(S)-3,4-DCPG
Based on 1 Customer Validation
(S)-3,4-DCPG ((S)-3,4-Dicarboxyphenylglycine) is a potent and selective mGlu8a receptor agonist with an EC50 of 31 nM for human mGlu8a. (S)-3,4-DCPG inhibits Forskolin (HY-15371)-stimulated cAMP formation by activating mGlu8, and modulates presynaptic glutamatergic transmission and synaptic plasticity. (S)-3,4-DCPG can be used in research on inflammatory pain, neuropathic pain, autism spectrum disorder, and glutamatergic synaptic plasticity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98%
- CAS 番号: 201730-11-2
- 分子式: C10H9NO6
- 分子量:239.18
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
hmGluR8a 31 nM (EC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
<100 μM
Compound: 10
|
Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active
Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active
|
[PMID: 15801843] |
| HEK293 | EC50 |
8.8 μM
Compound: 10
|
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
|
[PMID: 15801843] |
体外実験
(S)-3,4-DCPG ((S)-3,4-Dicarboxyphenylglycine) (≤ 100 μM) selectively activates mGlu8a in RGT (AV12-664) cells expressing human mGlu1-8, and inhibits forskolin-stimulated cAMP formation. It has an EC50 of 31 nM for mGlu8a, while the EC50 values for mGlu4a, mGlu6 and mGlu7a are 8.8 μM, 3.6 μM and > 100 μM, respectively, demonstrating its selectivity for mGlu8a[1].
(S)-3,4-DCPG (0.5-400 μM; 5 min) inhibits the fast component of dorsal root-evoked ventral root potential (fDR-VRP) in spinal cord preparations from neonatal rats, producing a biphasic concentration-response curve. The EC50 values of the high-affinity and low-affinity components are 1.3 μM and 391 μM, respectively, with the high-affinity component mainly mediated by mGlu8[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
(S)-3,4-DCPG (30 or 60 mg/kg; 15 min prior to carrageenan; i.p.) increases the thermal withdrawal latency and mechanical withdrawal threshold in the carrageenan (HY-125474) inflammatory pain model, whereas administration of (S)-3,4-DCPG at 1 h after carrageenan treatment exerts no significant effect[2].
(S)-3,4-DCPG (60 mg/kg; single dose; i.p.) increases paw withdrawal latency to heat and mechanical paw withdrawal threshold on day 3 after chronic constriction injury of the sciatic nerve, thereby alleviating thermal hyperalgesia and mechanical allodynia, but exerts no significant effect on day 7 post-injury[2].
(S)-3,4-DCPG (1 μM/0.5 μL per side; intra-DG) reverses the reduced social novelty preference index (SNPI) in prenatal VPA-induced Wistar rat models of autism, and enhances fEPSP LTP in the PP-DG pathway of VPA-exposed rats, while inhibiting LTP in normal control rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Swiss-Webster mice, formalin-induced pain model[2]
-
Dosage:10, 30, 60 mg/kg; 15 min before formalin
-
Administration:i.p.; single dose
-
Result:Dose-dependently decreased early and late nociceptive behaviors; the effect of 60 mg/kg was blocked by intra-PAG MSOP.
-
Animal Model:Male Swiss-Webster mice, formalin-induced pain model[2]
-
Dosage:10, 30, 60 mg/kg; 15 min before formalin
-
Administration:i.p.; single dose
-
Result:Dose-dependently decreased the late hyperalgesic phase.
-
Animal Model:Male Swiss-Webster mice, carrageenan-induced inflammatory pain model[2]
-
Dosage:30, 60 mg/kg; 15 min before carrageenan
-
Administration:i.p.; single dose
-
Result:Increased thermal withdrawal latency and mechanical withdrawal threshold; the 60 mg/kg effect was blocked by intra-PAG MSOP.
化学情報
-
CAS 番号 201730-11-2
-
性状 Solid
-
分子量 239.18
-
分子式 C10H9NO6
-
Color White to light yellow
-
SMILES
OC(C1=C(C=CC([C@H](N)C(O)=O)=C1)C(O)=O)=O
-
別名
(S)-3,4-Dicarboxyphenylglycine
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 20 mg/mL (83.62 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
-
Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
純度とドキュメンテーション
-
データシート (288 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Thomas NK, et al. (S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord. Neuropharmacology. 2001 Mar;40(3):311-8. [Content Brief]
[2]. Gholipour P, et al. Effects of (S)-3,4-DCPG, an mGlu8 receptor agonist, on hippocampal long-term potentiation at perforant pathway-dentate gyrus synapses in prenatal valproic acid-induced rat model of autism. Scientific reports. 2024 Jun 07;14(1):13168. [Content Brief]
[3]. Marabese I, et al. Effects of (S)-3,4-DCPG, an mGlu8 receptor agonist, on inflammatory and neuropathic pain in mice. Neuropharmacology. 2007 Feb;52(2):253-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.1810 mL | 20.9048 mL | 41.8095 mL | 104.5238 mL |
| 5 mM | 0.8362 mL | 4.1810 mL | 8.3619 mL | 20.9048 mL | |
| 10 mM | 0.4181 mL | 2.0905 mL | 4.1810 mL | 10.4524 mL | |
| 15 mM | 0.2787 mL | 1.3937 mL | 2.7873 mL | 6.9683 mL | |
| 20 mM | 0.2090 mL | 1.0452 mL | 2.0905 mL | 5.2262 mL | |
| 25 mM | 0.1672 mL | 0.8362 mL | 1.6724 mL | 4.1810 mL | |
| 30 mM | 0.1394 mL | 0.6968 mL | 1.3937 mL | 3.4841 mL | |
| 40 mM | 0.1045 mL | 0.5226 mL | 1.0452 mL | 2.6131 mL | |
| 50 mM | 0.0836 mL | 0.4181 mL | 0.8362 mL | 2.0905 mL | |
| 60 mM | 0.0697 mL | 0.3484 mL | 0.6968 mL | 1.7421 mL | |
| 80 mM | 0.0523 mL | 0.2613 mL | 0.5226 mL | 1.3065 mL |
(S)-3,4-DCPG 関連分類
HY-107516 関連分類
Powered by Bioz