1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. VU0152099

VU0152099 

Cat. No.: HY-119226 Purity: 98.35%
COA Handling Instructions

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.

For research use only. We do not sell to patients.

VU0152099 Chemical Structure

VU0152099 Chemical Structure

CAS No. : 612514-42-8

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5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
25 mg USD 210 In-stock
Estimated Time of Arrival: December 31
50 mg USD 340 In-stock
Estimated Time of Arrival: December 31
100 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine[1].

In Vitro

VU0152099 (30 µM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 µM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC50 values of 1.2 µM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (270-300 g) injected with Amphetamine[1]
Dosage: 56.6 mg/kg
Administration: i.p.; once
Result: Reversed Amphetamine-induced hyperlocomotion in rats.
Molecular Weight

355.41

Formula

C18H17N3O3S

CAS No.
SMILES

O=C(C1=C(N)C2=C(C)C=C(C)N=C2S1)NCC3=CC=C(OCO4)C4=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (35.17 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8137 mL 14.0683 mL 28.1365 mL
5 mM 0.5627 mL 2.8137 mL 5.6273 mL
10 mM 0.2814 mL 1.4068 mL 2.8137 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (3.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (3.52 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Product Name:
VU0152099
Cat. No.:
HY-119226
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