| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Animal Protocol |
Pithed Rat Model for α-Adrenoceptor Activity: Male Wistar rats (300-350 g) were used. Animals were pithed under anesthesia to destroy the central nervous system, then artificially ventilated (10 ml/kg, 50 strokes/min). They were treated with atropine and (+)-tubocurarine (1 mg/kg each, i.v.) to block parasympathetic and neuromuscular transmission, respectively. The vagus nerve was cut at the cervical level. Body temperature was maintained at 37°C. The left femoral vein was cannulated for drug administration, and arterial pressure was continuously recorded via a transducer connected to the left common carotid artery.
Pressor Response to Noradrenaline: A single dose of noradrenaline (0.5 µg/kg, i.v.) was administered to induce a rise in mean arterial pressure (approx. 69 ± 7 mmHg). The inhibitory effect of Tetrahydroalstonine (THA) was tested by injecting it intravenously 5 minutes before the noradrenaline challenge. One dose of THA was used per rat. The reduction in the pressor response was calculated as a percentage of the control response. Pressor Response to Electrical Stimulation: The complete sympathetic outflow from the spinal cord was stimulated using monophasic square wave pulses (2 ms, 10 V, 3 Hz) applied for 15 to 45 seconds at 10-minute intervals. This stimulation induced a rise in mean arterial pressure (approx. 71 ± 8 mmHg). The inhibitory effect of Tetrahydroalstonine (THA) was tested by injecting it intravenously 5 minutes before a stimulation period. One dose of THA was used per rat. The reduction in the pressor response was calculated as a percentage of the control response. Drug Formulation: Tetrahydroalstonine (THA) was dissolved in a 1% tartaric acid solution at a concentration of 35 mg/10 ml, and further diluted with saline (0.9% NaCl) to the required concentrations for intravenous administration. Doses refer to the free base. [2] |
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| References | |
| Additional Infomation |
Ajmalicine is a monoterpenoid indole alkaloid with the molecular formula C21H24N2O3, isolated from various plants in the genera Rauvolfia and Catharanthus. It is a selective α1-adrenergic receptor antagonist used to treat hypertension. It possesses antihypertensive, α-adrenergic antagonistic, and vasodilatory effects. Ajmalicine is a monoterpenoid indole alkaloid, belonging to the methyl ester class of compounds, and is also an organic heteropentacyclic compound. It is the conjugate base of Ajmalicine (1+). It has been reported that Ajmalicine is present in Rauvolfia yunnanensis, Campsis grandiflora, and other organisms with relevant data.
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| Molecular Formula |
C21H24N2O3
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|---|---|
| Molecular Weight |
352.4269
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| Exact Mass |
352.178
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| CAS # |
6474-90-4
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| PubChem CID |
441975
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
524.0±50.0 °C at 760 mmHg
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| Melting Point |
227ºC
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| Flash Point |
270.7±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
2.88
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
606
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@H]1[C@H]2CN3CCC4=C([C@@H]3C[C@@H]2C(=CO1)C(=O)OC)NC5=CC=CC=C45
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| InChi Key |
GRTOGORTSDXSFK-XJTZBENFSA-N
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| InChi Code |
InChI=1S/C21H24N2O3/c1-12-16-10-23-8-7-14-13-5-3-4-6-18(13)22-20(14)19(23)9-15(16)17(11-26-12)21(24)25-2/h3-6,11-12,15-16,19,22H,7-10H2,1-2H3/t12-,15-,16+,19-/m0/s1
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| Chemical Name |
methyl (1S,15R,16S,20S)-16-methyl-17-oxa-3,13-diazapentacyclo[11.8.0.02,10.04,9.015,20]henicosa-2(10),4,6,8,18-pentaene-19-carboxylate
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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 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~283.74 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 | 2.8374 mL | 14.1872 mL | 28.3744 mL | |
| 5 mM | 0.5675 mL | 2.8374 mL | 5.6749 mL | |
| 10 mM | 0.2837 mL | 1.4187 mL | 2.8374 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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