RFRP-1(human) is a homolog of gonadotropin-inhibiting hormone (GnIH). RFRP-1(human) targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropins and potently inhibits gonadotropins. RFRP-1(human) is a potent neuropeptide FF (NPFF) receptor agonist/activator with EC50s of 0.0011 nM and 29 nM for NPFF2 and NPFF1, respectively.

Physicochemical Properties

Molecular Formula	C67H101N19O14S
Molecular Weight	1428.70
Exact Mass	1427.75
CAS #	311309-25-8
PubChem CID	71462794
Appearance	White to off-white solid powder
LogP	3.277
Hydrogen Bond Donor Count	16
Hydrogen Bond Acceptor Count	18
Rotatable Bond Count	41
Heavy Atom Count	101
Complexity	2840
Defined Atom Stereocenter Count	12
SMILES	C[C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CN=CN4)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CCSC)N
InChi Key	STXUPUZSJMRDJT-IWPKOFGPSA-N
InChi Code	InChI=1S/C67H101N19O14S/c1-37(2)28-46(59(93)77-44(20-13-24-74-67(71)72)57(91)78-45(55(70)89)30-40-16-9-7-10-17-40)81-64(98)53-22-15-26-86(53)66(100)50(29-38(3)4)83-61(95)49(33-54(69)88)79-56(90)39(5)76-58(92)47(31-41-18-11-8-12-19-41)80-62(96)51(35-87)84-60(94)48(32-42-34-73-36-75-42)82-63(97)52-21-14-25-85(52)65(99)43(68)23-27-101-6/h7-12,16-19,34,36-39,43-53,87H,13-15,20-33,35,68H2,1-6H3,(H2,69,88)(H2,70,89)(H,73,75)(H,76,92)(H,77,93)(H,78,91)(H,79,90)(H,80,96)(H,81,98)(H,82,97)(H,83,95)(H,84,94)(H4,71,72,74)/t39-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-/m0/s1
Chemical Name	(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-N-[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]butanediamide
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 Vivo

In isolated mammalian cardiac myocytes, RFRP-1(human) quickly and reversibly reduces shortening and relaxation in a dose-dependent manner[2]. Mice receiving an intravenous injection of RFRP-1(human) exhibit decreased cardiac output, ejection fraction, heart rate, and stroke volume[2].

References

[1]. Identification of human GnIH homologs, RFRP-1 and RFRP-3, and the cognate receptor, GPR147 in the human hypothalamic pituitary axis. PLoS One. 2009 Dec 22;4(12):e8400. [2]. Human RFamide-related peptide-1 diminishes cellular and integrated cardiac contractile performance. Peptides. 2010 Nov;31(11):2067-74. [3]. Functional differences between NPFF1 and NPFF2 receptor coupling: high intrinsic activities of RFamide-related peptides on stimulation of [35S]GTPgammaS binding. Neuropharmacology. 2007 Feb;52(2):376-86.

Solubility Data

Solubility (In Vitro)	H2O: 100 mg/mL (69.99 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 50 mg/mL (35.00 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	0.6999 mL	3.4997 mL	6.9994 mL
	5 mM	0.1400 mL	0.6999 mL	1.3999 mL
	10 mM	0.0700 mL	0.3500 mL	0.6999 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.