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LY2119620

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Catalog No. T6575Cas No. 886047-22-9

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

LY2119620

LY2119620

🥰Excellent
Purity: 99.7%
Catalog No. T6575Cas No. 886047-22-9
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
Pack SizePriceAvailabilityQuantity
1 mg$52In Stock
5 mg$125In Stock
10 mg$198In Stock
25 mg$345In Stock
50 mg$483In Stock
100 mg$679In Stock
1 mL x 10 mM (in DMSO)$132In Stock
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Purity:99.7%
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Product Introduction

Bioactivity
Description
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
In vitro
LY2119620 displays modest allosteric agonism and positively modulates the functional G protein–signaling ability of an agonist at the M2/M4 receptor subtypes by placing the M2 and M4 receptors into an active G protein–bound state. LY2119620 enhances the potency of three muscarinic acetylcholine receptor agonists, ACh, Oxo-M and iperoxo. [1] [3H]LY2119620 can be used as a probe for the human M(2) and M(4) muscarinic receptor allosteric binding sites. [2]
Kinase Assay
Biochemical Assay: For IC50 determination, EI1 is serial diluted threefold in DMSO for a total of 12 concentrations, with the starting concentration at 1 μM. The reaction is incubated at room temperature for 120 min, and stopped by adding quench solution (2.5% TFA with 320 nM d4-SAH). SAH production is quantitated using an API 4000 triple quadrupole mass spectrometry with Turbulon Spray coupled with Prominence UFLC. The percentage of inhibition is normalized using positive (no inhibitor) and negative (no enzyme) controls, and IC50 calculated using PRISM. Enzymology studies of S-Adenosyl methionine (SAM) competition are performed with slight modification of reaction condition: 10 μM EI1 is used as the starting dose for serial dilution. SAM is titrated over a range between 1 μM and 50 μM (corresponding to 1 × Km and 50 × Km), and substrate peptide is present in the final reaction mixture at its saturated condition (10 μM). For histone methyltransferase (HMT) profiling in Table 1, all HMTs are purified recombinant proteins from either Escherichia coli or Baculovirus system. The catalytic domain of G9a, SuV39H2, Set7/9, CARM1, SETD8, NSD3, SETD2, and Dot1L, and the full-length SmyD2 protein were used in the biochemical assays. HMT biochemical reactions are carefully characterized with enzymology studies and the SAM and substrate Km determined. The SAM and substrate concentrations are kept at their respective Km for most of the HMTs, except the ones (SmyD2 and Set7/9) with low SAM-Km value, for which 0.5 μM SAM is used. All HMT reactions are performed using the same assay format where the production of SAH from the biochemical reaction is quantitated by LC-MS.
Chemical Properties
Molecular Weight437.94
FormulaC19H24ClN5O3S
Cas No.886047-22-9
SmilesCN1CCN(CC1)C(=O)COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl
Relative Density.1.46 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (114.17 mM)
Ethanol: 10 mg/mL, Heating is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2834 mL11.4171 mL22.8342 mL114.1709 mL
5 mM0.4567 mL2.2834 mL4.5668 mL22.8342 mL
10 mM0.2283 mL1.1417 mL2.2834 mL11.4171 mL
20 mM0.1142 mL0.5709 mL1.1417 mL5.7085 mL
50 mM0.0457 mL0.2283 mL0.4567 mL2.2834 mL
100 mM0.0228 mL0.1142 mL0.2283 mL1.1417 mL

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