| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
| ln Vitro |
Twenty-four hours after treatment, lenurine (0, 5, 10, 20, 40, 80 μM) increases apoA-I, or HDL-mediated cholesterol efflux, and decreases lipid accumulation as well as cellular cholesterol content, including total cholesterol (TC), free cholesterol (FC), and cholesteryl esters (CE). In human THP-1 macrophages, lenurine also dramatically and dose-dependently upregulates the mRNA and protein expression of ABCA1 and ABCG1, an effect that is associated with PPARγ [1]. After being cultured with free fatty acid (FFA) and palmitic acid (PA) for 24 hours, HepG2 and HL-7702 cells demonstrated a protective impact from leucine hydrochloride (LH) on their ability to survive. By triggering the AMPK/SREBP1 pathway, lenurine hydrochloride (125, 250, and 500 μM) enhances cellular lipid accumulation in HepG2 and HL-7702 cells [2]. In human chondrocytes, leonurine (5, 10, 20 μM) reduces the production of iNOS, COX-2, PGE2, NO, TNF-α, and IL-6 caused by IL-1β. It also inhibits the breakdown of extracellular matrix (ECM) in human OA chondrocytes. Furthermore, in a dose-dependent way, blocking IL-1β causes PI3K and Akt activation.
|
|
|---|---|---|
| ln Vivo |
In mouse serum, leonurine (10 mg/kg/d, po) dramatically raises the expression of PPARγ, LXRα, ABCA1, and ABCG1 while lowering TG and TC levels [1]. By activating the AMPK/SREBP1 pathway, levonurine hydrochloride (50, 100, or 200 mg/kg) improves intracellular lipid accumulation, biochemical parameters, liver lipid peroxides, and antioxidant levels in mice [2]. In a mouse model of DMM, leonurine (20 mg/kg, orally) ameliorates the development of osteoarthritis [3].
|
|
| Cell Assay |
|
|
| References |
|
| Molecular Formula |
C₁₄H₂₂CLN₃O₅
|
|---|---|
| Molecular Weight |
347.79
|
| Exact Mass |
347.124
|
| CAS # |
24735-18-0
|
| Related CAS # |
Leonurine;24697-74-3
|
| PubChem CID |
46837042
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
194 ºC
|
| LogP |
2.822
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
23
|
| Complexity |
360
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GHVZIMAVDJZQGP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H21N3O5.ClH/c1-20-10-7-9(8-11(21-2)12(10)18)13(19)22-6-4-3-5-17-14(15)16;/h7-8,18H,3-6H2,1-2H3,(H4,15,16,17);1H
|
| Chemical Name |
4-(diaminomethylideneamino)butyl 4-hydroxy-3,5-dimethoxybenzoate;hydrochloride
|
| Synonyms |
SCM-198 HCl SCM 198HClSCM198HCl SCM-198 SCM 198SCM198SCM-198 hydrochlorideSCM198 hydrochlorideSCM 198 hydrochloride
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 31 mg/mL (~89.13 mM)
H2O : ~5 mg/mL (~14.38 mM) |
|---|---|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8753 mL | 14.3765 mL | 28.7530 mL | |
| 5 mM | 0.5751 mL | 2.8753 mL | 5.7506 mL | |
| 10 mM | 0.2875 mL | 1.4376 mL | 2.8753 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
