Cat. No.: HY-N0105

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Rhein

(Synonyms: Rheic Acid; Rhubarb yellow; Monorhein)

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

Rhein is an anthraquinone compound with anti-inflammatory, antioxidant, and anti-cancer effects^{[1]^.}

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Pureté: 99.56%
CAS No.: 478-43-3
Formule: C₁₅H₈O₆
Masse moléculaire:284.22

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Rhein Chemical Structure

CAS No.: 478-43-3

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Rhein is an anthraquinone compound with anti-inflammatory, antioxidant, and anti-cancer effects^{[1]^.}

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.08 mM Compound: Rhein	Antiproliferative activity against human A549 cells Antiproliferative activity against human A549 cells	10.1039/C6MD00252H
A549	IC₅₀	120.4 μM Compound: Rhein	Antiproliferative activity in human A549 cells after 72 hrs by MTT assay Antiproliferative activity in human A549 cells after 72 hrs by MTT assay	10.1039/C6MD00252H
A549	IC₅₀	138 μM Compound: Rhein	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
A549	IC₅₀	265.59 μM Compound: Rhein	Anticancer activity against human A549 cells incubated for 48 hrs by MTT assay Anticancer activity against human A549 cells incubated for 48 hrs by MTT assay	[PMID: 38516604]
A549	IC₅₀	77.11 μg/mL Compound: A	Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 35963130]
A549	IC₅₀	95.8 μM Compound: Rhein	Antitumor activity against human A549 cells after 3 days by SRB assay Antitumor activity against human A549 cells after 3 days by SRB assay	[PMID: 25050882]
Bel-7402	IC₅₀	0.11 mM Compound: Rhein	Antiproliferative activity against human Bel7402 cells after 24 to 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 24 to 72 hrs by MTT assay	10.1039/C6MD00252H
Bel-7402	IC₅₀	120.27 μM Compound: Rhein	Antiproliferative activity in human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity in human Bel7402 cells after 72 hrs by MTT assay	10.1039/C6MD00252H
Bel-7402	IC₅₀	136.19 μM Compound: Rhein	Antiproliferative activity in 5-FU resistant human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity in 5-FU resistant human Bel7402 cells after 72 hrs by MTT assay	10.1039/C6MD00252H
CNE	IC₅₀	>100 μM Compound: Rhein	Cytotoxicity against human CNE cells after 48 hrs by MTT assay Cytotoxicity against human CNE cells after 48 hrs by MTT assay	[PMID: 24378217]
CNE	IC₅₀	81.7 μM Compound: Rhein	Antiproliferative activity against human CNE cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human CNE cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
COLO 320DM	IC₅₀	62.5 μM Compound: Rhein	Cytotoxicity against human COLO320DM cells Cytotoxicity against human COLO320DM cells	[PMID: 24378217]
HCT-116	IC₅₀	>100 μM Compound: Rhein	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 24378217]
HCT-116	IC₅₀	115.7 μM Compound: Rhein	Antiproliferative activity in human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity in human HCT116 cells after 72 hrs by MTT assay	10.1039/C6MD00252H
HCT-116	IC₅₀	13 μM Compound: 5	Cytotoxicity against MDR1 Pgp under-expressing human HCT116 cells after 24 hrs by MTT assay Cytotoxicity against MDR1 Pgp under-expressing human HCT116 cells after 24 hrs by MTT assay	[PMID: 17949858]
HCT-116	IC₅₀	135 μM Compound: Rhein	Cytotoxicity against human HCT116 cells Cytotoxicity against human HCT116 cells	[PMID: 24378217]
HeLa	IC₅₀	>100 μM Compound: Rhein	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	[PMID: 24378217]
HeLa	IC₅₀	92.2 μM Compound: Rhein	Antitumor activity against human HeLa cells after 3 days by SRB assay Antitumor activity against human HeLa cells after 3 days by SRB assay	[PMID: 25050882]
HepG2	IC₅₀	>100 μM Compound: Rhein	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 24378217]
HepG2	IC₅₀	0.71 mM Compound: Rhein	Antiproliferative activity against human HepG2 cells Antiproliferative activity against human HepG2 cells	10.1039/C6MD00252H
HepG2	IC₅₀	100.8 μM Compound: Rhein	Antiproliferative activity in human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity in human HepG2 cells after 72 hrs by MTT assay	10.1039/C6MD00252H
HepG2	IC₅₀	12.3 μM Compound: 5	Cytotoxicity against MDR1 Pgp overexpressing human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against MDR1 Pgp overexpressing human HepG2 cells after 24 hrs by MTT assay	[PMID: 17949858]
HepG2	IC₅₀	74.6 μM Compound: Rhein	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
HL-60	IC₅₀	0.1 mM Compound: Rhein	Antiproliferative activity against human HL60 cells Antiproliferative activity against human HL60 cells	10.1039/C6MD00252H
HUVEC	IC₅₀	89.74 μM Compound: Rhein	Cytotoxicity against human HUVEC after 48 hrs by MTT assay Cytotoxicity against human HUVEC after 48 hrs by MTT assay	[PMID: 24378217]
MCF7	IC₅₀	0.13 mM Compound: Rhein	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	10.1039/C6MD00252H
MCF7	IC₅₀	105.7 μM Compound: Rhein	Antiproliferative activity in human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity in human MCF7 cells after 72 hrs by MTT assay	10.1039/C6MD00252H
MDA-MB-231	IC₅₀	41.8 μM Compound: Rhein	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
SCC-4	IC₅₀	0.058 mM Compound: Rhein	Antiproliferative activity against human SCC4 cells Antiproliferative activity against human SCC4 cells	10.1039/C6MD00252H
SGC-7901	IC₅₀	0.15 mM Compound: Rhein	Antiproliferative activity against human SGC7901 cells after 24 to 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 24 to 72 hrs by MTT assay	10.1039/C6MD00252H
SK-OV-3	IC₅₀	71.5 μM Compound: Rhein	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
WI-38	IC₅₀	324.9 μM Compound: Rhein	Cytotoxicity against human WI-38 cells incubated for 48 hrs by MTT assay Cytotoxicity against human WI-38 cells incubated for 48 hrs by MTT assay	[PMID: 38516604]
WI-38	IC₅₀	92.34 μg/mL Compound: A	Antiproliferative activity against human WI-38 cells measured after 48 hrs by MTT assay Antiproliferative activity against human WI-38 cells measured after 48 hrs by MTT assay	[PMID: 35963130]

