| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
α1-adrenergic receptors are preferentially blocked by ajmalicine, as opposed to α2-adrenergic receptors [1]. In a concentration-dependent manner, ajmalicine inhibits contraction (IC50=72.3 ± 22.5 μM)[2]. Ajmalicine operates preferentially on the postsynaptic site, with a pA2 value of 6.2[3] indicating that it blocks the inhibitory action of clonidine and competitively antagonizes the effect of norepinephrine on postsynaptic α-adrenergic receptors.
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|---|---|
| ln Vivo |
Ajmalicine is active on sympathetic stimulation and inhibits the pressor impact of electrical stimulation [1]. A substantial dose-dependent reduction of the pressor response to norepinephrine is produced by ajmalicine (0.5–4 mg/kg) [1].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (300-350 g) [1]
Doses: 0.5, 1, 2 and 4 mg/kg Route of Administration: intravenous (iv) (iv)injection, once Experimental Results: Significant pressor response to norepinephrine dose-dependent inhibition. |
| References |
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| Additional Infomation |
Ajmalicine is a monoterpenoid indole alkaloid with formula C21H24N2O3, isolated from several Rauvolfia and Catharanthus species. It is a selective alpha1-adrenoceptor antagonist used for the treatment of high blood pressure. It has a role as an antihypertensive agent, an alpha-adrenergic antagonist and a vasodilator agent. It is a monoterpenoid indole alkaloid, a methyl ester and an organic heteropentacyclic compound. It is a conjugate base of an ajmalicine(1+).
Ajmalicine has been reported in Rauvolfia yunnanensis, Sarcococca saligna, and other organisms with data available. |
| Molecular Formula |
C21H24N2O3
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|---|---|
| Molecular Weight |
352.4269
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| Exact Mass |
352.178
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| CAS # |
483-04-5
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| Related CAS # |
Ajmalicine hydrochloride;4373-34-6
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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 |
258°C (rough estimate)
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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
|
| Heavy Atom Count |
26
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| Complexity |
606
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
C[C@H]1[C@H]2CN3CCC4=C([C@@H]3C[C@@H]2C(=CO1)C(=O)OC)NC5=CC=CC=C45
|
| 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
|
| 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 |
| 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 : ~5.56 mg/mL (~15.78 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.56 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (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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