| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Natural alkaloid
The primary molecular target of Methyl reserpate is the vesicular monoamine transporter (VMAT). It inhibits norepinephrine transport into chromaffin granules. The compound competitively inhibits VMAT with a Ki of 38 nM without triggering depletion or exocytosis. It is a reversible inhibitor of VMAT2, distinguishing it from reserpine's irreversible inhibition. |
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| ln Vitro |
Forty-three indole alkaloids were isolated from 7 kg Rauwolfia vomitoria stem bark; 39 were identified and 2 partially characterised. At least 72 alkaloids classified into 19 types occur in the plant and the interrelationship of the alkaloids and their distribution throughout the plant has been discussed. The major alkaloids of the stems were heteroyohimbines (especially reserpiline) and Na-demethyldihydroindoles [1].
Methyl reserpate inhibits norepinephrine transport into chromaffin vesicles in a concentration-dependent manner. It acts as a competitive inhibitor of VMAT2, with a Ki of 38 nM. The compound is used in pharmacological research to study catecholamine storage and vesicular monoamine transporters in both in vitro and ex vivo experimental models. |
| ln Vivo |
In vivo, Methyl reserpate exhibits prolonged antihypertensive effects with little risk of central nervous system depression. It was investigated as an antihypertensive medicine. The compound lacks the profound CNS-depleting effects of reserpine, making it useful for dissecting structure-activity relationships.
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| Enzyme Assay |
For VMAT2 binding assays, membranes from cells expressing recombinant VMAT2 or chromaffin granules are incubated with [3H]reserpine and increasing concentrations of Methyl reserpate. Nonspecific binding is determined with excess unlabeled reserpine. Bound radioactivity is quantified by filtration and scintillation counting.
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| Cell Assay |
For in vitro monoamine uptake assays, chromaffin granules or VMAT2-expressing cells are incubated with radiolabeled norepinephrine and Methyl reserpate. Vesicular uptake is measured by filtration and scintillation counting. Monoamine content in tissue slices is measured by HPLC.
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| Animal Protocol |
For in vivo antihypertensive studies, hypertensive rats or dogs receive Methyl reserpate by oral or intraperitoneal administration. Blood pressure is measured by tail-cuff plethysmography or intra-arterial catheters. Tissue monoamine content is measured by HPLC to confirm VMAT inhibition.
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| Toxicity/Toxicokinetics |
The oral LD50 in rats was 479 mg/kg (French patent application document No. 2390163); the oral LD50 in mice was 210 mg/kg (French patent application document No. 2390163); and the intravenous LD50 in mice was 48 mg/kg (French patent application document No. 2390163).
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| References | |
| Additional Infomation |
Reserpine methyl ester is a monoterpenoid indole alkaloid.
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| Molecular Formula |
C23H30N2O5
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|---|---|
| Molecular Weight |
414.502
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| Exact Mass |
414.215
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| Elemental Analysis |
C, 66.65; H, 7.30; N, 6.76; O, 19.30
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| CAS # |
2901-66-8
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| PubChem CID |
73532
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.32g/cm3
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| Boiling Point |
587.8ºC at 760 mmHg
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| Flash Point |
309.3ºC
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| Vapour Pressure |
1.17E-14mmHg at 25°C
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| Index of Refraction |
1.634
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| Source |
Originated from plants: Apocynaceae Rauvolfia vomitoria Afzel.
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| LogP |
2.218
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
647
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| Defined Atom Stereocenter Count |
6
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| SMILES |
COC(C1C(OC)C(O)CC2C1CC1C3NC4C=C(OC)C=CC=4C=3CCN1C2)=O
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| InChi Key |
MDJQWFFIUHUJSB-UQVJXISSSA-N
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| InChi Code |
InChI=1S/C23H30N2O5/c1-28-13-4-5-14-15-6-7-25-11-12-8-19(26)22(29-2)20(23(27)30-3)16(12)10-18(25)21(15)24-17(14)9-13/h4-5,9,12,16,18-20,22,24,26H,6-8,10-11H2,1-3H3/t12-,16+,18-,19-,20+,22+/m1/s1
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| Chemical Name |
methyl (1R,15S,17R,18R,19S,20S)-17-hydroxy-6,18-dimethoxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate
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| Synonyms |
NSC-81464; NSC 81464; Methyl reserpate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4125 mL | 12.0627 mL | 24.1255 mL | |
| 5 mM | 0.4825 mL | 2.4125 mL | 4.8251 mL | |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4125 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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