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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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Purity: ≥98%
Rhein (also known as Monorhein; NSC 38629; Rheic acid; Rheinic acid) is a naturally occuring anthraquinone compound isolated from the fresh rhizome of Rheum coreanum Nakai, showing anti-inflammation and antitumor activities. Rhein at 35 μM can effectively inhibit the synthesis of IL-1β on human osteoarthritis synovium, as well as the action of this cytokine at the cartilage level, by reducing the number of chondrocyte IL-1R and inhibiting IL-1β induced NO production in chondrocytes and cartilage. Rhein also induces apoptosis in human promyelocytic leukemia cells (HL-60), characterized by caspase activation, poly(ADP)ribose polymerase (PARP) cleavage, and DNA fragmentation.
| ln Vitro |
Rhein reduces NB4 cell viability in a dose-dependent manner (0-80 μM, 72 hours) [2]. Rhein (5 μM, 72 hours) enhances the formation of ROS in ATRA-activated NB4 cells, as well as semi-adherent macrophage-like cells and phagocytosis, as well as the expression of CD11b, CD14, CCR-1, and CCR-2 [2]. Rhein (5 μM, 72 hours) inhibits the mTOR pathway and triggers apoptosis in NB4 cells [2]. In MCF-7 and MDA-MB-435 cells, Rhein (50-200 μM, 48 hours) suppresses angiogenesis [4]. HUVEC proliferation, migration, invasion, and tube formation are inhibited by Rhein (0-50 μM, 24 hours) (inhibition of VEGF165, EGF in supernatant, and HIF-1α in nuclear extract) [4].
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| ln Vivo |
In rats, acetaminophen-induced liver and renal damage is prevented by Rhein (10–40 mg/kg, ig) [3].
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| Cell Assay |
RT-PCR[2]
Cell Types: acute promyelocytic leukemia (APL) cell (NB4 cells) Tested Concentrations: 5 μM Incubation Duration: 72 h Experimental Results: Increased mRNA expression of PU.1, C/EBPA, and C/EBPE. Increased ATRA activated mRNA expression of CCR1 and CCR2. Western Blot Analysis[2] Cell Types: NB4 cells Tested Concentrations: 0-40 μM Incubation Duration: 48 and 72 h Experimental Results: Increased the expression of cleaved caspase-3, Bax. diminished the expression of Bcl -xl,procaspase-3. |
| Animal Protocol |
Animal/Disease Models: 2.5 g/kg APAP (ig) induced rats[3]
Doses: 10, 20 and 40 mg/kg Route of Administration: ig Experimental Results: Ameliorated histopathological damage of liver and kidney. decreased GPT, GOT, UREA and CREA levels and ROS production. Restored NO, MDA, GSH contents. |
| References |
[1]. Hou ML, et al. The Drug-Drug Effects of Rhein on the Pharmacokinetics and Pharmacodynamics of Clozapine in Rat Brain Extracellular Fluid by In Vivo Microdialysis. J Pharmacol Exp Ther. 2015 Oct;355(1):125-34.
[2]. Heo SK, et al. Rhein augments ATRA-induced differentiation of acute promyelocytic leukemia cells. Phytomedicine. 2018 Oct 1;49:66-74. [3]. Zhao YL, et al. Rhein protects against acetaminophen-induced hepatic and renal toxicity. Food Chem Toxicol. 2011 Aug;49(8):1705-10. [4]. Fernand VE, et al. Rhein inhibits angiogenesis and the viability of hormone-dependent and -independent cancer cells under normoxic or hypoxic conditions in vitro. Chem Biol Interact. 2011 Jul 15;192(3):220-32. |
| Molecular Formula |
C15H8O6
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| Molecular Weight |
284.22
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| CAS # |
478-43-3
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| Related CAS # |
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| SMILES |
O([H])C1=C([H])C(C(=O)O[H])=C([H])C2C(C3C([H])=C([H])C([H])=C(C=3C(C=21)=O)O[H])=O
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| InChi Key |
FCDLCPWAQCPTKC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8O6/c16-9-3-1-2-7-11(9)14(19)12-8(13(7)18)4-6(15(20)21)5-10(12)17/h1-5,16-17H,(H,20,21)
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| Chemical Name |
4,5-Dihydroxyanthraquinone-2-carboxylic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (5.88 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5184 mL | 17.5920 mL | 35.1840 mL | |
| 5 mM | 0.7037 mL | 3.5184 mL | 7.0368 mL | |
| 10 mM | 0.3518 mL | 1.7592 mL | 3.5184 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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