Alarelin Acetate | CAS#79561-22-1 |148029-26-9 | LH-RH agonist

Alarelin Acetate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 326636

CAS#: 79561-22-1 (acetate)

Description: Alarelin is a potent LH-RH agonist in rats and mice. Alarelin reversibly delays sexual maturation in rats, stimulates spawning activity in fish. GnRH ( gonadotropin-releasing hormone, Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2), which is also referred as LHRH (luteinizing hormone-releasing hormone) or gonadorelin, is crucial for mammalian reproduction and is released from hypothalamic neurons. It is responsible for the secretion of gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), from the pituitary glands.

Chemical Structure

Alarelin Acetate

CAS# 79561-22-1 (acetate)

Instruction

Theoretical Analysis

MedKoo Cat#: 326636
Name: Alarelin Acetate
CAS#: 79561-22-1 (acetate)
Chemical Formula: C60H86N16O16
Exact Mass: 0.00
Molecular Weight: 1,287.444
Elemental Analysis: C, 55.98; H, 6.73; N, 17.41; O, 19.88

Price and Availability

Size	Price	Availability
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2450	2 Weeks
1g	USD 3250	2 Weeks
2g	USD 5050	2 Weeks
5g	USD 7950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 79561-22-1 (acetate) 148029-26-9 (free base),

Synonym: Alarelin Acetate; LHRH-A; 6-D-Ala-10-D-gly-LHRH-ethylamide. Pyr-His-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-NHEt. 6-D-Ala-10-D-gly-LHRH-ethylamide.

IUPAC/Chemical Name: (S)-1-((3S,6S,9S,12S,15R,18S,21S)-3-((1H-imidazol-5-yl)methyl)-6-((1H-indol-3-yl)methyl)-21-(3-((diaminomethylene)amino)propyl)-12-(4-hydroxybenzyl)-9-(hydroxymethyl)-18-isobutyl-15-methyl-1,4,7,10,13,16,19-heptaoxo-1-((S)-5-oxopyrrolidin-2-yl)-2,5,8,11,14,17,20-heptaazadocosan-22-oyl)-N-ethylpyrrolidine-2-carboxamide diacetate

InChi Key: DPWSRXJWCYEGIV-PFHUABGLSA-N

InChi Code: InChI=1S/C56H78N16O12.2C2H4O2/c1-5-60-54(83)45-13-9-21-72(45)55(84)39(12-8-20-61-56(57)58)66-50(79)40(22-30(2)3)67-47(76)31(4)64-49(78)41(23-32-14-16-35(74)17-15-32)68-53(82)44(28-73)71-51(80)42(24-33-26-62-37-11-7-6-10-36(33)37)69-52(81)43(25-34-27-59-29-63-34)70-48(77)38-18-19-46(75)65-38;2*1-2(3)4/h6-7,10-11,14-17,26-27,29-31,38-45,62,73-74H,5,8-9,12-13,18-25,28H2,1-4H3,(H,59,63)(H,60,83)(H,64,78)(H,65,75)(H,66,79)(H,67,76)(H,68,82)(H,69,81)(H,70,77)(H,71,80)(H4,57,58,61);2*1H3,(H,3,4)/t31-,38+,39+,40+,41+,42+,43+,44+,45+;;/m1../s1

SMILES Code: O=C([C@H](CC1)NC1=O)N[C@@H](CC2=CN=CN2)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CO)C(N[C@@H](CC5=CC=C(O)C=C5)C(N[C@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](CCC/N=C(N)\N)C(N6[C@H](C(NCC)=O)CCC6)=O)=O)=O)=O)=O)=O)=O.CC(O)=O.CC(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

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.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,287.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Carel JC, Eugster EA, Rogol A, Ghizzoni L, Palmert MR; ESPE-LWPES GnRH Analogs Consensus Conference Group; Antoniazzi F, Berenbaum S, Bourguignon JP, Chrousos GP, Coste J, Deal S, de Vries L, Foster C, Heger S, Holland J, Jahnukainen K, Juul A, Kaplowitz P, Lahlou N, Lee MM, Lee P, Merke DP, Neely EK, Oostdijk W, Phillip M, Rosenfield RL, Shulman D, Styne D, Tauber M, Wit JM. Consensus statement on the use of gonadotropin-releasing hormone analogs in children. Pediatrics. 2009 Apr;123(4):e752-62. doi: 10.1542/peds.2008-1783. Epub 2009 Mar 30. PMID: 19332438.

2: Wang B, Bissell DM. Hereditary Coproporphyria. 2012 Dec 13 [updated 2022 May 19]. In: Adam MP, Mirzaa GM, Pagon RA, Wallace SE, Bean LJH, Gripp KW, Amemiya A, editors. GeneReviews® [Internet]. Seattle (WA): University of Washington, Seattle; 1993–2023. PMID: 23236641.

3: Agarwal SK, Hamrang C, Henzl MR, Judd HL. Nafarelin vs. leuprolide acetate depot for endometriosis. Changes in bone mineral density and vasomotor symptoms. Nafarelin Study Group. J Reprod Med. 1997 Jul;42(7):413-23. PMID: 9252932.

