1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. ML375

ML375 (Synonyms: VU0483253)

Cat. No.: HY-12567
Handling Instructions

ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4.

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

ML375 Chemical Structure

ML375 Chemical Structure

CAS No. : 1488362-55-5

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4[1].

In Vitro

ML375 possesses high metabolic stability with low hepatic microsomal intrinsic clearance (CLint; human 2.6 mL/min/kg, cynomolgus monkey (cyno), 20 mL/min/kg, rat, 24 mL/min/kg) and a corresponding low predicted hepatic clearance in multiple species (CLhep; human, 2.3 mL/min/kg, cyno, 14 mL/min/kg rat, 18 mL/min/kg)[1].

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

In Vivo

ML375 (10-30 mg/kg; i.p.; once) attenuates both the reinforcing effects and the relative strength of cocaine[2].
ML375 exhibits low clearance (CLp, 2.5 mL/min/kg) and a long elimination half-life (T1/2, 80 hr) in rodents (male, Sprague-Dawley rat, 1 mg/kg IV,) and nonhuman primates (male, cynomolgus monkey, 1 mg/kg, CLp, 3.0 mL/min/kg, T1/2, 10 hr)[1].
ML375 also demonstrates high oral bioavailability (%F, 80) following administration of a suspension-dose to male SD rats with a maximal plasma concentration (Cmax) of 1.4 μM and a corresponding time to reach Cmax (Tmax) of 7 hours[1].

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

Animal Model: Male Sprague-Dawley rats (70 days old; 260-300 g) injected with cocaine[2]
Dosage: 10 mg/kg, 30 mg/kg
Administration: i.p.; once
Result: Produced dose-related reductions in cocaine self-administration.
Molecular Weight

424.83

Formula

C₂₃H₁₅ClF₂N₂O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ML375
Cat. No.:
HY-12567
Quantity:
MCE Japan Authorized Agent: