Goserelin AcetateCAS# 65807-02-5 |
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Chemical structure
3D structure
| Cas No. | 65807-02-5 | SDF | Download SDF |
| PubChem ID | 47725 | Appearance | Powder |
| Formula | C59H84N18O14 | M.Wt | 1269.41 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | ICI 118630 | ||
| Solubility | Soluble in sterile water | ||
| Chemical Name | N-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2-[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-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 | ||
| SMILES | CC(C)CC(C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NNC(=O)N)NC(=O)C(COC(C)(C)C)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CO)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CN=CN5)NC(=O)C6CCC(=O)N6 | ||
| Standard InChIKey | BLCLNMBMMGCOAS-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C59H84N18O14/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H3,62,76,90) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Goserelin Acetate Dilution Calculator
Goserelin Acetate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 0.7878 mL | 3.9388 mL | 7.8777 mL | 15.7554 mL | 19.6942 mL |
| 5 mM | 0.1576 mL | 0.7878 mL | 1.5755 mL | 3.1511 mL | 3.9388 mL |
| 10 mM | 0.0788 mL | 0.3939 mL | 0.7878 mL | 1.5755 mL | 1.9694 mL |
| 50 mM | 0.0158 mL | 0.0788 mL | 0.1576 mL | 0.3151 mL | 0.3939 mL |
| 100 mM | 0.0079 mL | 0.0394 mL | 0.0788 mL | 0.1576 mL | 0.1969 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Goserelin(ICI 118630) is an injectable gonadotropin releasing hormone superagonist (GnRH agonist). IC50 value: Target: GnRH agonist Goserelin is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot. Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner.
References:
[1]. Goserelin, From Wikipedia
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Both castration and goserelin acetate ameliorate myocardial ischemia reperfusion injury and apoptosis in male rats.[Pubmed:24729888]
ISRN Pharmacol. 2014 Mar 4;2014:206951.
Although reperfusion of an ischemic organ is essential to prevent irreversible tissue damage, it may amplify tissue injury. This study investigates the role of endogenous testosterone in myocardial ischemia reperfusion and apoptosis in male rats. Material and method. Twenty four male rats were randomized into 4 equal groups: Group (1), sham group, rats underwent the same anesthetic and surgical procedure as the control group except for LAD ligation; Group (2), Active control group, rats underwent LAD ligation; Group (3), castrated, rats underwent surgical castration, left 3wks for recovery, and then underwent LAD ligation; and Group (4), Goserelin Acetate treated, rats received 3.6 mg of Goserelin 3 wks before surgery and then underwent LAD ligation. At the end of experiment, plasma cTn I, cardiac TNF- alpha , IL1- beta , ICAM-1, and Apoptosis level were measured and histological examination was made. Results. Compared to sham group, the levels of myocardial TNF- alpha , IL-1 beta , ICAM-1, apoptosis, and plasma cTn I were significantly increased (P < 0.05) in control group and all rats showed significant myocardial injury (P < 0.05). Castration and Goserelin Acetates significantly counteract the increase in myocardial levels of TNF- alpha , IL-1 beta , ICAM-1, plasma cTn I, and apoptosis (P < 0.05) and significantly reduce (P < 0.05) the severity of myocardial injury. We conclude that castration and Goserelin Acetates ameliorate myocardial I/R injury and apoptosis in rats via interfering with inflammatory reactions.
Goserelin acetate before transurethral resection of moderately enlarged benign prostatic hyperplasia: Prospective randomised-controlled clinical trial.[Pubmed:26966595]
Arab J Urol. 2016 Mar;14(1):59-65.
