2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. MK-8768

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.

MK-8768 Chemical Structure

MK-8768 Chemical Structure

CAS No. : 1432729-22-0

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MK-8768 Related Antibodies

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Description

MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.

IC50 & Target

IC50:9.6 nM(mGluR2)[1]
In Vitro

MK-8768 (40 n M, 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.

MK-8768 Related Antibodies

Cell Viability Assay

Cell Line: CHOdhfr- cells expressing human mGluR2[1]
Concentration: 40 nM
Incubation Time: 5 min
Result: Inhibits the viability of mGluR2.
In Vivo

MK-8768 has a preferred administration of intramuscular (i.m.)[1].
MK-8768 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]

MK-8768 药代动力学分析[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.

Animal Model: Rhesus monkey ORD model[2]
Dosage: 3 mg/kg
Administration: Intramuscular (i.m.), 2 times weekly
Result: Improved object retrieval following scopolamine impairment obviously at the concentration of 0.3 mg/ml.
Molecular Weight

433.43

Formula

C21H22F3N5O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MK-8768 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-87681432729-22-0MK8768MK 8768mGluRMetabotropic glutamate receptorsmGluR2Rhesus monkey ORD modelInhibitorinhibitorinhibit

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