2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU6019650

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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VU6019650 Chemical Structure

VU6019650 Chemical Structure

CAS No. : 2926782-31-0

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Based on 1 publication(s) in Google Scholar

VU6019650 Related Antibodies

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Description

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)[1][2].

IC50 & Target[1][2]

mAChR5

36 nM (IC50)

In Vitro

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.

VU6019650 Related Antibodies
In Vivo

VU6019650 (10-56.6 mg/kg; i.p.; single dose) inhibits the rewarding effects of Oxycodone and reduces oxycodone self-administration in rats[1].

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.

Animal Model: Oxycodone-induced rats[1]
Dosage: 10 mg/kg, 30 mg/kg, and 56.6 mg/kg in 10% Tween
Administration: Intraperitoneal injection; single dose
Result: Dose dependently reduced the number of reinforcers earned when Oxycodone is self-administered at a dose of 56.6 μg/kg/infusion.
Molecular Weight

411.51

Formula

C18H22FN3O3S2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC2=C(OCC2)C=C1)(N(CC[C@@H]3CSC4=NC=CN4C)C[C@@H]3F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4301 mL 12.1504 mL 24.3007 mL
5 mM 0.4860 mL 2.4301 mL 4.8601 mL
View the 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.

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Purity & Documentation
References

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
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VU6019650 Related Classifications

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:

VU60196502926782-31-0VU 6019650VU-6019650mAChRMuscarinic acetylcholine receptorM5 mAChRopioid use disorderventral tegmental areaInhibitorinhibitorinhibit

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