| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Valtrate up-regulates GABA_A receptor and GAD65, down-regulates caspase-3, and up-regulates Bcl-2 in the brain of chronic epileptic rats. No significant effect on GABA_B receptor. [2]
|
|---|---|
| ln Vivo |
At dosages of 5, 10, and 20 mg/kg, valepotriate demonstrated strong anti-epileptic action against MES- and PTZ-induced epilepsy, with ED50 values of 7.84 and 7.19 mg/kg for MES- and PTZ-induced epilepsy, respectively. Furthermore, in the sodium pentobarbital-induced sleep time test, the doses of 10 and 20 mg/kg significantly increased sleep duration and decreased latency. Furthermore, valepotriate (5, 10 and 20 mg/kg) has no discernible effect on caspase-3 expression, but it can dramatically up-regulate the expression of GABAA, GAD65, and Bcl-2 and down-regulate the production of caspase-3. Gababu [2].
Valtrate (5, 10, 20 mg/kg, intraperitoneal injection) showed significant anti-epileptic activity in maximal electroshock-induced seizure (MES) model in mice, with ED50 = 7.84 mg/kg. It dose-dependently inhibited convulsions and reduced mortality compared to control. At 20 mg/kg, inhibition rate of convulsions was 80% (P<0.05 vs control). [2] Valtrate (5, 10, 20 mg/kg, i.p.) significantly protected against pentylenetetrazole (PTZ)-induced seizures in mice, with ED50 = 7.19 mg/kg. At 20 mg/kg, inhibition rate of convulsions was 73.3% (P<0.01 vs control) and mortality was 0% (control: 100%). [2] Valtrate (10 and 20 mg/kg, i.p.) significantly prolonged pentobarbital sodium-induced sleeping time in mice and shortened the latency time. At 20 mg/kg, sleeping time was significantly increased (P<0.01 vs control). [2] In a PTZ-induced chronic epileptic rat model (PTZ 32 mg/kg i.p. daily for 28 days), Valtrate (5, 10, 20 mg/kg/d i.p. for 3 weeks) significantly up-regulated GABA_A, GAD65, and Bcl-2 protein expression, and down-regulated caspase-3 expression in brain tissues (P<0.01 vs control, dose-dependent). [2] |
| Animal Protocol |
Maximal electroshock (MES)-induced seizure model in mice: ICR mice (20±2 g) were pretreated intraperitoneally (i.p.) with Valtrate at doses of 5, 10, or 20 mg/kg, or with phenytoin sodium (20 mg/kg) as positive control, or with 1% DMSO (20 mL/kg) as vehicle control. After 30 min, an alternating current stimulus (50 mA, 50 Hz, 1 s duration) was applied. The occurrence of hind limb tonic extension (HLTE) within 10 s after stimulation was recorded. [2]
Pentylenetetrazole (PTZ)-induced epilepsy model in mice: ICR mice (20±2 g) were pretreated i.p. with Valtrate (5, 10, 20 mg/kg), diazepam (4 mg/kg) as positive control, or 1% DMSO (20 mL/kg) as vehicle control. After 30 min, PTZ (90 mg/kg, i.p.) was administered. Animals were observed for 30 min for HLTE. [2] Pentobarbital sodium-induced sleeping time model in mice: ICR mice (20±2 g) were pretreated i.p. with Valtrate (5, 10, 20 mg/kg), diazepam (4 mg/kg) as positive control, or 1% DMSO (20 mL/kg) as vehicle control. After 30 min, pentobarbital sodium (50 mg/kg, i.p.) was given. Latency time (from injection to loss of righting reflex) and sleeping time (from loss to recovery of righting reflex) were recorded. [2] PTZ-induced chronic epileptic rat model: SD rats (200±20 g) were administered PTZ (32 mg/kg, i.p.) once daily in the morning for 28 days to induce chronic epilepsy. After model establishment, rats were treated i.p. with Valtrate (5, 10, 20 mg/kg/d) or 1% DMSO (20 mL/kg/d, control) for 3 weeks. Rats were then sacrificed under anesthesia, and whole brains were collected for protein extraction. [2] |
| Toxicity/Toxicokinetics |
Acute toxicity study in mice: Mice were divided into 7 groups (n=10). Groups 1-6 received Valtrate at doses of 5, 10, 20, 40, 80, and 120 mg/kg (i.p.), respectively. Group 7 received 1% DMSO (20 mL/kg, i.p.) as control. Within 24 h, no death or abnormal neurobehaviors (including ataxia, motor coordination, etc.) were observed. The 50% lethal dose (LD50) could not be determined due to lack of observable toxicity at all tested doses. [2]
|
| References |
|
| Additional Infomation |
Valtratum ester is a fatty acid ester. It has been reported to be found in creeping Valtratum, Sitka Valtratum, and other organisms with relevant data. See also: Viburnum bark (partial).
Background and mechanism: Valtrate (isolated from Valeriana jatamansi Jones) is a key bioactive component of Valeriana. It has been reported to exert anti-proliferative cytotoxic effects by regulating redox balance or suppressing the MAPK pathway in cancer cells. [1] Anti-epileptic mechanism: Valtrate increases GABA_A (an ionotropic receptor related to chloride ion channel, leading to hyperpolarization of nerve cells) and GAD65 (rate-limiting enzyme for GABA synthesis), while having no significant effect on GABA_B (a metabotropic receptor). It also inhibits neuronal apoptosis by up-regulating Bcl-2 (anti-apoptotic) and down-regulating caspase-3 (pro-apoptotic). [2] Indications: The study suggests Valtrate has anti-epileptic activity and may be useful for treating epilepsy. [2] |
| Molecular Formula |
C22H30O8
|
|---|---|
| Molecular Weight |
422.4688
|
| Exact Mass |
422.194
|
| CAS # |
18296-44-1
|
| PubChem CID |
442436
|
| Appearance |
Light brown to brown ointment
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
525.9±50.0 °C at 760 mmHg
|
| Flash Point |
226.5±30.2 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.528
|
| LogP |
2.36
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
30
|
| Complexity |
765
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O1C([H])([H])[C@@]21[C@]([H])(C([H])=C1C(C([H])([H])OC(C([H])([H])[H])=O)=C([H])O[C@]([H])([C@]21[H])OC(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)OC(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O
|
| InChi Key |
BDIAUFOIMFAIPU-KVJIRVJXSA-N
|
| InChi Code |
InChI=1S/C22H30O8/c1-12(2)6-18(24)29-17-8-16-15(9-26-14(5)23)10-27-21(20(16)22(17)11-28-22)30-19(25)7-13(3)4/h8,10,12-13,17,20-21H,6-7,9,11H2,1-5H3/t17-,20+,21-,22+/m0/s1
|
| Chemical Name |
[(1S,6S,7R,7aS)-4-(acetyloxymethyl)-1-(3-methylbutanoyloxy)spiro[6,7a-dihydro-1H-cyclopenta[c]pyran-7,2'-oxirane]-6-yl] 3-methylbutanoate
|
| 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) |
DMSO : ~100 mg/mL (~236.70 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 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 25.0 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: 2.5 mg/mL (5.92 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3670 mL | 11.8352 mL | 23.6703 mL | |
| 5 mM | 0.4734 mL | 2.3670 mL | 4.7341 mL | |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3670 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.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
