214766-78-6,MFCD05860888
Catalog No.:AA00BF3V

214766-78-6 | DEGARELIX

Pack Size
Purity
Availability
Price(USD)
Quantity
  
2mg
99%
1 week  
$222.00   $155.00
- +
5mg
99%
1 week  
$336.00   $235.00
- +
10mg
99%
1 week  
$527.00   $369.00
- +
50mg
99%
1 week  
$1,114.00   $780.00
- +
100mg
99%
1 week  
$1,717.00   $1,202.00
- +
  • Technical Information
  • Properties
  • Literature
  • Request for Quotation
  • Download SDS
Technical Information
Catalog Number:
AA00BF3V
Chemical Name:
DEGARELIX
CAS Number:
214766-78-6
Molecular Formula:
C82H103ClN18O16
Molecular Weight:
1632.2592
MDL Number:
MFCD05860888
SMILES:
OC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)N)C)CCCCNC(C)C)CC(C)C)Cc1ccc(cc1)NC(=O)N)Cc1ccc(cc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)NC(=O)[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc2c(c1)cccc2)NC(=O)C)Cc1ccc(cc1)Cl)Cc1cccnc1
Properties
Computed Properties
 
Complexity:
3390  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
11  
Defined Bond Stereocenter Count:
0  
Formal Charge:
0  
Heavy Atom Count:
117  
Hydrogen Bond Acceptor Count:
18  
Hydrogen Bond Donor Count:
17  
Isotope Atom Count:
0  
Rotatable Bond Count:
41  
Undefined Atom Stereocenter Count:
0  
Undefined Bond Stereocenter Count:
0  
XLogP3:
3.5  

Literature

Title: Rapid elimination kinetics of free PSA or human kallikrein-related peptidase 2 after initiation of gonadotropin-releasing hormone-antagonist treatment of prostate cancer: potential for rapid monitoring of treatment responses.

Journal: Clinical chemistry and laboratory medicine 20121101

Title: Gonadotropin-releasing hormone: an update review of the antagonists versus agonists.

Journal: International journal of urology : official journal of the Japanese Urological Association 20120701

Title: The effect of baseline testosterone on the efficacy of degarelix and leuprolide: further insights from a 12-month, comparative, phase III study in prostate cancer patients.

Journal: Urology 20120701

Title: Editorial comment.

Journal: Urology 20120701

Title: [The efficacy of degarelix on LUTS (Lower urinary tract symptoms) relief in patients with prostate cancer].

Journal: Urologia 20120701

Title: The efficacy and safety of degarelix, a GnRH antagonist: a 12-month, multicentre, randomized, maintenance dose-finding phase II study in Japanese patients with prostate cancer.

Journal: Japanese journal of clinical oncology 20120601

Title: Androgen deprivation therapy: past, present and future.

Journal: BJU international 20120601

Title: Short-term testosterone manipulations modulate visual recognition memory and some aspects of emotional reactivity in male rhesus monkeys.

Journal: Physiology & behavior 20120515

Title: Cost-effectiveness analysis of degarelix for advanced hormone-dependent prostate cancer.

Journal: BJU international 20120401

Title: Follicular and endocrine profiles associated with different GnRH-antagonist regimens: a randomized controlled trial.

Journal: Reproductive biomedicine online 20120201

Title: Gonadotropin-releasing hormone blockers and cardiovascular disease risk: analysis of prospective clinical trials of degarelix.

Journal: The Journal of urology 20111101

Title: In vitro studies investigating the interactions between degarelix, a decapeptide gonadotropin-releasing hormone blocker, and cytochrome P450.

Journal: Basic & clinical pharmacology & toxicology 20110901

Title: A phase III extension trial with a 1-arm crossover from leuprolide to degarelix: comparison of gonadotropin-releasing hormone agonist and antagonist effect on prostate cancer.

Journal: The Journal of urology 20110901

Title: Hot flushes in prostatic cancer patients during androgen-deprivation therapy with monthly dose of degarelix or leuprolide.

Journal: Prostate cancer and prostatic diseases 20110601

Title: Efficacy and safety of androgen deprivation therapy after switching from monthly leuprolide to monthly degarelix in patients with prostate cancer.

Journal: International journal of clinical practice 20110501

Title: Response to degarelix after resistance to luteinizing hormone-releasing hormone agonist therapy for metastatic prostate cancer.

