B2167-10mg | MRS 2578 [711019-86-2] Clinisciences

Background

MRS 2578 is a potent and insurmountable antagonist of P2Y6 nucleotide receptor with IC50 value of 37nM [1].

MRS 2578, a diisothiocyanate derivative, is an insurmountable antagonist of P2Y6 receptors which are associated with vasoconstriction. Thus MRS 2578 is expected to be used in treatment of vasospasm. In 1321N1 human astrocytes expressing P2Y6 receptors, MRS 2578 inhibits the UDP-induced accumulation of inositol phosphates in a dose-dependent manner. MRS 2578 also inhibits the rat P2Y6 receptor activation with IC50 value of 98nM. These effects are selective. MRS 2578 has no effect on the UTP-induced responses of cells expressing human P2Y2 or P2Y4 receptors. It also has no effect on the 2-MeSADP-induced responses of cells expressing the P2Y1 receptor. Moreover, since the UDP-induced activation of P2Y6 receptor can protect the cells from apoptosis induced by TNFα, MRS 2578 completely blocks the protection of cells [1].

References:
[1] Mamedova L K, Joshi B V, Gao Z G, et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors[J]. Biochemical pharmacology, 2004, 67(9): 1763-1770.

Product Citation

1. Wen RX, Shen H, et al. "P2Y6 receptor inhibition aggravates ischemic brain injury by reducing microglial phagocytosis." CNS Neurosci Ther. 2020;26(4):416-429. PMID:32154670

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	472.68
Cas No.	711019-86-2
Formula	C20H20N6S4
Solubility	insoluble in EtOH; insoluble in H2O; ≥19.75 mg/mL in DMSO
Chemical Name	1-(3-isothiocyanatophenyl)-3-[4-[(3-isothiocyanatophenyl)carbamothioylamino]butyl]thiourea
SDF	Download SDF
Canonical SMILES	C1=CC(=CC(=C1)NC(=S)NCCCCNC(=S)NC2=CC=CC(=C2)N=C=S)N=C=S
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description	MRS2578 is a potent antagonist of P2Y6 receptor with an IC50 value of 37 nM.
Targets	P2Y6
IC50	37 nM

Quality Control

Purity = 98.04%

COA (Certificate Of Analysis)
HPLC (Retest)
NMR (Nuclear Magnetic Resonance) (Retest)
MSDS (Material Safety Data Sheet)
Datasheet

MRS 2578 [711019-86-2]

Referencia B2167-10mg

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Marca : APExBIO Technology