| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
mGlu4/glutamate receptor
|
|---|---|
| References | |
| Additional Infomation |
Glutamate is a major excitatory neurotransmitter in the central nervous system (CNS), exerting its neuroregulatory effects by activating metabolite glutamate (mGlu) receptors. Currently, eight mGlu receptor subtypes (mGlu1-8) are known, widely distributed throughout the brain and classified into three groups (I-III) based on signaling pathways and pharmacological characteristics. Group III mGlu receptors (mGlu4/6/7/8) are primarily (but not entirely) located at the presynaptic terminals, acting as both autoreceptors and heteroreceptors, inhibiting neurotransmitter release. Until recently, our understanding of the mechanisms of action of each group III mGlu receptor subtype remained limited due to a lack of subtype-selective pharmacological tools. However, recent years have seen significant progress in the development of ortho- and allosteric compounds targeting group III mGlu receptors, prompting in-depth research into the potential functional roles of these receptors in the CNS and revealing their associations with various pathological conditions, such as epilepsy, anxiety disorders, and Parkinson's disease. The heterogeneous expression of group III mGlu receptor subtypes in the brain, and their different distributions in glutamatergic and GABAergic synapses, make them ideal therapeutic targets. This article reviews the latest advances in subtype-selective pharmacology and explores the individual physiological roles of group III mGlu receptors and their potential roles in diseases. [1]
|
| Molecular Formula |
C6H12NO5P
|
|---|---|
| Molecular Weight |
209.14
|
| Exact Mass |
418.091
|
| CAS # |
103439-17-4
|
| PubChem CID |
146156284
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.398
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
26
|
| Complexity |
274
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C1CC(CC1P(=O)(O)O)(C(=O)O)N.C1CC(CC1P(=O)(O)O)(C(=O)O)N
|
| InChi Key |
GLBQBTFFQHNHGC-OIKBUBQJSA-N
|
| InChi Code |
InChI=1S/2C6H12NO5P/c2*7-6(5(8)9)2-1-4(3-6)13(10,11)12/h2*4H,1-3,7H2,(H,8,9)(H2,10,11,12)/t2*4?,6-/m10/s1
|
| Chemical Name |
(1S)-1-amino-3-phosphonocyclopentane-1-carboxylic acid;(1R)-1-amino-3-phosphonocyclopentane-1-carboxylic acid
|
| Synonyms |
103439-17-4; (+/-)-1-AMINO-TRANS-3-PHOSPHONO-CYCLOPEN TANE CARBO; (1S,3R)-1-amino-3-phosphonocyclopentane-1-carboxylic acid;(1R,3S)-1-amino-3-phosphonocyclopentane-1-carboxylic acid; AKOS024457506; (1R,3S)-1-amino-3-phosphonocyclopentanecarboxylic acid
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 4.7815 mL | 23.9074 mL | 47.8149 mL | |
| 5 mM | 0.9563 mL | 4.7815 mL | 9.5630 mL | |
| 10 mM | 0.4781 mL | 2.3907 mL | 4.7815 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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