| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| Other Sizes |
| Targets |
mGluR1 3.92 (pEC50) mGluR2 3.9 (pEC50) mGluR4 2.7 (pEC50) mGluR5 4.6 (pEC50) mGluR6 4.0 (pEC50) mGluR8 3.94 (pEC50) Human Endogenous Metabolite
mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, mGluR8; NMDA receptors; PLD-coupled metabotropic receptors. |
|---|---|
| ln Vitro |
An endogenous agonist of a metabotropic receptor, L-cysteinesulfinic acid is linked to the stimulation of phospholipase D (PLD) activity. The PLD-coupled metabotropic excitatory amino acid (EAA) receptor is endogenously agonistic to L-CSA. PLD-coupled receptors are preferentially activated by L-CSA. In hippocampal slices, 1 mM concentrations of L-CSA significantly increases PLD activity, while 1 mM concentrations of L-glutamate, L-aspartate, and L-HCA have no impact. When iGluR antagonists are present, L-CSA causes a dose-dependent rise in PLD activity in rat hippocampus slices, with an estimated EC50 of 500 uM. In the presence of 1 uM tetrodotoxin, the PLD response elicited by 1 mM L-CSA does not significantly diminish, indicating that this response is independent of L-CSA-induced increases in cell firing[1].
L-Cysteinesulfinic acid is a potent agonist at rat mGluRs with pEC50 values of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively. This broad-spectrum agonist activity makes it useful for studying mGluR-mediated signaling pathways, though its lack of selectivity limits its use in dissecting individual receptor subtypes. |
| ln Vivo |
As an endogenous agonist, L-Cysteinesulfinic acid plays a physiological role in modulating excitatory neurotransmission. Its in vivo effects are complex due to its activity at multiple receptor types, including NMDA and mGluRs. It can influence synaptic plasticity, neuronal excitability, and potentially contribute to excitotoxic processes when present at elevated levels.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays are performed to determine the affinity of L-Cysteinesulfinic acid for various receptor subtypes. These assays typically use radioligand binding techniques with membrane preparations from cells or tissues expressing the target receptors. The compound's ability to displace specific radiolabeled ligands is measured to calculate its binding affinity (Ki).
|
| Cell Assay |
For in vitro cell-based assays, cells expressing specific mGluR subtypes (e.g., RGT cell lines expressing mGluR1α and mGluR5a) are used. The cells are stimulated with L-Cysteinesulfinic acid, and receptor activation is measured by downstream signaling events such as PI hydrolysis, calcium mobilization, or PLD activity. These functional assays are used to determine the compound's potency (EC50).
|
| Animal Protocol |
In vivo studies are typically conducted in rodents to assess the compound's effects on behavior and physiology. Due to its poor blood-brain barrier penetration, it is often administered directly into the brain via intracerebroventricular (i.c.v.) injection. Its effects on seizure activity, motor function, and cognitive processes can be evaluated to understand the role of excitatory amino acid receptors in these phenomena.
|
| ADME/Pharmacokinetics |
No specific pharmacokinetic data are publicly available for L-Cysteinesulfinic acid. As a polar, endogenous-like amino acid, it is unlikely to have favorable oral bioavailability and may be rapidly metabolized. For research purposes, its disposition is typically studied following direct CNS administration or intravenous injection in animal models.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available. As an endogenous compound, it is generally well-tolerated at physiological concentrations. However, at high concentrations, its agonist activity at NMDA and mGlu receptors could potentially lead to excitotoxicity, which may manifest as neuronal damage or seizure activity.
|
| References |
|
| Additional Infomation |
L-Cysteinesulfinic acid is a valuable tool for studying the pharmacology of excitatory amino acid receptors, particularly mGluRs and NMDA receptors. Its endogenous nature and broad agonist profile make it useful for understanding the physiological roles of these receptors. However, its lack of selectivity limits its application in dissecting specific receptor subtypes. It is not approved for clinical use.
|
| Molecular Formula |
C3H9NO5S
|
|---|---|
| Molecular Weight |
171.17
|
| Exact Mass |
171.02
|
| CAS # |
207121-48-0
|
| Related CAS # |
L-Cysteinesulfinic acid;1115-65-7
|
| PubChem CID |
16211766
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
580.6ºC at 760 mmHg
|
| Melting Point |
163ºC (dec.)(lit.)
|
| Flash Point |
304.9ºC
|
| Vapour Pressure |
2.73E-15mmHg at 25°C
|
| LogP |
0.121
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
10
|
| Complexity |
136
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C([C@@H](C(=O)O)N)S(=O)O.O
|
| InChi Key |
YQIXTMZYGQXTCZ-DKWTVANSSA-N
|
| InChi Code |
InChI=1S/C3H7NO4S.H2O/c4-2(3(5)6)1-9(7)8;/h2H,1,4H2,(H,5,6)(H,7,8);1H2/t2-;/m0./s1
|
| Chemical Name |
(2R)-2-amino-3-sulfinopropanoic acid;hydrate
|
| 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) |
H2O: 41.67 mg/mL (243.44 mM)
|
|---|---|
| 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 | 5.8421 mL | 29.2107 mL | 58.4215 mL | |
| 5 mM | 1.1684 mL | 5.8421 mL | 11.6843 mL | |
| 10 mM | 0.5842 mL | 2.9211 mL | 5.8421 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