Journal: Anti-cancer drugs 20110301

Title: Cardiovascular safety of degarelix: results from a 12-month, comparative, randomized, open label, parallel group phase III trial in patients with prostate cancer.

Journal: The Journal of urology 20101201

Title: Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples.

Journal: British journal of clinical pharmacology 20101001

Title: Changes in alkaline phosphatase levels in patients with prostate cancer receiving degarelix or leuprolide: results from a 12-month, comparative, phase III study.

Journal: BJU international 20100701

Title: Degarelix. More rapid medical castration, nothing more.

Journal: Prescrire international 20100601

Title: Additional analysis of the secondary end point of biochemical recurrence rate in a phase 3 trial (CS21) comparing degarelix 80 mg versus leuprolide in prostate cancer patients segmented by baseline characteristics.

Journal: European urology 20100501

Title: New Drugs2010, PART 1.

Journal: Nursing 20100201

Title: Evaluation of degarelix in the management of prostate cancer.

Journal: Cancer management and research 20100101

Title: Degarelix 240/80 mg: a new treatment option for patients with advanced prostate cancer.

Journal: Expert review of anticancer therapy 20091201

Title: Degarelix (firmagon) for prostate cancer.

Journal: The Medical letter on drugs and therapeutics 20091019

Title: Degarelix.

Journal: Drugs 20091001

Title: Degarelix acetate for the treatment of prostate cancer.

Journal: Drugs of today (Barcelona, Spain : 1998) 20091001

Title: Degarelix for prostate cancer.

Journal: Expert opinion on investigational drugs 20090601

Title: [GnRH antagonists--a new therapy option for advanced prostate cancer].

Journal: Aktuelle Urologie 20090501

Title: Degarelix: a novel gonadotropin-releasing hormone blocker for the treatment of prostate cancer.

Journal: Future oncology (London, England) 20090501

Title: Twenty-five year evolution of medical hormonal therapy for prostate cancer.

Journal: BJU international 20090101

Title: Degarelix and its therapeutic potential in the treatment of prostate cancer.

Journal: Clinical interventions in aging 20090101

Title: Degarelix: a new approach for the treatment of prostate cancer.

Journal: Neuroendocrinology 20090101

Title: Degarelix: a gonadotropin-releasing hormone antagonist for the management of prostate cancer.

Journal: Clinical therapeutics 20090101

Title: The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer.

Journal: BJU international 20081201

Title: A 1-year, open label, randomized phase II dose finding study of degarelix for the treatment of prostate cancer in North America.

Journal: The Journal of urology 20081101

Title: Management of advanced prostate cancer: gonadotropin-releasing hormone blockers might improve prognosis.

Journal: European urology 20081001

Title: Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor blocker--results from a 1-yr, multicentre, randomised, phase 2 dosage-finding study in the treatment of prostate cancer.

Journal: European urology 20081001

Title: Management of advanced prostate cancer: can we improve on androgen deprivation therapy?

Journal: BJU international 20080601

Title: Testosterone surge: rationale for gonadotropin-releasing hormone blockers?

Journal: Urology 20080601

Title: A new model of patient tumor-derived breast cancer xenografts for preclinical assays.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070701

Title: Population pharmacokinetic/pharmacodynamic (PK/PD) modelling of the hypothalamic-pituitary-gonadal axis following treatment with GnRH analogues.

Journal: British journal of clinical pharmacology 20070601

Title: Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist.

Journal: The Journal of pharmacology and experimental therapeutics 20070301

Title: Semi-mechanistic pharmacodynamic modeling for degarelix, a novel gonadotropin releasing hormone (GnRH) blocker.

Journal: Journal of pharmacokinetics and pharmacodynamics 20061001

Title: Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.

Journal: Journal of medicinal chemistry 20060615

Title: Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.

Journal: Journal of medicinal chemistry 20050728

Title: Synthesis and biological activity of GnRH antagonists modified at position 3 with 3-(2-methoxy-5-pyridyl)-alanine.

Journal: The journal of peptide research : official journal of the American Peptide Society 20050201

Title: Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix.

Journal: The Journal of pharmacology and experimental therapeutics 20020401

Title: GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.

