| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
TLR9; Autophagy
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|---|---|
| ln Vitro |
Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It interferes with an essential step in the autophagic process by preventing lysosomal acidification. Treatment with HCQ reduces the growth of RCC (renal cell cancer) cells, boosts glycolysis, encourages apoptosis, and prevents mitochondrial oxygen consumption[2].
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| ln Vivo |
In an in vivo rat model of I/R injury, hydroxychloroquine sulfate treatment reduces the infarct size, and the cardioprotective effect of hydroxychloroquine is ERK1/2 dependent[3].
Additionally, hydroxychloroquine sulfate exhibits an early protective effect on the vascular system. Endothelial dysfunction (ED) appears to be avoided in treated animals by HCQ[4]. |
| Enzyme Assay |
Recombinant S6 protein and recombinant active P70S6K are used with purified proteins, and they are incubated in 1x kinase buffer with varying concentrations of HCQ or RAD001 in either the presence (25 μM) or absence of ATP for 30 minutes at 30°C. With the aid of phosphospecific antibodies and western analysis, total and phosphorylated S6 at the positions ser235/236 and ser240/244 are found. On the western blot, recombinant GST-tagged S6 (53 kd) can be distinguished from endogenous S6 (32 kd).
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| Cell Assay |
All cells are cultured in RPMI containing 10% FBS, 1% glutamine, and 1% Pen/Strep. After overnight cell seeding on the appropriate plates, HCQ (75 or 100 μM) is applied for 48 hours.
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| References | |
| Additional Infomation |
Epipodophyllotoxin has been reported in Juniperus sabina and Podophyllum peltatum with data available.
A lignan (LIGNANS) found in PODOPHYLLIN resin from the roots of PODOPHYLLUM plants. It is a potent spindle poison, toxic if taken internally, and has been used as a cathartic. It is very irritating to skin and mucous membranes, has keratolytic actions, has been used to treat warts and keratoses, and may have antineoplastic properties, as do some of its congeners and derivatives. |
| Molecular Formula |
C22H22O8
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|---|---|
| Molecular Weight |
414.40528
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| Exact Mass |
414.131
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| CAS # |
4375-07-9
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| Related CAS # |
4375-07-9
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| PubChem CID |
105111
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| Appearance |
Solid
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| Density |
1.37g/cm3
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| Boiling Point |
597.9ºC at 760 mmHg
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| Melting Point |
160.3 °C
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| Flash Point |
210.2ºC
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| Index of Refraction |
1.605
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| LogP |
2.409
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
629
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| Defined Atom Stereocenter Count |
4
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| SMILES |
COC1C(OC)=CC([C@@H]2C3=CC4OCOC=4C=C3[C@@H](O)[C@H]3COC(=O)[C@H]23)=CC=1OC
|
| InChi Key |
YJGVMLPVUAXIQN-LGWHJFRWSA-N
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| InChi Code |
InChI=1S/C22H22O8/c1-25-16-4-10(5-17(26-2)21(16)27-3)18-11-6-14-15(30-9-29-14)7-12(11)20(23)13-8-28-22(24)19(13)18/h4-7,13,18-20,23H,8-9H2,1-3H3/t13-,18+,19-,20+/m0/s1
|
| Chemical Name |
(5S,5aR,8aR,9R)-5-hydroxy-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[5,6-f][1,3]benzodioxol-8-one
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| Synonyms |
(-)-Epipodophyllotoxin
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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 |
| 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: ~87 mg/mL (~200.5 mM)
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|---|---|
| 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 | 2.4131 mL | 12.0653 mL | 24.1307 mL | |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8261 mL | |
| 10 mM | 0.2413 mL | 1.2065 mL | 2.4131 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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