In Vitro

Rhein (0-80 μM, 72 h) inhibits the viability of NB4 cells in a dose-dependent manner [2].
Rhein (5 μM, 72 h) increases semi-adherent, macrophage-like cells, and expression of CD11b, CD14, CCR-1 and CCR-2, and increases ROS production and phagocytosis in ATRA-activated NB4 cells^[2].
Rhein (5 μM, 72 h) induces NB4 cell death by activating apoptosis and inhibiting the mTOR pathway ^[2].
Rhein (50-200 μM, 48 h) inhibits angiogenesis in MCF-7 and MDA-MB-435 cells^[4].
Rhein (0-50 μM, 24 h) inhibits HUVEC roliferation, migration, invasion, and tube formation (inhibits VEGF165, EGF in supernatant and HIF-1α in nuclear extract)^[4].

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

RT-PCR^[2]

Cell Line:

acute promyelocytic leukemia (APL) cell (NB4 cells)
Concentration:

5 μM
Incubation Time:

72 h
Result:

Increaseed mRNA expression of PU.1, C/EBPA, and C/EBPE.
Increaseed ATRA activated mRNA expression of CCR1 and CCR2.

Western Blot Analysis^[2]

Cell Line:

NB4 cells
Concentration:

0-40 μM
Incubation Time:

48 and 72 h
Result:

Increased the expression of cleaved caspase-3, Bax.
Decreased the expression of Bcl-xl, procaspase-3.

In Vivo

Rhein (10-40 mg/kg, i.g.) protects against Acetaminophen (HY-66005)-induced hepatic and renal toxicity in rats^[3].

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

Animal Model:

2.5 g/kg APAP (i.g.) induced rats^[3]
Dosage:

10, 20 and 40 mg/kg
Administration:

i.g.
Result:

Ameliorated histopathological damage of liver and kidney.
Reduced GPT, GOT, UREA and CREA levels and ROS production.
Restored NO, MDA, GSH contents.

Chemical Information

CAS No. 478-43-3
Appearance Solid
Masse moléculaire 284.22
Formule C₁₅H₈O₆
Color Light yellow to yellow
SMILES

O=C(C(C=C1C2=O)=CC(O)=C1C(C3=C2C=CC=C3O)=O)O
Synonyms

Rheic Acid; Rhubarb yellow; Monorhein
Structure Classification
- Quinones
- Anthraquinones
- Phenols
- Polyphenols
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

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Journal Impact Factor

J Nanobiotechnology

All-in-one: a CGRP-encapsulated Rh-GelMA supramolecular dual-network hydrogel orchestrating immune-vascular coupling for diabetic wound healing. [Abstract]

2026 May 16;24(1):645. PMID: 42143359
Small Methods

2020, 2000483.
Phytomedicine

Yinchenhao decoction and its active compound rhein ameliorate intrahepatic cholestasis of pregnancy in mice via modulation of intestinal flora. [Abstract]

2025 Oct 14:148:157397. PMID: 41135275
Br J Pharmacol

Rhein regulates redox-mediated activation of NLRP3 inflammasomes in intestinal inflammation through macrophage-activated crosstalk. [Abstract]

2022 May;179(9):1978-1997. PMID: 34882785
Cell Rep

Activated CD38+ mast cells promote gastric cancer progression by suppressing CD8+ T cell cytotoxic activity through adenosine metabolism. [Abstract]

2026 Jan 22;45(2):116863. PMID: 41579372
Mol Med

A novel mechanism of FTO modulating the progression of endometriosis through mediating the m6A methylation of GEF-H1 in a YTHDF1-dependent manner. [Abstract]

