| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| ln Vitro |
In the neurons of silkworm larvae, asperparaline A (1 μM; 1 min) significantly and reversibly inhibits the current generated by acetylcholine (Ach; 10 µM)[2]. With IC50s of 20.2 and 39.6 nM, respectively, asperparaline A (1-1000 nM; 1 min) differentially blocks the peak and gradually desensitizing currents[2]. Asperparaline A (10 μM; 1 min) marginally affects the amplitudes of the responses to ACh of the α4β2 and α7 nAChRs in X, but decreases the peak current amplitude of the ACh (100 µM)-induced response of α3β4 nAChR by 33.4%. Ovum laevis [2].
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| ln Vivo |
Asperparaline A (10 μg/g; po) acts against silk worms to cause paralysis after one hour and continues to do so for seven to ten hours[1]. Asperparaline A (3 μg/g; injection with a micro-syringe) paralyzes silk worms within 20 minutes and keeps the effect going for 4 to 5 hours[1].
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| References |
[1]. Hayashi H, et, al. New paralytic alkaloids, asperparalines A, B and C, from Aspergillus japonicus JV-23. Biosci Biotechnol Biochem. 2000 Jan;64(1):111-5.
[2]. Hirata K, et, al. A fungal metabolite asperparaline a strongly and selectively blocks insect nicotinic acetylcholine receptors: the first report on the mode of action. PLoS One. 2011 Apr 1;6(4):e18354. |
| Molecular Formula |
C20H29N3O3
|
|---|---|
| Molecular Weight |
359.46
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| CAS # |
195966-93-9
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| SMILES |
O=C1C23[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])N2C([H])([H])[C@@]2(C([H])([H])[C@@]4(C(N(C([H])([H])[H])C(C4([H])[H])=O)=O)C(C([H])([H])[H])(C([H])([H])[H])[C@]2([H])C3([H])[H])N1C([H])([H])[H]
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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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7820 mL | 13.9098 mL | 27.8195 mL | |
| 5 mM | 0.5564 mL | 2.7820 mL | 5.5639 mL | |
| 10 mM | 0.2782 mL | 1.3910 mL | 2.7820 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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