| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 5g |
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| Other Sizes |
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Purity: ≥98%
| Targets |
5-Lipoxygenase (5-LO); TRPV1
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|---|---|
| ln Vitro |
Caffeic acid modulates histamine-induced reactions. When the concentration of light is increased from 0.1 to 1 mM, the modulatory impact of caffeic acid progressively increases, mimicking a normal dose-modulated response. Capsaicin-induced responses were considerably reduced in HEK293T-TRPV1 cells treated with 1 mM caffeine. Lower doses of caffeic acid inhibit capsaicin-induced reactions. Experiments have shown that caffeic acid can dramatically suppress histamine-sensitive dorsal root ganglion (DRG) neurons. The administration of caffeic acid (1 mM) reduced the percentage of DRG neurons responding to histamine application from 12.5% to 2.1%. The allyl isothiocyanate (AITC)-induced rise in intracellular calcium in TRPA1-expressing cells was thought to be considerably inhibited by 1 mM caffeic acid. Caffeic acid may also inhibit AITC-induced TRPA1 activation [1].
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| ln Vivo |
In the mouse model, histamine-induced scratching (30.50±10.87 times/1 hour, n=6) was seen when caffeic acid (500 mg/kg) was used. Furthermore, although there appeared to be a declining trend (49.40±12.35 times/1 h, n=5), the anti-scratch effect of a lower dose of caffeic acid (100 mg/kg) in histamine-induced scratching was not determined to be significant. Scratching caused by chlorine buffer can be considerably reduced by 500 mg/kg caffeic acid (161.6±31.42 times/1 h, n=5)[1]. In the hippocampal regions, caffeineic acid dramatically decreased 5-LO mRNA (P<0.01). The 5-LO protein expression in the I/R-caffeic acid group was significantly lower (P<0.05 or P<0.01) than in the potential reperfusion (I/R) untreated group. This was particularly true when comparing the I/R-caffeic acid and I/R untreated groups. The latency of finding the platform was significant throughout the process in both the low-dose and high-dose caffeic acid groups, and the entire platform latency was in I/R. Group R-caffeic acid (50 mg/kg). Hippocampal neuron nuclear pyknosis was dramatically reduced in the high-dose caffeic acid group, with a pyknosis rate of (13.3) ±3.0)%, while cell damage was still evident in the low-dose group (63.6±2.8)% [2].
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| Cell Assay |
Itch is an unpleasant sensation that evokes a desire to scratch. Although often regarded as a trivial 'alarming' sensation, itch may be debilitating and exhausting, leading to reduction in quality of life. In the current study, the question of whether caffeic acid can be used to alleviate itch sensation induced by various pruritic agents, including histamine, chloroquine, SLIGRL-NH2, and β-alanine was investigated. It turned out that histamine-induced intracellular calcium increase was significantly blocked by caffeic acid in HEK293T cells that express H1R and TRPV1, molecules required for transmission of histamine-induced itch in sensory neurons. In addition, inhibition of histamine-induced intracellular calcium increase by caffeic acid was demonstrated in primary cultures of mouse dorsal root ganglion (DRG). When chloroquine, an anti-malaria agent known to induce histamine-independent itch - was used, it was also found that caffeic acid inhibits the induced response in both DRG and HEK293T cells that express MRGPRA3 and TRPA1, underlying molecular entities responsible for chloroquine-mediated itch. Likewise, intracellular calcium changes by SLIGRL-NH2 - an itch-inducing agent via PAR2 and MRGPRC11 - were decreased by caffeic acid as well. However, it was found that caffeic acid is not capable of inhibiting β-alanine-induced responses via its specific receptor MRGPRD [1].
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| Animal Protocol |
Experimental design [2]
Rats were divided into five groups: the sham group (n = 9), I/R non-treated group (n = 9), I/R-caffeic acid group (10 mg · kg−1) (n = 9), I/R-caffeic acid group (30 mg · kg−1) (n = 9) and I/R-caffeic acid group (50 mg · kg−1) (n = 9). In I/R-caffeic acid groups, the rats were administrated caffeic acid at 10, 30, 50 mg · kg−1 (prepared with 0.3% sodium carboxymethyl cellulose) by intraperitoneal injection at 30 min prior to ischemia. The sham group and I/R group were treated with an equal volume of 0.3% sodium carboxymethyl cellulose. Induction of global cerebral I/R model[2] Rats were anesthetized by intraperitoneal injection of chloral hydrate (400 mg/kg), and fixed in a supine position. Global cerebral ischemia was induced as previously described. A midline incision was made in the neck, after that the incision was extended 1 cm to the right. Then both common carotid arteries and the right common jugular vein were exposed carefully by blunt dissection. The distal end of the common jugular vein was ligated following 2 ml heparinized saline (100 mL 0.9% saline containing heparin (250 U)) were perfused. The blood accounting for about 30 percent of the total blood volumes were taken from the right common jugular vein leading to hypotension. Global cerebral ischemia was induced by bilateral clamping of the common carotid arteries combined with hypotension. After ischemia for 20 min, the artery clamps were removed, and the extracted blood was reinfused. Rats in the sham group were subjected to the same operation as above, excepted for the bilateral carotid artery occlusion and hemospasia from the right common jugular vein. |
| References |
[1]. Pradhananga S, et al. Caffeic acid exhibits anti-pruritic effects by inhibition of multiple itch transmission pathways in mice. Eur J Pharmacol. 2015 Sep 5;762:313-21.
[2]. Liang G, et al. The protective effect of caffeic acid on global cerebral ischemia-reperfusion injury in rats. Behav Brain Funct. 2015 Apr 18;11:18 |
| Molecular Formula |
C9H8O4
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|---|---|
| Molecular Weight |
180.1574
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| Exact Mass |
180.042252
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| CAS # |
331-39-5
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| Related CAS # |
trans-Caffeic acid;501-16-6;Caffeic acid phenethyl ester;104594-70-9;Caffeic acid-13C3;1185245-82-2
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| Appearance |
Off-white to light yellow solid
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| LogP |
1.42
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| tPSA |
77.76
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| SMILES |
O=C(O)/C=C/C1=CC=C(O)C(O)=C1
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| InChi Key |
QAIPRVGONGVQAS-DUXPYHPUSA-N
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| InChi Code |
InChI=1S/C9H8O4/c10-7-3-1-6(5-8(7)11)2-4-9(12)13/h1-5,10-11H,(H,12,13)/b4-2+
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| Chemical Name |
(E)-3-(3,4-dihydroxyphenyl)prop-2-enoic acid
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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 (~555.06 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (13.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (11.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5506 mL | 27.7531 mL | 55.5062 mL | |
| 5 mM | 1.1101 mL | 5.5506 mL | 11.1012 mL | |
| 10 mM | 0.5551 mL | 2.7753 mL | 5.5506 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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