Journal: Journal of medicinal chemistry 20010201

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Related Products of 214766-78-6
Tags:214766-78-6 Molecular Formula|214766-78-6 MDL|214766-78-6 SMILES|214766-78-6 DEGARELIX
Catalog No.: AA00BF3V
214766-78-6,MFCD05860888
214766-78-6 | DEGARELIX
Pack Size: 2mg
Purity: 99%
1 week
$222.00 $155.00
Pack Size: 5mg
Purity: 99%
1 week
$336.00 $235.00
Pack Size: 10mg
Purity: 99%
1 week
$527.00 $369.00
Pack Size: 50mg
Purity: 99%
1 week
$1,114.00 $780.00
Pack Size: 100mg
Purity: 99%
1 week
$1,717.00 $1,202.00
Quantity
- +
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Technical Information
Catalog Number: AA00BF3V
Chemical Name: DEGARELIX
CAS Number: 214766-78-6
Molecular Formula: C82H103ClN18O16
Molecular Weight: 1632.2592
MDL Number: MFCD05860888
SMILES: OC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)N)C)CCCCNC(C)C)CC(C)C)Cc1ccc(cc1)NC(=O)N)Cc1ccc(cc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)NC(=O)[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc2c(c1)cccc2)NC(=O)C)Cc1ccc(cc1)Cl)Cc1cccnc1
Properties
Complexity: 3390  
Covalently-Bonded Unit Count: 1  
Defined Atom Stereocenter Count: 11  
Defined Bond Stereocenter Count: 0  
Formal Charge: 0  
Heavy Atom Count: 117  
Hydrogen Bond Acceptor Count: 18  
Hydrogen Bond Donor Count: 17  
Isotope Atom Count: 0  
Rotatable Bond Count: 41  
Undefined Atom Stereocenter Count: 0  
Undefined Bond Stereocenter Count: 0  
XLogP3: 3.5  
Literature fold

Title: Rapid elimination kinetics of free PSA or human kallikrein-related peptidase 2 after initiation of gonadotropin-releasing hormone-antagonist treatment of prostate cancer: potential for rapid monitoring of treatment responses.

Journal: Clinical chemistry and laboratory medicine20121101

Title: Gonadotropin-releasing hormone: an update review of the antagonists versus agonists.

Journal: International journal of urology : official journal of the Japanese Urological Association20120701

Title: The effect of baseline testosterone on the efficacy of degarelix and leuprolide: further insights from a 12-month, comparative, phase III study in prostate cancer patients.

Journal: Urology20120701

Title: Editorial comment.

Journal: Urology20120701

Title: [The efficacy of degarelix on LUTS (Lower urinary tract symptoms) relief in patients with prostate cancer].

Journal: Urologia20120701

Title: The efficacy and safety of degarelix, a GnRH antagonist: a 12-month, multicentre, randomized, maintenance dose-finding phase II study in Japanese patients with prostate cancer.

Journal: Japanese journal of clinical oncology20120601

Title: Androgen deprivation therapy: past, present and future.

Journal: BJU international20120601

Title: Short-term testosterone manipulations modulate visual recognition memory and some aspects of emotional reactivity in male rhesus monkeys.

Journal: Physiology & behavior20120515

Title: Cost-effectiveness analysis of degarelix for advanced hormone-dependent prostate cancer.

Journal: BJU international20120401

Title: Follicular and endocrine profiles associated with different GnRH-antagonist regimens: a randomized controlled trial.

Journal: Reproductive biomedicine online20120201

Title: Gonadotropin-releasing hormone blockers and cardiovascular disease risk: analysis of prospective clinical trials of degarelix.

Journal: The Journal of urology20111101

Title: In vitro studies investigating the interactions between degarelix, a decapeptide gonadotropin-releasing hormone blocker, and cytochrome P450.

Journal: Basic & clinical pharmacology & toxicology20110901

Title: A phase III extension trial with a 1-arm crossover from leuprolide to degarelix: comparison of gonadotropin-releasing hormone agonist and antagonist effect on prostate cancer.

Journal: The Journal of urology20110901

Title: Hot flushes in prostatic cancer patients during androgen-deprivation therapy with monthly dose of degarelix or leuprolide.

Journal: Prostate cancer and prostatic diseases20110601

Title: Efficacy and safety of androgen deprivation therapy after switching from monthly leuprolide to monthly degarelix in patients with prostate cancer.

