VU6077564
VU6077564 is a reversible competitive antagonist of M1 mAChR, with an IC50 of 31 nM in human (CHO cells) and 39.5 nM in rats. VU6077564 promotes axon growth of sensory neurons from adult rat dorsal root ganglia cultured in vitro. VU6077564 can be used for the research of peripheral neuropathy.
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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。
- 分子式: C26H27FN6O3S
- 分子量:522.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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mAChR1 |
VU6077564 potently and selectively inhibits the human M1 muscarinic acetylcholine receptor in hM1-CHO cells, with an hM1 IC50 of 31 nM[1].
VU6077564 (10-point serial dilution curves) potently inhibits rat M1 muscarinic acetylcholine receptors, with an rM1 IC50 of 39.5 nM and an rM1 KB of 12 nM[1].
VU6077564 (0-1000 nM; 42 h) promotes axonal growth in cultured adult rat DRG sensory neurons, with an ED50 of 55 nM. It achieves a maximum 2-fold induction effect at 1000 nM without reducing neuronal viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CLplasma | Vss | T1/2 (Elimination) |
|---|---|---|---|---|---|
| Rat[1] | 0.2 mg/kg | i.v. | 71.7 mL/min/kg | 27.6 L/kg | 35.2 h |
化学情報
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分子量 522.59
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分子式 C26H27FN6O3S
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SMILES
O=S(C1=C2C=CC=NC2=C(F)C=C1)(N[C@H]3C[C@@H](C(N4[C@@H](C)CN(C5=NC(C)=C(C#N)C=C5)CC4)=O)C3)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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)
- VU6077564
- VU 6077564
- VU-6077564
- mAChR
- peripheral neuropathy
- MDCKII-MDR1 P-gp
- P-glycoprotein
- hM1-CHO cells
- adult rat DRG sensory neurons
- human M1 muscarinic acetylcholine receptor
- adult rat dorsal root ganglia sensory neurons
- M1 mAChR
- central nervous system
- rat M1 muscarinic acetylcholine receptor
- Inhibitor
- inhibitor
- inhibit