Kanglexin is a novel orally effective anthraquinone compound. Kanglexin can inhibit NLRP3 inflammasome activation and pyroptosis, and has a cardioprotective effect. Kanglexin promotes angiogenesis through the FGFR1/ERK signaling pathway and accelerates diabetic wound healing. In addition, Kanglexin has the effects of lowering lipids and inhibiting the dedifferentiation of vascular smooth muscle cells, and can be used in the study of hyperlipidemia, fatty liver and atherosclerosis.

Physicochemical Properties

Molecular Formula	C21H18O8
Molecular Weight	398.36
CAS #	2228847-12-7
Appearance	Typically exists as solids at room temperature
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	NLRP3
ln Vitro	Kanglexin (10-20 μM; 24 hours) inhibits pyroptosis in cardiomyocytes treated with hypoxia or LPS[1]. Kanglexin (5-20 μM; 24 hours) reduces lipid levels in oleic acid-treated HepG2 cells via the AMPK/SREBP-2/PCSK9/LDLR signaling pathway[2].
ln Vivo	Kanglexin (20-40 mg/kg; oral administration; 7 days) has an ameliorative effect in a mouse model of myocardial infarction[1]. Kanglexin (20-80 mg/kg; oral administration; 2 weeks) has an ameliorative effect in a rat model of hyperlipidemia[2].
Cell Assay	Western Blot Analysis[1] Cell Types: LPS treated neonatal mouse ventricular cardiomyocytes Tested Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Inhibited the levels of NLRP3 and the pyroptosis-related proteins mature IL-1β and IL-18.
Animal Protocol	Animal/Disease Models: Male C57BL/6 mice aged 8 weeks old (20 ± 2 g) with myocardial infarction (MI) model[1] Doses: 20 and 40 mg/kg Route of Administration: Oral gavage (i.g.); 7 days Experimental Results: Reduced myocardial injury in MI mice. Effectively inhibited pyroptosis processes in the mouse hearts with MI. Attenuated the activation of the NLRP3 inflammasome upon MI in mouse hearts. Animal/Disease Models: High fat diet treated Sprague-Dawley rats[2] Doses: 20, 40 and 80 mg/kg Route of Administration: Oral administration (p.o.); 2 weeks Experimental Results: Had prominent effects on reducing blood lipids, hepatic lipid accumulation, body weight and the ratio of liver weight/body weight.
References	[1]. Kanglexin, a novel anthraquinone compound, protects against myocardial ischemic injury in mice by suppressing NLRP3 and pyroptosis. Acta Pharmacol Sin. 2020 Mar;41(3):319-326. [2]. Kanglexin, a new anthraquinone compound, attenuates lipid accumulation by activating the AMPK/SREBP-2/PCSK9/LDLR signalling pathway. Biomed Pharmacother. 2021 Jan;133:110802. [3]. Kanglexin counters vascular smooth muscle cell dedifferentiation and associated arteriosclerosis through inhibiting PDGFR. Phytomedicine. 2024 Jul 25;130:155704. [4]. Kanglexin accelerates diabetic wound healing by promoting angiogenesis via FGFR1/ERK signaling. Biomed Pharmacother. 2020 Dec;132:110933.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5103 mL	12.5515 mL	25.1029 mL
	5 mM	0.5021 mL	2.5103 mL	5.0206 mL
	10 mM	0.2510 mL	1.2551 mL	2.5103 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.