4: Dantas ZN, Vicino M, Balmaceda JP, Asch RH, Stone SC. Comparison between nafarelin and leuprolide acetate for in vitro fertilization: preliminary clinical study. Fertil Steril. 1994 Apr;61(4):705-8. doi: 10.1016/s0015-0282(16)56649-7. PMID: 8150114.

5: Takeuchi S, Minoura H, Shibahara T, Tsuiki Y, Noritaka F, Toyoda N. A prospective randomized comparison of routine buserelin acetate and a decreasing dosage of nafarelin acetate with a low-dose gonadotropin-releasing hormone agonist protocol for in vitro fertilization and intracytoplasmic sperm injection. Fertil Steril. 2001 Sep;76(3):532-7. doi: 10.1016/s0015-0282(01)01977-x. PMID: 11532477.

6: Chu NI, Chan RL, Hama KM, Chaplin MD. Disposition of nafarelin acetate, a potent agonist of luteinizing hormone-releasing hormone, in rats and rhesus monkeys. Drug Metab Dispos. 1985 Sep-Oct;13(5):560-5. PMID: 2865103.

7: Tanos V, Friedler S, Shushan A, Strauss N, Hetsroni I, Lewin A. Comparison between nafarelin acetate and D-Trp6-LHRH for temporary pituitary suppression in in vitro fertilization (IVF) patients: a prospective crossover study. J Assist Reprod Genet. 1995 Nov;12(10):715-9. doi: 10.1007/BF02212899. PMID: 8624429.

8: Letassy NA, Thompson DF, Britton ML, Suda RR Sr. Nafarelin acetate: a gonadotropin-releasing hormone agonist for the treatment of endometriosis. DICP. 1990 Dec;24(12):1204-9. doi: 10.1177/106002809002401212. Erratum in: DICP 1991 Mar;25(3):321. PMID: 2151003.

9: Yuzpe AA, Nisker JA, Kaplan BR, Tummon IS, Auckland J. Nafarelin acetate for pituitary down-regulation in in vitro fertilization. Comparison of two dosages. J Reprod Med. 1995 Feb;40(2):83-8. PMID: 7738933.

10: Alizadeh B, Bahari Javan N, Akbari Javar H, Khoshayand MR, Dorkoosh F. Prolonged injectable formulation of Nafarelin using in situ gel combination delivery system. Pharm Dev Technol. 2018 Feb;23(2):132-144. doi: 10.1080/10837450.2017.1321662. Epub 2017 May 5. PMID: 28430010.

11: Minaguchi H, Wong JM, Snabes MC. Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. J Reprod Med. 2000 Jun;45(6):481-9. PMID: 10900582.

12: Kennedy SH, Williams IA, Brodribb J, Barlow DH, Shaw RW. A comparison of nafarelin acetate and danazol in the treatment of endometriosis. Fertil Steril. 1990 Jun;53(6):998-1003. doi: 10.1016/s0015-0282(16)53574-2. PMID: 2140996.

13: Harada T. [Endometriosis]. Nihon Rinsho. 2006 Apr;64 Suppl 4:70-4. Japanese. PMID: 16689287.

14: Brenner PF, Shoupe D, Mishell DR Jr. Ovulation inhibition with nafarelin acetate nasal administration for six months. Contraception. 1985 Dec;32(6):531-51. doi: 10.1016/s0010-7824(85)80001-9. PMID: 2936564.

15: Chrisp P, Goa KL. Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. Drugs. 1990 Apr;39(4):523-51. doi: 10.2165/00003495-199039040-00005. PMID: 2140979.

16: Valle RF, Sciarra JJ. Endometriosis: treatment strategies. Ann N Y Acad Sci. 2003 Nov;997:229-39. doi: 10.1196/annals.1290.026. PMID: 14644830.

17: Lockwood GM, Pinkerton SM, Barlow DH. A prospective randomized single-blind comparative trial of nafarelin acetate with buserelin in long-protocol gonadotrophin-releasing hormone analogue controlled in-vitro fertilization cycles. Hum Reprod. 1995 Feb;10(2):293-8. doi: 10.1093/oxfordjournals.humrep.a135930. PMID: 7769051.

18: Chan RL, Chaplin MD. Plasma binding of LHRH and nafarelin acetate, a highly potent LHRH agonist. Biochem Biophys Res Commun. 1985 Mar 15;127(2):673-9. doi: 10.1016/s0006-291x(85)80214-x. PMID: 3156598.

19: Batheja P, Thakur R, Michniak B. Transdermal iontophoresis. Expert Opin Drug Deliv. 2006 Jan;3(1):127-38. doi: 10.1517/17425247.3.1.127. Erratum in: Expert Opin Drug Deliv. 2006 Mar;3(2):303. Priya, Batheja [corrected to Batheja, Priya]; Rashmi, Thakur [corrected to Thakur, Rashmi]; Bozena, Michniak [corrected to Michniak, Bozena]. PMID: 16370945.

20: Goldman JA, Dicker D, Feldberg D, Ashkenazi J, Voliowich I. A prospective randomized comparison of two gonadotrophin-releasing hormone agonists, nafarelin acetate and buserelin acetate, in in-vitro fertilization-embryo transfer. Hum Reprod. 1994 Feb;9(2):226-8. doi: 10.1093/oxfordjournals.humrep.a138486. PMID: 8027276.

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Alarelin Acetate featured