Hexa-D-arginine (Furin Inhibitor II) is a stable furin inhibitor (antagonist) with Kis of 106 nM, 580 nM and 13.2 μM for furin, PACE4 and PC1 respectively. Hexa-D-arginine blocks the toxicity of Pseudomonas exotoxin A and anthrax toxin both in vitro & in vivo.

Physicochemical Properties

Molecular Formula	C36H75N25O6
Molecular Weight	954.1446
Exact Mass	953.633
CAS #	673202-67-0
Related CAS #	Hexa-D-arginine TFA;958204-56-3
PubChem CID	57358476
Appearance	White to off-white solid powder
LogP	2.303
Hydrogen Bond Donor Count	19
Hydrogen Bond Acceptor Count	13
Rotatable Bond Count	35
Heavy Atom Count	67
Complexity	1750
Defined Atom Stereocenter Count	6
SMILES	C(C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N)N)CN=C(N)N
InChi Key	BMLTZEAFQLJTIZ-TZNXUKFXSA-N
InChi Code	InChI=1S/C36H75N25O6/c37-19(7-1-13-51-31(39)40)26(63)58-21(9-3-15-53-33(43)44)28(65)60-23(11-5-17-55-35(47)48)30(67)61-24(12-6-18-56-36(49)50)29(66)59-22(10-4-16-54-34(45)46)27(64)57-20(25(38)62)8-2-14-52-32(41)42/h19-24H,1-18,37H2,(H2,38,62)(H,57,64)(H,58,63)(H,59,66)(H,60,65)(H,61,67)(H4,39,40,51)(H4,41,42,52)(H4,43,44,53)(H4,45,46,54)(H4,47,48,55)(H4,49,50,56)/t19-,20-,21-,22-,23-,24-/m1/s1
Chemical Name	(2R)-2-amino-N-[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)pentanamide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Hexa-D-arginine can effectively prevent cell lysis mediated by Pseudomonas aeruginosa exotoxin A (PEA) without being harmful by itself [1].
ln Vivo	Hexa-D-arginine (0.1, 1, or 10 nM) administration was shown to reduce circulating TNF-α levels and enhance the survival rate of mice treated with Pseudomonas aeruginosa exotoxin A (PEA) (6-week-old FVB and 129/Sv mice)[1].
References	[1]. The furin inhibitor hexa-D-arginine blocks the activation of Pseudomonas aeruginosa exotoxin A in vivo. Infect Immun. 2002 Dec;70(12):7136-9. [2]. Protection against anthrax toxemia by hexa-D-arginine in vitro and in vivo. Infect Immun. 2004 Jan;72(1):602-5. [3]. Polyarginines are potent furin inhibitors. J Biol Chem. 2000 Nov 24;275(47):36741-9.
Additional Infomation	Hexa-D-arginine is a peptide.

Solubility Data

Solubility (In Vitro)	H2O : ~50 mg/mL (~52.40 mM) DMSO : ~5 mg/mL (~5.24 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 100 mg/mL (104.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.0481 mL	5.2403 mL	10.4806 mL
	5 mM	0.2096 mL	1.0481 mL	2.0961 mL
	10 mM	0.1048 mL	0.5240 mL	1.0481 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.