VU0448088 (Synonyms: ML253)

Name: VU0448088
Brand: MedChemExpress
SKU: HY-162663
Rating: 4.5 (1 reviews)

Cat. No.: HY-162663 Purity: 98.67%: FAQs
Data Sheet SDS COA Handling Instructions

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VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC₅₀ values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic.

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

VU0448088 Chemical Structure

CAS No. : 1417616-42-2

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

mAChR4

56 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	> 30 μM Compound: 4, ML253 (VU0448088)	Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization	[PMID: 23177787]
CHO-K1	EC₅₀	> 30 μM Compound: 4, ML253 (VU0448088)	Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization	[PMID: 23177787]
CHO-K1	EC₅₀	> 30 μM Compound: 4, ML253 (VU0448088)	Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization	[PMID: 23177787]
CHO-K1	EC₅₀	> 30 μM Compound: 4, ML253 (VU0448088)	Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization	[PMID: 23177787]
CHO-K1	EC₅₀	56 nM Compound: 4, ML253 (VU0448088)	Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization	[PMID: 23177787]

In Vivo

VU0448088 (3, 10, 30, 56.6, 100 mg/kg; i.p.) reverses amphetamine-induced hyperlocomotion in a dose-dependent manner ^[1].

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

Animal Model:	Rat (amphetamine-induced hyperlocomotion)^[1]
Dosage:	3, 10, 30, 56.6, 100 mg/kg
Administration:	IP
Result:	Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, showed a modest reduction of 26% at a dose of 10 mg/kg; at the three highest doses (30, 56.6 and 100 mg/kg), showed significant reductions of 47.9%, 53.7% and 57.3%, respectively.

Molecular Weight

346.83

Formula

C₁₆H₁₅ClN₄OS

CAS No.

1417616-42-2

Appearance

Solid

Color

White to off-white

SMILES

CC1=C(Cl)C(C)=NC2=C1C(N)=C(C(NCC3=CC=NC=C3)=O)S2

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 : 5 mg/mL (14.42 mM; Need ultrasonic; 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	2.8833 mL	14.4163 mL	28.8326 mL
5 mM	0.5767 mL	2.8833 mL	5.7665 mL
10 mM	0.2883 mL	1.4416 mL	2.8833 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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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.67%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (250 KB) HNMR (258 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Le U, et al. Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett. 2013 Jan 1;23(1):346-50. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8833 mL	14.4163 mL	28.8326 mL	72.0814 mL
	5 mM	0.5767 mL	2.8833 mL	5.7665 mL	14.4163 mL
	10 mM	0.2883 mL	1.4416 mL	2.8833 mL	7.2081 mL

VU0448088 Related Classifications

Neurological Disease

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:

VU04480881417616-42-2ML253VU 0448088VU-0448088ML 253ML-253mAChRMuscarinic acetylcholine receptorblood-brain barrierpsychoticamphetamineInhibitorinhibitorinhibit

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VU0448088 (Synonyms: ML253)

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Complete Stock Solution Preparation Table

VU0448088 Related Classifications

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