[CAS NO. 1801253-04-2] LSP-249

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PRODUCTS SPECIFICATIONS [1801253-04-2]

Catalog

HY-126378

Brand

MCE

CAS

1801253-04-2

DESCRIPTION [1801253-04-2]

Overview

MDL	-
Molecular Weight	431.92
Molecular Formula	C24H22ClN5O
SMILES	O=C(C1=CC(CC2=CC=C3N=CC(Cl)=CC3=C2)=NC=C1)NCC4=C(C)C=C(N)N=C4C

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

Summary

LSP-249 (example 35), extracted from patent WO2016011209A1, is a plasma kallikrein inhibitor under the study for angioedema, with an EC ₅₀ less than 100 nM in cell ^[1] .

IC50 & Target

EC50：< 100 nM (kallikrein in cell) ^[1] .

Appearance

Solid

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 : 31.25 mg/mL ( 72.35 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3152 mL	11.5762 mL	23.1524 mL
5 mM	0.4630 mL	2.3152 mL	4.6305 mL
10 mM	0.2315 mL	1.1576 mL	2.3152 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (4.82 mM); Suspended solution; Need ultrasonic
3.

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

Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Andrew Mcdonald, et al. Therapeutic inhibitory compounds. Patent. WO2016011209A1.