Journal: International journal of clinical practice20110501

Title: Response to degarelix after resistance to luteinizing hormone-releasing hormone agonist therapy for metastatic prostate cancer.

Journal: Anti-cancer drugs20110301

Title: Cardiovascular safety of degarelix: results from a 12-month, comparative, randomized, open label, parallel group phase III trial in patients with prostate cancer.

Journal: The Journal of urology20101201

Title: Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples.

Journal: British journal of clinical pharmacology20101001

Title: Changes in alkaline phosphatase levels in patients with prostate cancer receiving degarelix or leuprolide: results from a 12-month, comparative, phase III study.

Journal: BJU international20100701

Title: Degarelix. More rapid medical castration, nothing more.

Journal: Prescrire international20100601

Title: Additional analysis of the secondary end point of biochemical recurrence rate in a phase 3 trial (CS21) comparing degarelix 80 mg versus leuprolide in prostate cancer patients segmented by baseline characteristics.

Journal: European urology20100501

Title: New Drugs2010, PART 1.

Journal: Nursing20100201

Title: Evaluation of degarelix in the management of prostate cancer.

Journal: Cancer management and research20100101

Title: Degarelix 240/80 mg: a new treatment option for patients with advanced prostate cancer.

Journal: Expert review of anticancer therapy20091201

Title: Degarelix (firmagon) for prostate cancer.

Journal: The Medical letter on drugs and therapeutics20091019

Title: Degarelix.

Journal: Drugs20091001

Title: Degarelix acetate for the treatment of prostate cancer.

Journal: Drugs of today (Barcelona, Spain : 1998)20091001

Title: Degarelix for prostate cancer.

Journal: Expert opinion on investigational drugs20090601

Title: [GnRH antagonists--a new therapy option for advanced prostate cancer].

Journal: Aktuelle Urologie20090501

Title: Degarelix: a novel gonadotropin-releasing hormone blocker for the treatment of prostate cancer.

Journal: Future oncology (London, England)20090501

Title: Twenty-five year evolution of medical hormonal therapy for prostate cancer.

Journal: BJU international20090101

Title: Degarelix and its therapeutic potential in the treatment of prostate cancer.

Journal: Clinical interventions in aging20090101

Title: Degarelix: a new approach for the treatment of prostate cancer.

Journal: Neuroendocrinology20090101

Title: Degarelix: a gonadotropin-releasing hormone antagonist for the management of prostate cancer.

Journal: Clinical therapeutics20090101

Title: The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer.

Journal: BJU international20081201

Title: A 1-year, open label, randomized phase II dose finding study of degarelix for the treatment of prostate cancer in North America.

Journal: The Journal of urology20081101

Title: Management of advanced prostate cancer: gonadotropin-releasing hormone blockers might improve prognosis.

Journal: European urology20081001

Title: Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor blocker--results from a 1-yr, multicentre, randomised, phase 2 dosage-finding study in the treatment of prostate cancer.

Journal: European urology20081001

Title: Management of advanced prostate cancer: can we improve on androgen deprivation therapy?

Journal: BJU international20080601

Title: Testosterone surge: rationale for gonadotropin-releasing hormone blockers?

Journal: Urology20080601

Title: A new model of patient tumor-derived breast cancer xenografts for preclinical assays.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20070701

Title: Population pharmacokinetic/pharmacodynamic (PK/PD) modelling of the hypothalamic-pituitary-gonadal axis following treatment with GnRH analogues.

Journal: British journal of clinical pharmacology20070601

Title: Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist.

Journal: The Journal of pharmacology and experimental therapeutics20070301

Title: Semi-mechanistic pharmacodynamic modeling for degarelix, a novel gonadotropin releasing hormone (GnRH) blocker.

Journal: Journal of pharmacokinetics and pharmacodynamics20061001

Title: Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.

Journal: Journal of medicinal chemistry20060615

Title: Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.

Journal: Journal of medicinal chemistry20050728

Title: Synthesis and biological activity of GnRH antagonists modified at position 3 with 3-(2-methoxy-5-pyridyl)-alanine.

Journal: The journal of peptide research : official journal of the American Peptide Society20050201

Title: Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix.

Journal: The Journal of pharmacology and experimental therapeutics20020401

Title: GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.

Journal: Journal of medicinal chemistry20010201

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