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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.56%
- CAS No.: 1432729-22-0
- 화학식: C21H22F3N5O2
- 분자량:433.43
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
IC50:9.6 nM(mGluR2)[1]
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 1432729-22-0
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Appearance Solid
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분자량 433.43
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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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.
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
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