VU6019650
Based on 2 publication(s) in Google Scholar
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA).
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- 純度: 99.83%
- CAS 番号: 2926782-31-0
- 分子式: C18H22FN3O3S2
- 分子量:411.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 VU6019650
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生物活性
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mAChR5 36 nM (IC50) |
VU6019650 (0-10 μM) shows high selectivity for M5 (IC50=36 nM) over other subtypes (>100-fold selectivity against human M1-4)[1].
VU6019650 (1 μM) blocks Oxo-M-induced activation of VTA neurons[1].
VU6019650 exhibits brain penetrance with rat brain and plasma Kp, Kp, uu values of 0.27 and 0.43, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis in rats[1]
| Route | Dose (mg/kg) | t(term) (min) | MRT (min) | Cl_obs (mL/min/kg) | Vdss(L/kg) | AUC (ng·h/mL) |
| i.v. | 1 | 876 | 644 | 56.5 | 36.6 | 301 |
| Route | Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | AUG (ng·h/mL) | F (%) | |
| p.o. | 10 | 433 | 0.25 | 830 | 27.6 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Oxycodone-induced rats[1]
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Dosage:10 mg/kg, 30 mg/kg, and 56.6 mg/kg in 10% Tween
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Administration:Intraperitoneal injection; single dose
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Result:Dose dependently reduced the number of reinforcers earned when Oxycodone is self-administered at a dose of 56.6 μg/kg/infusion.
化学情報
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CAS 番号 2926782-31-0
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性状 Solid
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分子量 411.51
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分子式 C18H22FN3O3S2
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Color White to light yellow
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SMILES
O=S(C1=CC2=C(OCC2)C=C1)(N(CC[C@@H]3CSC4=NC=CN4C)C[C@@H]3F)=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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Rep
Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]2025 May 14;44(5):115712. PMID: 40372911 -
Mol Cell Endocrinol
Vagotomy suppresses food intake by increasing GLP-1 secretion via the M3 AChR-AMPKα pathway in mice. [Abstract]2025 Jan 21:599:112464. PMID: 39848433
溶剤 & 溶解度
DMSO : 8.33 mg/mL (20.24 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Garrison AT, et al. Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder. J Med Chem. 2022 Apr 28;65(8):6273-6286. [Content Brief]
[2]. Capstick RA, et al. Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists. Bioorg Med Chem Lett. 2022 Nov 15;76:128988. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4301 mL | 12.1504 mL | 24.3007 mL | 60.7519 mL |
| 5 mM | 0.4860 mL | 2.4301 mL | 4.8601 mL | 12.1504 mL | |
| 10 mM | 0.2430 mL | 1.2150 mL | 2.4301 mL | 6.0752 mL | |
| 15 mM | 0.1620 mL | 0.8100 mL | 1.6200 mL | 4.0501 mL | |
| 20 mM | 0.1215 mL | 0.6075 mL | 1.2150 mL | 3.0376 mL |
VU6019650 関連分類
HY-148502 関連分類
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