1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. LY2119620

LY2119620 

Cat. No.: HY-15885 Purity: 99.74%
Handling Instructions

LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.

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

LY2119620 Chemical Structure

LY2119620 Chemical Structure

CAS No. : 886047-22-9

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10 mM * 1 mL in DMSO USD 154 In-stock
Estimated Time of Arrival: December 31
5 mg USD 140 In-stock
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10 mg USD 220 In-stock
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25 mg USD 420 In-stock
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50 mg USD 760 In-stock
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100 mg USD 1360 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.

IC50 & Target

M2/M4 receptor[1]

In Vitro

LY2119620 shows a modest allosteric agonism of 23.2±2.18% and 16.8±5.01% at the M2 and M4 receptors, respectively. Minimal allosteric agonism (<20%) is observed for LY2119620 at the M1, M3, and M5 receptors. The variable KB of LY2119620 for the allosteric binding site on the unoccupied receptor is found to be consistently about 1.9 to 3.4 µM. Results show a Bmax increase at the M2 receptor from 793±1.95 fmol/mg to 2850±162 fmol/mg upon addition of 10 µM LY2119620, and about a 5-fold increase in Bmax at the M4 receptor, 284±18.3 fmol/mg to 1340±42.2 fmol/mg[1].

Molecular Weight

437.94

Formula

C₁₉H₂₄ClN₅O₃S

CAS No.

886047-22-9

SMILES

NC1=C(C(NC2CC2)=O)SC3=C1C(C)=C(Cl)C(OCC(N4CCN(C)CC4)=O)=N3

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 : 67.5 mg/mL (154.13 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2834 mL 11.4171 mL 22.8342 mL
5 mM 0.4567 mL 2.2834 mL 4.5668 mL
10 mM 0.2283 mL 1.1417 mL 2.2834 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 (5.71 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

[3H]LY2119620 equilibrium binding is achieved by incubating 15 µg membranes, orthosteric ligand (100 µM), and various concentrations of [3H]LY2119620 (0.2 to 60 nM) for 1 hour at 25°C. The specific binding versus time data are fit to a one-site specific binding model, and the Bmax and Kd for the allosteric molecule are calculated for each orthosteric ligand[1].

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

References

Purity: 99.74%

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Keywords:

LY2119620LY 2119620LY-2119620mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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Product name:
LY2119620
Cat. No.:
HY-15885
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