Nafarelin Acetate - CAS 86220-42-0
Catalog number:
B0084-078531
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C68H89N17O16
Molecular Weight:
1400.56
COA:
Inquire
Targets:
GNRH Receptor
Description:
Nafarelin is a GnRH (gonadotropin-releasing hormone) agonist . Its proposed mechanism of action is the desensitization of pituitary gonadotropin-releasing hormone receptors leading to a decrease in gonadotropin release, and ovarian hormone serum concentrations similar to those achieved in postmenopausal women. It can decrease pituitary secretion of the gonadotropins LH and FSH. Nafarelin can be used for the treatment of precocious puberty in chirldren and Premature LG surges.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-078531 10 mg $998 In stock
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Sequence:
XHWSYXLRPG
Purity:
95%
Appearance:
white solid
Synonyms:
acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-naphthalen-2-yl-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;hydrate
Solubility:
H2O: >5 mg/mL
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
precocious puberty in chirldren;Premature LG surges
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
1840.1℃ at 760 mmHg
InChIKey:
FSBTYDWUUWLHBD-UDXTWCDOSA-N
InChI:
InChI=1S/C66H83N17O13.C2H4O2.H2O/c1-36(2)25-48(58(89)76-47(13-7-23-71-66(68)69)65(96)83-24-8-14-54(83)64(95)73-33-55(67)86)77-60(91)50(28-38-15-18-39-9-3-4-10-40(39)26-38)78-59(90)49(27-37-16-19-43(85)20-17-37)79-63(94)53(34-84)82-61(92)51(29-41-31-72-45-12-6-5-11-44(41)45)80-62(93)52(30-42-32-70-35-74-42)81-57(88)46-21-22-56(87)75-46;1-2(3)4;/h3-6,9-12,15-20,26,31-32,35-36,46-54,72,84-85H,7-8,13-14,21-25,27-30,33-34H2,1-2H3,(H2,67,86)(H,70,74)(H,73,95)(H,75,87)(H,76,89)(H,77,91)(H,78,90)(H,79,94)(H,80,93)(H,81,88)(H,82,92)(H4,68,69,71);1H3,(H,3,4);1H2/t46-,47-,48-,49-,50+,51-,52-,53-,54-;;/m0../s1
Canonical SMILES:
CC(C)CC(C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NCC(=O)N)NC(=O)C(CC2=CC3=CC=CC=C3C=C2)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.O
Current Developer:
originator Pfizer
1.Evaluation of drug interactions with nanofibrillar cellulose.
Kolakovic R1, Peltonen L, Laukkanen A, Hellman M, Laaksonen P, Linder MB, Hirvonen J, Laaksonen T. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):1238-44. doi: 10.1016/j.ejpb.2013.05.015. Epub 2013 Jun 15.
Nanofibrillar cellulose (NFC) (also referred to as cellulose nanofibers, nanocellulose, microfibrillated, or nanofibrillated cellulose) has recently gotten wide attention in various research areas and it has also been studied as excipient in formulation of the pharmaceutical dosage forms. Here, we have evaluated the interactions between NFC and the model drugs of different structural characteristics (size, charge, etc.). The series of permeation studies were utilized to evaluate the ability of the drugs in solution to diffuse through the thin, porous, dry NFC films. An incubation method was used to determine capacity of binding of chosen model drugs to NFC as well as isothermal titration calorimetry (ITC) to study thermodynamics of the binding process. A genetically engineered fusion protein carrying double cellulose binding domain was used as a positive control since its affinity and capacity of binding for NFC have already been reported.
2.Stability of peptide drugs in the colon.
Wang J1, Yadav V1, Smart AL1, Tajiri S1, Basit AW2. Eur J Pharm Sci. 2015 Oct 12;78:31-6. doi: 10.1016/j.ejps.2015.06.018. Epub 2015 Jun 23.
This study was the first to investigate the colonic stability of 17 peptide molecules (insulin, calcitonin, glucagon, secretin, somatostatin, desmopressin, oxytocin, Arg-vasopressin, octreotide, ciclosporin, leuprolide, nafarelin, buserelin, histrelin, [D-Ser(4)]-gonadorelin, deslorelin, and goserelin) in a model of the large intestine using mixed human faecal bacteria. Of these, the larger peptides - insulin, calcitonin, somatostatin, glucagon and secretin - were metabolized rapidly, with complete degradation observed within 5 min. In contrast, a number of the smaller peptides - Arg-vasopressin, desmopressin, oxytocin, gonadorelin, goserelin, buserelin, leuprolide, nafarelin and deslorelin - degraded more slowly, while octreotide, histrelin and ciclosporin were seen to be more stable as compared to the other small peptides under the same conditions. Peptide degradation rate was directly correlated to peptide lipophilicity (logP); those peptides with a higher logP were more stable in the colonic model (R(2)=0.
3.Cyclophosphamide: As bad as its reputation? Long-term single centre experience of cyclophosphamide side effects in the treatment of systemic autoimmune diseases.
Dan D1, Fischer R1, Adler S1, Förger F1, Villiger PM1. Swiss Med Wkly. 2014 Oct 23;144:w14030. doi: 10.4414/smw.2014.14030. eCollection 2014.
OBJECTIVES: Despite new treatment modalities, cyclophosphamide (CYC) remains a cornerstone in the treatment of organ or life-threatening vasculitides and connective tissue disorders. We aimed at analysing the short- and long-term side-effects of CYC treatment in patients with systemic autoimmune diseases.
4.Using the ovarian sensitivity index to define poor, normal, and high response after controlled ovarian hyperstimulation in the long gonadotropin-releasing hormone-agonist protocol: suggestions for a new principle to solve an old problem.
Huber M1, Hadziosmanovic N, Berglund L, Holte J. Fertil Steril. 2013 Nov;100(5):1270-6. doi: 10.1016/j.fertnstert.2013.06.049. Epub 2013 Aug 6.
OBJECTIVE: To explore the utility of using the ratio between oocyte yield and total dose of FSH, i.e., the ovarian sensitivity index (OSI), to define ovarian response patterns.
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