DESLORELIN

DESLORELIN ACETATE

Synonyms. Tryptal; (D-Trp(6)-pro(9)-NEt)-GNRH; (D-Trp(6)-pro(9))-LHRH; (D-Trp(6)-pro(9))-luteinizing hormone-releasing; (D-Trp6,Pro9-NHEt)LH-RH; (D-Trp6,des-Gly-NH210)-LH-RH; (D-Trp6,des-Gly10)-LH-RH; (Des-Gly10(D-Tro6)-LH-RH; (de-Gly10,D-Trp6,Pro-NHEt)-LH-RH; Somagard; [des-Gly10, D-Trp6]-LH-RH; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-N-ethyl-L- prolinamide; D-Trp LHRH-PEA; D-Trp(sup 6)-pro(sup 9)-N-ethylamide-LHRH; Deslorelin; Deslorelina; Deslorelina; Desloreline; Deslorelinum; GNRH (D-Trp6,pro9-net);

PRODUCT IDENTIFICATION
CAS RN	82318-06-7 (acetate); 57773-65-6(ethylamide)
EINECS RN
FORMULA	C₆₄H₈₃N₁₇O₁₂
MOLE WEIGHT	1282.46
H.S CODE	2937.90.0000
SMILES	c1(C[C@@H](C(N[C@@H](CO)C(N[C@H](C(N[C@@H](C(=O)N [C@@H](CC (C) C)C(=O)N[C@H](C(N2CCC[C@H]2C(=O)NCC)=O) CCCNC(N)= N)Cc2c[nH] c3ccccc23)=O)Cc2ccc(cc2)O)=O) =O)NC ([C@H](Cc2cnc[nH]2 )NC([C@ @H] 2NC (=O)CC2)=O)=O)c2c ([nH]c1) cccc2
CLASSIFICATION	Polypeptide, LHRH agonist
EXTRA NOTES	Long-acting analog of LHFSHRH

PHYSICAL AND CHEMICAL PROPERTIES
PHYSICAL STATE.	white powder
MELTING POINT
BOILING POINT
DENSITY
SOLUBILITY IN WATER	Soluble (soluble in 1% acetic acid)
SOLVENT SOLUBILITY
VAPOR DENSITY
log P(octanol-water)
VAPOR PRESSURE
AUTOIGNITION TEMP
pH
REFRACTIVE INDEX
FLASH POINT

STABILITY AND REACTIVITY
STABILITY	Stable under normal conditions.
INCOMPATIBLE MATERIALS	Strong acids, Strong bases
POLYMERIZATION	Has not been reported
NFPA RATINGS	Health: 2,Flammability:0, Reactivity: 0

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking: http://en.wikipedia.org/wiki/Deslorelin

Prostate cancer hormone therapy treatment may use LHRH agonists, also known as Luteinizing hormone-releasing hormone (LHRH) agonists or Gonadotropin releasing hormone (GnRH) agonists. Luteinizing hormone-releasing hormone and Gonadotropin-releasing hormone are essentially the same chemicals which are released by the hypothalamus when it detects lowering levels of testosterone. An agonist is a chemical that mimics a naturally-occurring substance in the body and produces the same physiological effect. The agonist will occupy the cell receptors of the chemical it is mimicking. An agonist has a longer biological half-life, meaning the body takes longer to metabolize and eliminate the agonist. The agonist therefore will occupy a receptor for a longer period of time. Agonists are sometimes referred to as analogues because they are inserted beneath the skin where they continuously emit LHRH agonist of GnRH agonist for a prostate cancer treatment. LHRH and GnRH agonists are also administered as an injection that can be performed in a doctor’s office or at home.(http://www.prostate-cancer.com/)

Triptorelin is a synthetic analogue of gonadorelin (natural GnRH decapeptide) with amino acid (D-tryptophan) substitution in position 6 to inhibit rapid degradation for long activity. Used as triptorelin pamoate or acetate form, triptorelin is used as an antineoplastic in the palliative treatment of prostatic carcinoma, administered intramuscularly. Other analogues with two substituents in position 6 and 10 include Buserelin, Deslorelin. Goserelin, Histrelin, Leuprolide, Nafarelin,

GnRH agonist
Product	CAS RN.
Deslorelin	57773-65-6
Goserelin	65807-02-5
Leuprolide acetate	74381-53-6
Leuprolide	53714-56-0
Histrelin	76712-82-8
Lutrelin acetate	83784-18-3
Nafarelin acetate	86220-42-0
Buserelin	57982-77-1
Buserelin acetate	68630-75-1
Triptorelin	57773-63-4
Nafarelin	76932-56-4
GnRH antagonist
Product	CAS RN.
Detirelix	89662-30-6
Detirelix acetate	102583-46-0
Abarelix	183552-38-7
Teverelix	144743-92-0
Cetrorelix	120287-85-6
Ganirelix	124904-93-4
Iturelix	112568-12-4

SALES SPECIFICATION
APPEARANCE	white to off-white powder
IDENTIFICATION	Pass Test (HPLC)
PEPTIDE PURITY	98.5% min
AMINO AID ANALYSIS	Ser: 0.8 - 1.1 Glx: 0.9 - 1.1 Pro: 0.9 - 1.1 Leu: 0.9 - 1.1 Tyr: 0.9 - 1.1 His: 0.9 - 1.1 Arg: 0.9 - 1.1 Trp: Present
PEPTIDE CONTENT	80.0% min (N determination)
OPTICAL ROTATION	-70° ~ -82°(c=0.1, 1% acetic acid)
WATER	7.0% max
ACETIC ACID	12.0% max
TRIFLUOROACETIC ACID	0.3% max
RELATED SUBSTANCES	[D-pGlu1]Deslorelin: 0.5% max [D-His2]Deslorelin: 0.5% max Ser(Ac)4-Deslorelin: 0.5% max Oher individual impurity: 0.3% max Total impurity: 1.5% max
MICROBIOLOGICAL TEST	Total viable aerobic count: 100 CFU/g max Bacterial endotoxins: 2 IU/mg max
RESIDUAL SOLVENTS	0.1% max

TRANSPORT & REGULATORY INFORMATION
UN NO.	Not known
HAZARD CLASS
PACKING GROUP

SAFETY INFORMATION
HAZARD OVERVIEW	May damage fertility or the unborn child.
GHS
SIGNAL WORD	Danger
PICTOGRAMS
HAZARD STATEMENTS	H360
P STATEMENTS	P201-P308 + P313
EC DIRECTIVES
HAZARD CODES
RISK PHRASES	60
SAFETY PHRASES	53-22-36/37/39-45

PACKING