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

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 Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 185 In-stock
25 mg USD 390 In-stock
50 mg USD 665 In-stock
100 mg USD 1130 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ML375:

ML375 Related Antibodies

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  • Purity & Documentation

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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].

IC50 & Target

mAChR5

 

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N2[C@@](N(C(C3=CC=C(F)C(F)=C3)=O)CC2)(C4=CC=C(Cl)C=C4)C5=C1C=CC=C5
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 : 40 mg/mL (94.16 mM; Need ultrasonic and warming; 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 2.3539 mL 11.7694 mL 23.5388 mL
5 mM 0.4708 mL 2.3539 mL 4.7078 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

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: 99.70%

COA (261 KB) HNMR (159 KB) RP-HPLC (217 KB) LCMS (370 KB)

Handling Instructions (2659 KB)
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 2.3539 mL 11.7694 mL 23.5388 mL 58.8471 mL
5 mM 0.4708 mL 2.3539 mL 4.7078 mL 11.7694 mL
10 mM 0.2354 mL 1.1769 mL 2.3539 mL 5.8847 mL
15 mM 0.1569 mL 0.7846 mL 1.5693 mL 3.9231 mL
20 mM 0.1177 mL 0.5885 mL 1.1769 mL 2.9424 mL
25 mM 0.0942 mL 0.4708 mL 0.9416 mL 2.3539 mL
30 mM 0.0785 mL 0.3923 mL 0.7846 mL 1.9616 mL
40 mM 0.0588 mL 0.2942 mL 0.5885 mL 1.4712 mL
50 mM 0.0471 mL 0.2354 mL 0.4708 mL 1.1769 mL
60 mM 0.0392 mL 0.1962 mL 0.3923 mL 0.9808 mL
80 mM 0.0294 mL 0.1471 mL 0.2942 mL 0.7356 mL
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ML375 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:

ML3751488362-55-5VU0483253ML 375ML-375VU 0483253VU-0483253mAChRMuscarinic acetylcholine receptorM5negativeallostericmodulatorNAMbrain-penetrantInhibitorinhibitorinhibit

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