| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
mGlu2R (EC50 = 0.35 microM) and mGlu3R (EC50 = 0.09 microM). Also is a competitive antagonist at group I mGluRs (IC50: mGlu1R = 389 microM; mGlu5R = 630 microM) and group III mGluRs (IC50: mGlu4R = 22.5 microM, mGlu6R = 39.6 microM, mGlu7R = 40.1 microM, mGlu8R = 32 microM). Also acts as an NMDA receptor agonist in rat cortical slices.
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| ln Vitro |
In rat cortical slices, DCG-IV is likewise an NMDA receptor agonist [3].
Potent agonist at mGlu2R (EC50=0.35 microM) and mGlu3R (EC50=0.09 microM). Competitive antagonist at group I (IC50 ~389-630 microM) and group III (IC50 ~22.5-40.1 microM) mGluRs. Also acts as an NMDA receptor agonist in rat cortical slices. These overlapping activities make DCG-IV a useful but complex pharmacological tool. |
| ln Vivo |
Intraperitoneal injection of DCG-IV (1–10 mg/kg) reduces the hypermotility produced by phencyclidine (PCP) [4].
In mice, DCG-IV (1-10 mg/kg; intraperitoneal) depresses phencyclidine (PCP)-induced hyperlocomotion. Specific anticonvulsant or neuroprotective in vivo models are referenced but not detailed in standard summaries. DCG-IV may have protective effects against excitotoxicity, though its NMDA agonist activity could limit its therapeutic window. |
| Enzyme Assay |
Dose-response / animal model: Detailed experimental protocols not provided. PCP-induced locomotor activity in male ICR mice (~40 g): DCG-IV (1, 5, or 10 mg/kg) administered intraperitoneally 30 min before PCP. Locomotor activity measured for 60 min in automated activity chambers (photocell beam breaks). Hyperlocomotion depressed at 5 and 10 mg/kg.
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| Cell Assay |
Radioligand binding assays: Membranes from CHO cells expressing recombinant rat mGlu receptors (group I, II, III) incubated with [3H]-agonist (e.g., [3H]-glutamate) and varying DCG-IV concentrations. For antagonist mode, [3H]-antagonist (e.g., [3H]-LY341495) used. IC50/Ki values calculated from competitive displacement curves. Not all subtypes have detailed protocols; binding data are typically derived from literature (Brabet et al., 1998).
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| Animal Protocol |
Animal/Disease Models: Male ICR mice weighing approximately 40 g (PCP-induced locomotor activity) [4]
Doses: 10, 5 or 1 mg/kg Route of Administration: intraperitoneally (ip) (ip) Experimental Results: Animals had diminished spontaneous activity at 10 or 5 mg/kg. Functional GTPgammaS assays: Membranes from CHO cells expressing recombinant mGlu2R/mGlu3R incubated with [3⁵S]-GTPgammaS, GDP, and varying DCG-IV concentrations. Agonist activity measured by increase in [3⁵S]-GTPgammaS binding (G-protein activation). EC50 values for mGlu2R (0.35 microM) and mGlu3R (0.09 microM) derived from concentration-response curves. NMDA receptor agonist activity confirmed in rat cortical slice electrophysiology. |
| ADME/Pharmacokinetics |
PCP-induced hyperlocomotion in mice: Male ICR mice weighing about 40 g. DCG-IV (1, 5, or 10 mg/kg; intraperitoneal) administered 30 minutes before phencyclidine (PCP) injection. Locomotor activity measured for 60 minutes using automated activity chambers (photocell beam breaks). Hyperlocomotion depressed at 5 and 10 mg/kg doses; spontaneous activity reduced at these doses. At 10 mg/kg, hyperlocomotion significantly reduced vs control.
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| Toxicity/Toxicokinetics |
PK data specific to DCG-IV are not detailed in standard references. As a polar amino acid derivative, it is likely water-soluble and has limited blood-brain barrier penetration following systemic administration. Direct CNS administration (intracerebroventricular, intrathecal, intrastriatal) is often used in studies to achieve brain exposure.
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| References |
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| Additional Infomation |
DCG-IV induces neurotoxicity in a dose-dependent manner in rat brain. Doses as low as 5 nmol cause toxicity (as measured by GAD mRNA and apoptosis), while 0.5 nmol induces no toxicity. At 50 nmol, DCG-IV causes repetitive seizures and selective neuronal damage in cingulate cortex, lateral septum, and hippocampus. Harmful if swallowed; H410 Very toxic to aquatic life with long lasting effects. Precautionary statements: P264 Wash skin thoroughly after handling; P270 Do not eat, drink or smoke when using this product.
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| Molecular Formula |
C₇H₉NO₆
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|---|---|
| Molecular Weight |
203.15
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| Exact Mass |
203.043
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| CAS # |
147782-19-2
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| PubChem CID |
5310979
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| Appearance |
White to off-white solid powder
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| Density |
1.819 g/cm3
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| Boiling Point |
503.9ºC at 760 mmHg
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| Flash Point |
258.5ºC
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| Vapour Pressure |
1.61E-11mmHg at 25°C
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| Index of Refraction |
1.643
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| LogP |
-4.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
281
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| Defined Atom Stereocenter Count |
3
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| SMILES |
[C@@H]1([C@@H](C1[C@@H](C(=O)O)N)C(=O)O)C(=O)O
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| InChi Key |
MATPZHBYOVDBLI-JJYYJPOSSA-N
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| InChi Code |
InChI=1S/C7H9NO6/c8-4(7(13)14)1-2(5(9)10)3(1)6(11)12/h1-4H,8H2,(H,9,10)(H,11,12)(H,13,14)/t2-,3-,4+/m1/s1
|
| Chemical Name |
(1R,2R)-3-[(S)-amino(carboxy)methyl]cyclopropane-1,2-dicarboxylic acid
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| Synonyms |
DCGIV DCG IV
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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 | 4.9225 mL | 24.6124 mL | 49.2247 mL | |
| 5 mM | 0.9845 mL | 4.9225 mL | 9.8449 mL | |
| 10 mM | 0.4922 mL | 2.4612 mL | 4.9225 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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