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| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
In isolated rat hypothalamic-neurohypophyseal explants, histrelin (10–100 nM) promotes the release of vasopressin (VP) [4]. In the rat hypothalamic-neurohypophyseal system, histrelin (100 nM) promotes the production of oxytocin (OT) [5].
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| ln Vivo |
In Csfmop/Csfmop mice, histrelin (0.1 mg/kg, subcutaneous injection) raises circulating LH concentrations [2]. Rabbit kidneys with subcutaneous injections of histrelin (10, 30, or 100 μg/day) have less intimal glands.
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| Animal Protocol |
Animal/Disease Models: Csfmop/Csfmop mice [2]
Doses: 0.001, 0.05, and 0.1 mg/kg Route of Administration: Results of subcutaneous injection: serum FSH concentration increased 4-fold. Animal/Disease Models: Rabbit [3] Doses: 10, 30 or 100 μg/day Route of Administration: subcutaneous injection for 4 weeks Experimental Results: Caused endometrial glandular degeneration and stroma thinning. |
| References |
[1]. Emma D Deeks, et al. Histrelin: in advanced prostate cancer. Drugs. 2010 Mar 26;70(5):623-30.
[2]. P E Cohen, et al. Colony-stimulating factor-1 plays a major role in the development of reproductive function in male mice. Mol Endocrinol. 1997 Oct;11(11):1636-50. [3]. D W Hahn, et al. Development of an animal model for quantitatively evaluating effects of drugs on endometriosis. Fertil Steril. 1985 Sep;44(3):410-5. [4]. E Boczek-Leszczyk, et al. Vasopressin release from the rat hypothalamo-neurohypophysial system: effects of gonadotrophin-releasing hormone (GnRH), its analogues and melatonin. J Physiol Pharmacol. 2010 Aug;61(4):459-66. [5]. Marlena Juszczak, et al. Hypothalamic gonadotropin-releasing hormone receptor activation stimulates oxytocin release from the rat hypothalamo-neurohypophysial system while melatonin inhibits this process. Brain Res Bull. 2010 Jan 15;81(1):185-90. |
| Molecular Formula |
C66H86N18O12
|
|---|---|
| Molecular Weight |
1323.50244
|
| CAS # |
76712-82-8
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| Related CAS # |
Histrelin acetate;220810-26-4
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| SMILES |
CC(=O)O.NC(NCCC[C@@H](C(N1CCC[C@H]1C(NCC)=O)=O)NC([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@H](CC1=CNC2=CC=CC=C12)NC([C@@H](NC([C@@H]1CCC(=O)N1)=O)CC1=CN=CN1)=O)=O)CO)=O)CC1=CC=C(O)C=C1)=O)CC1N=CN(CC2=CC=CC=C2)C=1)=O)CC(C)C)=O)=N
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7556 mL | 3.7779 mL | 7.5557 mL | |
| 5 mM | 0.1511 mL | 0.7556 mL | 1.5111 mL | |
| 10 mM | 0.0756 mL | 0.3778 mL | 0.7556 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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