| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
|
| Targets |
IC50: 872 nM (AChE)[1]
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|---|---|
| ln Vitro |
Jatrorrhizine exhibits antiplasmodial and antiamoebic properties, with IC50 values of 3.15 and 82.7 µM, respectively, against Plasmodium falciparum and E. histolytica[1]. Neurotransmitters known as monoamines can be transported in the brain via the hOCT2 (organic cation transporter 2), hOCT3, and PMAT (plasma membrane monoamine transporter)[3]. When it comes to 5-HT and NE uptake in hOCT2-, hOCT3-, and PMAT-transfected cells, jatrorrhizine exhibits the same inhibitory effectiveness. With a PMAT-mediated MPP+ uptake IC50 value of 1.05 μM, jatrorrhizine severely inhibits it. It also decreases 5-HT and NE uptake mediated by hOCT2, hOCT3, and hPMAT, with IC50 values of 1-10 μM for PMAT and 0.1-1 μM for OCT2 and OCT3[3]. Two separate processes determine the clearance of neurotransmitters produced into the synaptic cleft. The serotonin transporter, or "SERT," has a high affinity but a limited ability to take up [3H]5-HT. Uptake-1, the typical target of currently used antidepressants, is made up of this protein. An essential supplemental regulatory mechanism for the clearance of monoamines is the uptake-2 transporter.Low affinity but great capacity to absorb [3H]5-HT into brain slices characterizes what is believed to be the "NET." 5-HT and NE absorption in synaptosomes was markedly reduced by jatrorrhizine at 25 μM and 50 μM[3].
|
| ln Vivo |
In the tail suspension test (TST), jatrorrhizine (intraperitoneal injection; 5, 10, 20 mg/kg) can dramatically shorten the period of immobility in comparison to the vehicle control group[2].
|
| Animal Protocol |
Animal/Disease Models: Male ICR albino mice[2]
Doses: 5, 10, 20 mg/kg Route of Administration: intraperitoneal (ip)injection; 5, 10, 20 mg/kg Experimental Results: diminished immobility period in tail suspension test. |
| References |
|
| Molecular Formula |
C20H20NO4
|
|---|---|
| Molecular Weight |
338.377
|
| Exact Mass |
355.141
|
| CAS # |
483-43-2
|
| Related CAS # |
Jatrorrhizine chloride;6681-15-8;Jatrorrhizine;3621-38-3
|
| PubChem CID |
12304700
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| Appearance |
Brown to black solid powder
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
|
| Heavy Atom Count |
26
|
| Complexity |
461
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C12C([H])C3C([H])C([H])C(OC([H])([H])[H])C(OC([H])([H])[H])C3C([H])N1C(C(C1C2C([H])C(OC([H])([H])[H])C(O[H])C1[H])([H])[H])([H])[H]
|
| InChi Key |
FLLCSIZPVWDZQO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H19NO4.H2O/c1-23-18-5-4-12-8-16-14-10-19(24-2)17(22)9-13(14)6-7-21(16)11-15(12)20(18)25-3;/h4-5,8-11H,6-7H2,1-3H3;1H2
|
| Chemical Name |
2,9,10-trimethoxy-5,6-dihydroisoquinolino[2,1-b]isoquinolin-7-ium-3-ol;hydroxide
|
| 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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
H2O : 5 mg/mL (14.07 mM)
DMSO : 3.33 mg/mL (9.37 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 | 2.9553 mL | 14.7763 mL | 29.5526 mL | |
| 5 mM | 0.5911 mL | 2.9553 mL | 5.9105 mL | |
| 10 mM | 0.2955 mL | 1.4776 mL | 2.9553 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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