MK-8768
Based on 1 Customer Validation
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
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 : 99.56%
- CAS 番号: 1432729-22-0
- 分子式: C21H22F3N5O2
- 分子量:433.43
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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]
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生物活性
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化学情報
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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
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Help & FAQs
生物活性
製品説明
IC50 & Target
IC50:9.6 nM(mGluR2)[1]
体外実験
MK-8768 (40 nM, 5 min) inhibits the viability of mGluR2 in the overexpress CHOdhfr- cells with a IC50 value of 0.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:CHOdhfr- cells expressing human mGluR2[1]
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Concentration:40 nM
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Incubation Time:5 min
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Result:Inhibits the viability of mGluR2.
体内実験
MK-8768 (3 mg/kg, i.m., twice weekly) improves object retrieval following scopolamine impairment obviously which mains a good executive function and attention in the Rhesus monkey ORD model[1].
Pharmacokinetic Analysis[1]
| Species | Route | Dose (mg/kg) | t1/2 (h) | Clobs (mL·min/kg) | Vss_obs (mL/kg) | F (%) |
| Rat | i.v. | 1 | 3.3 | 24 | 7.3 | 32 |
| Dog | i.v. | 0.25 | 3.3 | 24 | 7.3 | 34 |
| Monkey | i.v. | 0.5 | 1.7 | 22 | 3.2 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rhesus monkey ORD model[2]
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Dosage:3 mg/kg
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Administration:Intramuscular (i.m.), 2 times weekly
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Result:Improved object retrieval following scopolamine impairment obviously at the concentration of 0.3 mg/ml.
化学情報
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CAS 番号 1432729-22-0
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性状 Solid
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分子量 433.43
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分子式 C21H22F3N5O2
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Color White to off-white
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SMILES
NC(C1=NC2=CC(CN3C[C@H](C(F)(F)F)O[C@H](C)C3)=CC=C2C(C4=CN(C)N=C4)=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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 : 50 mg/mL (115.36 mM; Need ultrasonic; 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
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Michael T. Rudd, et al. Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator. ACS Med. Chem. Lett.. 2023，14，8. [Content Brief]
[2]. Sean M Smith, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.Neuropharmacology, 2013 Jan;64:215-23. [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 | 2.3072 mL | 11.5359 mL | 23.0718 mL | 57.6794 mL |
| 5 mM | 0.4614 mL | 2.3072 mL | 4.6144 mL | 11.5359 mL | |
| 10 mM | 0.2307 mL | 1.1536 mL | 2.3072 mL | 5.7679 mL | |
| 15 mM | 0.1538 mL | 0.7691 mL | 1.5381 mL | 3.8453 mL | |
| 20 mM | 0.1154 mL | 0.5768 mL | 1.1536 mL | 2.8840 mL | |
| 25 mM | 0.0923 mL | 0.4614 mL | 0.9229 mL | 2.3072 mL | |
| 30 mM | 0.0769 mL | 0.3845 mL | 0.7691 mL | 1.9226 mL | |
| 40 mM | 0.0577 mL | 0.2884 mL | 0.5768 mL | 1.4420 mL | |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1536 mL | |
| 60 mM | 0.0385 mL | 0.1923 mL | 0.3845 mL | 0.9613 mL | |
| 80 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7210 mL | |
| 100 mM | 0.0231 mL | 0.1154 mL | 0.2307 mL | 0.5768 mL |
MK-8768 関連分類
HY-155088 関連分類
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