Histrelin Acetate

Histrelin acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.

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CAT No: 10-101-21

CAS No: 76712-82-8 (net)

Synonyms/Alias: Histrelin acetate;220810-26-4;Vantas;Supprelin;DTXSID30176580;Histrelin (acetate);MFCD00918679;Histrelin (acetate)?;SCHEMBL18715;CHEMBL1200509;AKOS040764197;FD110400;TS-10572;(Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH Acetate;(Des-Gly10,D-His(Bzl)6,Pro-NHEt 9)-LHRH acetate;

Chemical Name: acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-3-(1-benzylimidazol-4-yl)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide

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M.F/Formula	C68H90N18O14
M.W/Mr.	1383.6
Sequence	One Letter Code:XHWSYXLRP Three Letter Code:H-Pyr-His-Trp-Ser-Tyr-D-His(1-Bn)-Leu-Arg-Pro-NHEt.CH3CO2H
Labeling Target	Gonadotropin-releasing hormone receptor
Application	Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin has been proven to be highly effective in treating central precocious puberty in children.
Appearance	Solid powder
Purity	>98% (or refer to the Certificate of Analysis)
Activity	Agonist
Areas of Interest	Cardiovascular System & Diseases Pituitary & Hypothalamic Hormones
Target	Gonadotropin-releasing hormone (GnRH)

Source#	Synthetic
Long-term Storage Conditions	Soluble in DMSO, not in water
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Short-term Storage Conditions	Dry, dark and at 0 - 4 °C
Solubility	-20 °C
Organism	Human
InChI	InChI=1S/C66H86N18O12.C2H4O2/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47;1-2(3)4/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81,90)(H,82,91)(H4,67,68,71);1H3,(H,3,4)/t47-,48-,49-,50-,51-,52-,53+,54-,55-;/m0./s1
InChI Key	OWAUGAMNPZHEOJ-YKZVIGSYSA-N
Canonical SMILES	CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC2=CN(C=N2)CC3=CC=CC=C3)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CC7=CN=CN7)NC(=O)C8CCC(=O)N8.CC(=O)O
Isomeric SMILES	CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CN(C=N2)CC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8.CC(=O)O
BoilingPoint	1800.6ºC at 760 mmHg
ShelfLife	>2 years if stored properly
References	The once-yearly histrelin implant maintained testosterone suppression for repeated treatment cycles and was generally well tolerated. The histrelin implant provides a clinically attractive option for long-term androgen deprivation therapy in patients with advanced prostate cancer seeking fewer office visits and repeated injections. Shore, N., Cookson, M. S., & Gittelman, M. C. (2012). Long‐term efficacy and tolerability of once‐yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU international, 109(2), 226-232. The LHRH agonist histrelin acetate is the only available sustained-release hydrogel implant for once-yearly administration. The once-yearly implant allows patients to receive fewer cycles of implanting and replanting to maintain continuous ADT therapy. The histrelin acetate implant is 3.5 cm long, is 3 mm in diameter, and is administered subcutaneously into the inner aspect of the upper arm or abdomen. The inner aspect of the upper arm can clinically be difficult for the surgeon as it is a mobile insertion site and difficult for elderly patients limited by strength/arthritis to maintain the necessary abducted and extended arm position. Thus, the arm compared to the abdomen site is more difficult for surgeon and is less tolerated by patients. Woolen, S., Holzmeyer, C., Nesbitt, E., & Siami, P. F. (2014). Long-term efficacy and tolerability of abdominal once-yearly histrelin acetate subcutaneous implants in patients with advanced prostate cancer. Prostate cancer, 2014.
Melting Point	N/A

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