[CAS NO. 918407-35-9] Avoralstat

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PRODUCTS SPECIFICATIONS [918407-35-9]

Catalog

HY-16735

Brand

MCE

CAS

918407-35-9

DESCRIPTION [918407-35-9]

Overview

MDL	MFCD28502152
Molecular Weight	513.54
Molecular Formula	C28H27N5O5
SMILES	O=C(C1=NC(C(NCC2CC2)=O)=CC=C1C3=CC(OC)=C(C=C)C=C3C(NC4=CC=C(C(N)=N)C=C4)=O)O

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

4 Publications Citing Use of MCE

Summary

Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research ^[1] ^[2] .

In Vitro

C1 inhibitor (C1INH) is the primary regulator of contact activation, both by inhibiting the conversion of prekallikrein to plasma kallikrein (PKK) by FXIIa, and by directly inhibiting PKK. PKK cleaves high molecular weight kininogen, releasing bradykinin, whose actions are responsible for the signs and symptoms of hereditary angioedema (HAE) ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02218294	BioCryst Pharmaceuticals	Hereditary Angioedema	August 2014	Phase 1
NCT02303626	BioCryst Pharmaceuticals	Hereditary Angioedema\|HAE	November 2014	Phase 2\|Phase 3
NCT02670720	BioCryst Pharmaceuticals	Hereditary Angioedema\|HAE	December 2015	Phase 3
NCT01984788	BioCryst Pharmaceuticals	Hereditary Angioedema	November 2013	Phase 2
NCT02125162	BioCryst Pharmaceuticals	Hereditary Angioedema	April 2014	Phase 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 : 50 mg/mL ( 97.36 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9473 mL	9.7363 mL	19.4727 mL
5 mM	0.3895 mL	1.9473 mL	3.8945 mL
10 mM	0.1947 mL	0.9736 mL	1.9473 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 (4.87 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

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