LY2119620|cas 886047-22-9|DC Chemicals

Cas No.:	886047-22-9
Chemical Name:	3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methyl-1-piperazinyl)-2-oxoethoxy]-thieno[2,3-b]pyridine-2-carboxamide
Synonyms:	LY2119620,LY-2119620,LY 2119620
SMILES:	CN1CCN(C(COC2=C(Cl)C(C)=C3C(SC(C(NC4CC4)=O)=C3N)=N2)=O)CC1
Formula:	C₁₉H₂₄ClN₅O₃S
M.Wt:	437.94
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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

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].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC72037	CHF-6366	CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs.
DC9255	VU0357017	VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
DC9497	VU0152100	VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
DC8153	Umeclidinium bromide	Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).
DCAPI1449	Tiotropium Bromide	Tiotropium Bromide is a muscarinic acetylcholine receptor (mAChR M) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel. This stops signaling between neurons and leads to muscle relaxation.
DC8813	TD-4208	TD-4208 is a potent and selective inhaled muscarinic antagonist with functional lung selectivity and long duration of action in preclinical models of bronchoconstriction.
DC7932	TBPB	TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
DC11208	TAK-071	TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
DC10012	Pirmenol hydrochloride	Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
DC8435	LY2119620	LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.