OBJECTIVE: To evaluate the impact of a luteinising hormone-releasing hormone (LHRH) agonist, Goserelin Acetate (GA), on surgical blood loss during transurethral resection of the prostate (TURP), as well as its histopathological effect on prostatic microvessel density (MVD). PATIENTS AND METHODS: Patients who underwent TURP due to benign prostatic enlargement (60-100 mL) were randomly subdivided into two equal groups according to whether they received preoperative GA administration (3.6 mg; group A) or not (group B). Evaluation parameters were operative time, weight of resected prostatic tissue, perioperative haematocrit (HCT) changes, estimation of intraoperative blood loss, and suburethral and stromal prostatic MVD. Effects of GA on prostate weight and any possible side-effects were also monitored. RESULTS: In all, 35 and 33 patients were included in groups A and B, respectively. Operative time and HCT values' changes were significantly less in group A (P < 0.05). Also, operative blood loss (both total and adjusted per weight of resected tissue) was lower in group A, at a mean (SD) of 178.13 (77.71) mL and 3.74 (1.52) mL/g vs 371.75 (91.09) mL and 8.59 (2.42) mL/g (P < 0.001). The median MVD in both suburethral [8 vs 11 vessels/high-power field (HPF)] and stromal tissues (9 vs 17 vessels/HPF) were significantly lower in group A (P < 0.001). Side-effects were minimal. CONCLUSION: A single dose of GA, a LHRH agonist, before TURP is safe and effective in reducing surgical blood loss. It significantly reduced MVD in both suburethral and stromal nodular prostatic tissues without regional discrepancy.
[Giant subcutaneous hematoma with hemorrhagic shock induced by goserelin acetate injection for prostate cancer : report of a case].[Pubmed:25293802]
Hinyokika Kiyo. 2014 Sep;60(9):455-8.
A 87-year-old man was diagnosed with prostate cancer (cT2aN0M0 Gleason score 44 with initial prostate specific antigen of 23.4 ng/ml). Prostate cancer was treated with combined androgen blockade (Goserelin Acetate plus flutamide). He was administered Goserelin Acetate depot injection without any complications as an outpatient. However, 5 hours after he left the hospital, he came back to the hospital, complaining of lower abdominal pain. Abdominal computed tomography revealed a giant subcutaneous hematoma in the lower abdomen. Hemoglobin was 6.9 g/dl and blood pressure was lower than 80 mmHg. He was admitted and given a blood transfusion. Because of pre-disseminated intravascular coagulation score 6, it was hard to antagonize warfarin by Vitamin K (he had taken warfarin because of atrial fibrillation). Arteriography was performed and injury to a branch of the lower epigastric artery was found. Transcatheter arterial embolization was performed at the same time. Injecting Goserelin Acetate may cause severe arterial injury.
Effects of treadmill training on combined goserelin acetate and doxorubicin-induced osteopenia in female rats.[Pubmed:24583536]
J Musculoskelet Neuronal Interact. 2014 Mar;14(1):10-8.
OBJECTIVES: This study examined individual and combined effects of the cancer treatments Goserelin Acetate (GA) and doxorubicin (DOX) on bone and determined if treadmill running (TM) provides osteoprotection. METHODS: Ten-week-old female Sprague-Dawley rats were randomly assigned to sedentary (SED) or TM groups. SED received GA, DOX, combined GA and DOX (GA+DOX), or placebo and maintained normal cage activity. TM received GA, DOX, GA+DOX, or placebo and participated in a progressive motorized treadmill protocol. After 8 weeks, tibiae were evaluated using micro computed tomography. RESULTS: Negative drug effects were observed in cancellous bone (bone volume/tissue volume, trabecular number, trabecular thickness, trabecular spacing; P<0.05). An additive bone volume/tissue volume and trabecular spacing effect was observed in SED GA+DOX (vs. SED+GA and SED+DOX, P<0.05) but not in TM GA+DOX (vs. TM+GA and TM+DOX, P>0.05). Negative drug effects were observed in cortical bone (cross-sectional volume, cortical volume, marrow volume; P<0.05), but combined GA+DOX did not exacerbate these effects. Additionally, there were no protective cortical bone effects observed in TM. CONCLUSIONS: Combined GA+DOX exacerbates cancellous osteopenia in the tibia, and treadmill running provided only minor protection.
