2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. VU6033685

VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%.

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VU6033685 Chemical Structure

VU6033685 Chemical Structure

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VU6033685 Related Antibodies

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Description

VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%[1].

IC50 & Target

EC50: human mGlu5 (39 nM); human mGlu5 (3960 nM)
IC50: CYP1A2 (26 μM); CYP2C9 (22.3 μM); CYP2D6 (23.8 μM)
Molecular Weight

366.84

Formula

C20H19ClN4O
SMILES

CC1=NC(C2CC2)=CC=C1CNC(C3=CC(N4C=CC=N4)=CC=C3Cl)=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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VU6033685 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:

VU6033685VU 6033685VU-6033685mGluRMetabotropic glutamate receptorsorally activePAMSprague–Dawley ratInhibitorinhibitorinhibit

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