryptochlorogenic acid (20-80 μM, 2 h) can dose-dependent inhibit lipopolysaccharide (LPS: 1 μg/mL, 24 h) in RAW264.7 cells. induced the production of nitric oxide (NO), tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6), blocking the expression of iNOS, COX-2, TNF-α and IL-6[2].
Cryptochlorogenic acid (20-80 μM, 2 hours) inhibits the phosphorylation of IκB kinase (IKK), degrades I-κB, and reduces the nuclear translocation of NF-κB. At the same time, CCGA downregulates the phosphorylation level of MAPKs. Overall, CCGA effectively controls the expression of pro-inflammatory factors, thereby alleviating LPS-induced (1 μg/mL, 24 h) inflammation. It also promotes the nuclear translocation of Nrf2 to inhibit oxidative stress[2].
Cryptochlorogenic acid (1-200 μM, 48 hours) can effectively reduce the myocardial hypertrophy of H9c2 cells caused by ISO at a certain concentration. Cryptochlorogenic acid regulates the PI3Kα/Akt/mTOR/HIF-1α signaling pathway by significantly inhibiting the phosphorylation expression level of mTOR and over-expression of p-Akt and HIF-1α induced by ISO[3].

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

Cryptochlorogenic acid Related Antibodies

Western Blot Analysis[2]

Cell Line: RAW264.7 cells
Concentration: Cryptochlorogenic acid: 20-80 μM, LPS: 1 μg/mL
Incubation Time: Cryptochlorogenic acid: 2 h, LPS: 24 h
Result: Significantly inhibited the protein levels of iNOS, COX-2, IL-6, TNF-α and TLR4 in RAW264.7 macrophages stimulated by LPS.
Significantly inhibited the phosphorylation and degradation of IκB and the phosphorylation of IKKα/β induced by LPS.
Dose-dependent reduction of LPS-induced NF-κB(p65) transfer from cytoplasm to nucleus.
Significantly inhibited the phosphorylation of JNK1/2, ERK1/2, and p38 proteins induced by LPS.
significantly up-regulated Nrf2 protein levels in the nucleus and decreased NRF2 protein levels in the cytoplasm in a dose-dependent manner.

Cell Viability Assay[2]

Cell Line: RAW264.7 cells
Concentration: Cryptochlorogenic acid (CCGA) : 0-150 μM, LPS (HY-D1056) : 0-3 μg/ml
Incubation Time: 12, 24 or 48 h
Result: At doses of 150 μM and 100 μM, slight toxicity was shown to RAW264.7 cells with no significant decrease in cell viability.
RAW264.7 cells showed no toxicity after being treated with LPS at different concentrations for 12 hours. After being treated with LPS above 2 μg/ml for 24h, the cell viability decreased significantly.
Treated with 0-100 μM CCGA and 1 μg/ml LPS for 24 h, RAW264.7 cells had low toxicity and no significant effect on cell viability.

RT-PCR[3]

Cell Line: H9c2 Cells
Concentration: 1-200 μM
Incubation Time: 48 h
Result: Significantly decreased the expression levels of ANP, BNP and HIF-1α mRNA in H9c2 cells after ISO treatment.
In Vivo


Pharmacokinetic parameters of Cryptochlorogenic acid after intragastric administration of Cryptochlorogenic acid at three dosages[2]

Dose (mg/kg) Cmax (μg/L) tmax (h) t1/2 (h) AUC0-t (μg•h/L) AUC0-∞ (μg•h/L) MRT0-t (h) MRT0-∞ (h)
100 630 0.33 2.00 1938.91 1977.70 3.21 3.51
200 1270.09 0.47 1.97 3071.87 3179.41 3.23 3.39
400 2582.68 0.44 2.34 8825.32 9139.54 3.47 3.93

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

354.31

Formula

C16H18O9
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(/C=C/C1=CC(O)=C(O)C=C1)O[C@@H]([C@@H]2O)[C@@H](C[C@](C(O)=O)(O)C2)O
Structure Classification
Initial Source
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 : 50 mg/mL (141.12 mM; Need ultrasonic; 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 2.8224 mL 14.1119 mL 28.2239 mL
5 mM 0.5645 mL 2.8224 mL 5.6448 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.06 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (7.06 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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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

Purity: 99.87%

COA (249 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.8224 mL 14.1119 mL 28.2239 mL 70.5597 mL
5 mM 0.5645 mL 2.8224 mL 5.6448 mL 14.1119 mL
10 mM 0.2822 mL 1.4112 mL 2.8224 mL 7.0560 mL
15 mM 0.1882 mL 0.9408 mL 1.8816 mL 4.7040 mL
20 mM 0.1411 mL 0.7056 mL 1.4112 mL 3.5280 mL
25 mM 0.1129 mL 0.5645 mL 1.1290 mL 2.8224 mL
30 mM 0.0941 mL 0.4704 mL 0.9408 mL 2.3520 mL
40 mM 0.0706 mL 0.3528 mL 0.7056 mL 1.7640 mL
50 mM 0.0564 mL 0.2822 mL 0.5645 mL 1.4112 mL
60 mM 0.0470 mL 0.2352 mL 0.4704 mL 1.1760 mL
80 mM 0.0353 mL 0.1764 mL 0.3528 mL 0.8820 mL
100 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7056 mL
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Cryptochlorogenic acid 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:

Cryptochlorogenic acid905-99-74-Caffeoylquinic acid 4-O-Caffeoylquinic acidEndogenous MetaboliteNF-κBKeap1-Nrf2mTORHIF/HIF Prolyl-HydroxylaseNuclear factor-κBNuclear factor-kappaBMammalian target of RapamycinHypoxia-inducible factorsHIFsHIF-PHPhenolic acidAntioxidantAnti-inflammatoryCardiac hypertrophyInhibitorinhibitorinhibit

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