1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. ML380

ML380 

Cat. No.: HY-12439 Purity: 99.91%
Handling Instructions

ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.

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

ML380 Chemical Structure

ML380 Chemical Structure

CAS No. : 1627138-52-6

Size Price Stock Quantity
5 mg USD 85 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR[1][2][3].

IC50 & Target

IC50: 190 nM (hM5), 610 nM (rM5)[1]

In Vitro

ML380 (0.01 nM-100 μM) robustly stimulates inositol phosphate (IP) accumulation and Ca2+ mobilization in CHO-hM5 cells, with pEC50s of 5.33 and 5.71, respectively[2].
ML380 (0.01-30 μM) increases the ACh-stimulated IP accumulation and Ca2+ mobilization in CHO-hM5 cells[2].

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

In Vivo

ML380 (1 mg/kg; i.v.) displays high clearance (66 mL/min/kg), a moderate volume of distribution (1.6 L/kg), and a short half-life (t1/2, 22 min) in rats[1].

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

Molecular Weight

494.53

Formula

C₂₃H₂₅F₃N₄O₃S

CAS No.

1627138-52-6

SMILES

O=C(C1CCN(S(=O)(C2=CC3=C(NN=C3)C=C2)=O)CC1)N(CC)CC4=CC=CC=C4C(F)(F)F

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 : 100 mg/mL (202.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0221 mL 10.1106 mL 20.2212 mL
5 mM 0.4044 mL 2.0221 mL 4.0442 mL
10 mM 0.2022 mL 1.0111 mL 2.0221 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: 2.5 mg/mL (5.06 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.06 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ML380ML 380ML-380mAChRMuscarinic acetylcholine receptorpositiveallostericmodulatorPAMM5AChInhibitorinhibitorinhibit

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Product Name:
ML380
Cat. No.:
HY-12439
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