VU0476406
VU0476406 is a blood-brain barrier-permeable and selective muscarinic acetylcholine receptor subtype 4 (M4) activator with human EC50 of 91.0 nM and human pEC50 of 7.04. VU0476406 potentiates endogenous acetylcholine activity at M4 receptors. VU0476406 can be used for the research of Parkinson's disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1451993-12-6
- 分子式: C21H18FN5OS
- 分子量:407.46
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
mAChR4 91 nM (EC50) |
mAChR4 7.04 (pEC50) |
VU0476406 (Compound 8p) potently acts as a positive allosteric modulator of human M4 receptors in M4/Gqi5-CHO cells, with an EC50 of 91.0 nM and 74% acetylcholine maximum efficacy[1].
VU0476406 potently acts as a positive allosteric modulator of rat, dog, and cynomolgus monkey M4 receptors, with EC50 values of 13.5 nM, 111 nM, and 87.3 nM respectively[1].
VU0476406 is highly selective for M4 receptors, with no detectable activity (EC50 > 30 μM) at rat and human M1-3,5 receptors or dog and cynomolgus monkey M2 receptors[1].
VU0476406 has minimal inhibition of human CYP enzymes, with IC50 values ≥11 μM across tested CYP 1A2, 2C9, 2D6, and 3A4[1].
VU0476406 does not inhibit hERG channels, with an IC50 >33 μM[1].
VU0476406 (48 h) does not induce human CYP 1A2, 2B6, or 3A4 enzymes in cryopreserved human hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
VU0476406 ameliorates deficits in synaptic plasticity and behavior in mice with L-DOPA-induced dyskinesia[1].
VU0476406 (10 mg/kg; p.o.; daily; 4 days) shows little to no auto-induction in Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Cynomolgus monkey (non-human primate; L-DOPA-induced dyskinesia model)[1]
-
Dosage:10 mg/kg
-
Administration:i.v.; single dose
-
Result:Significantly reduced dyskinesia scores and involuntary movements.
-
Animal Model:Sprague-Dawley rat[1]
-
Dosage:10 mg/kg
-
Administration:p.o.; daily; 4 days
-
Result:Exhibited a day 4 versus day 1 AUC0-∞ ratio of 0.77, indicating little to no auto-induction in vivo.
化学情報
-
CAS 番号 1451993-12-6
-
分子量 407.46
-
分子式 C21H18FN5OS
-
SMILES
O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(C4=CC=CN=C4F)C=C3
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
VU0476406 関連分類
HY-183203 関連分類
Powered by Bioz