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.
For research use only. We do not sell to patients.
- Purity: 99.56%
- CAS No.: 1432729-22-0
- Formula: C21H22F3N5O2
- Molecular Weight:433.43
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Storage: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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50:9.6 nM(mGluR2)[1]
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.
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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.
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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Molecular Weight 433.43
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Formula C21H22F3N5O2
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (273 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-8768 Related Classifications
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