Ro4491533
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 579482-31-8
- 화학식: C24H20F3N3O
- 분자량:423.43
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
<0.01 μM
Compound: 7am
|
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
| CHO | IC50 |
<0.01 μM
Compound: 7am
|
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
| CHO | IC50 |
0.003 μM
Compound: 7am
|
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
|
[PMID: 20971004] |
| CHO | IC50 |
0.014 μM
Compound: 7am
|
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
Chemical Information
-
CAS No. 579482-31-8
-
분자량 423.43
-
화학식 C24H20F3N3O
-
SMILES
O=C1NC2=CC(C(F)(F)F)=C(C=C2N=C(C1)C3=CC=CC(C4=CC(C)=NC(C)=C4)=C3)C
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)