2025 Feb 25;31(1):78. PMID: 40000966
Biochem Pharmacol

Rhein suppresses osteosarcoma progression via modulating the miR-328-3p/TCF7L2/FABP4 axis. [Abstract]

2025 Jul 11:241:117152. PMID: 40653025
J Ethnopharmacol

Discovery and validation of anti-arthritic ingredients and mechanisms of Qingfu Juanbi Tang, a Chinese herbal formulation, on rheumatoid arthritis. [Abstract]

2024 Jul 15:329:118140. PMID: 38565409
J Inflamm Res

Rhein Mitigates Lung Injury in Severe Acute Pancreatitis Through the Inhibition of MARK4-Mediated Microtubule Destabilization. [Abstract]

2025 Jan 30:18:1395-1412. PMID: 39906137

Rhein purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Jan 30:18:1395-1412. [Abstract]

Toxicity of different doses of Rhein (5, 10, 20, 40, 60, 80, 100 μM) on R-PMVEC was detected by CCK8.

Rhein purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Jan 30:18:1395-1412. [Abstract]

MARK4 mRNA relative expression in R-PMVEC treated with different doses of Rhein (5, 20, 40 μM) was performed by Real-Time quantitative PCR.

Rhein purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Jan 30:18:1395-1412. [Abstract]

Protein expression levels of MARK4 and p-MAP4 (S1073) in R-PMVEC treated with different doses of Rhein (5, 20, 40 μM) were performed by Western blot.

Rhein purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Jan 30:18:1395-1412. [Abstract]

Rhein (200, 250 mg/kg, i.g.) induced kidney histopathology sections showed edema, necrosis, and immune cell infiltration.

Rhein purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Jan 30:18:1395-1412. [Abstract]

Immunofluorescence staining showed that apparent MT damage happened in the lungs of SAP group rats. After administration of the MARK4 inhibitor or Rhein (150 mg/kg, i.g.), the MT damage was significantly alleviated.
J Pharm Pharmacol

A novel rhein derivative Y01 inhibits hepatocellular carcinoma by inducing apoptosis through regulating PI3K/AKT/mTOR pathway. [Abstract]

2025 Dec 3:rgaf120. PMID: 41332198
World J Tradit Chin Med

Anti-inflammatory mechanism of rhein in treating asthma based on network pharmacology. [Abstract]

2022 Apr;42(2):296-303. PMID: 35473352
J Orthop Surg Res

Fibrin glue delivery system containing rhein ameliorates intervertebral disc degeneration by anti-inflammatory efficacy. [Abstract]

2023 Jul 6;18(1):485. PMID: 37415165
Biochem Biophys Res Commun

A novel Rhein derivative AQ-NC inhibits prostate cancer by suppressing the PI3K/AKT pathway. [Abstract]

2025 Sep 30:786:152718. PMID: 41045575
Biochem Biophys Res Commun

Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. [Abstract]

2018 Sep 3;503(1):297-303. PMID: 29890135
Neurosci Lett

Rhein attenuates PTZ‑induced epilepsy and exerts neuroprotective activity via inhibition of the TLR4-NFκB signaling pathway. [Abstract]

2021 Jul 27:758:136002. PMID: 34090938
Biocell

2025 Sep 25;49(9):1711-1731.
Research Square Preprint

2024 Jan 3.
Research Square Print

2023 Mar 17.

Solvant et solubilité

In Vitro:

DMSO : 7.14 mg/mL (25.12 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)

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

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: 1.67 mg/mL (5.88 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.67 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 (16.7 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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC-Na/saline water

Solubility: 10 mg/mL (35.18 mM); Suspended solution; Need ultrasonic

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[2]. Heo SK, et al. Rhein augments ATRA-induced differentiation of acute promyelocytic leukemia cells. Phytomedicine. 2018 Oct 1;49:66-74. [Content Brief]

[3]. Zhao YL, et al. Rhein protects against acetaminophen-induced hepatic and renal toxicity. Food Chem Toxicol. 2011 Aug;49(8):1705-10. [Content Brief]

[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. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5184 mL	17.5920 mL	35.1840 mL	87.9600 mL
	5 mM	0.7037 mL	3.5184 mL	7.0368 mL	17.5920 mL
	10 mM	0.3518 mL	1.7592 mL	3.5184 mL	8.7960 mL
	15 mM	0.2346 mL	1.1728 mL	2.3456 mL	5.8640 mL
	20 mM	0.1759 mL	0.8796 mL	1.7592 mL	4.3980 mL
	25 mM	0.1407 mL	0.7037 mL	1.4074 mL	3.5184 mL

Keywords

Rhein

18 Cited Publications

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Rhein

Natural Product Library Plus

Drug Fragment Library

Publications Citing Use of MedChemExpress (MCE) Rhein

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Rhein

Natural Product Library Plus

Drug Fragment Library

Publications Citing Use of MedChemExpress (MCE) Rhein

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Rhein Related Classifications

HY-N0105 Related Classifications