Synonym
Delmadinone acetate; RS1301; RS-1301; RS 1301
IUPAC/Chemical Name
Pregna-1,4,6-triene-3,20-dione, 17-(acetyloxy)-6-chloro-
InChi Key
CGBCCZZJVKUAMX-DFXBJWIESA-N
InChi Code
InChI=1S/C23H27ClO4/c1-13(25)23(28-14(2)26)10-7-18-16-12-20(24)19-11-15(27)5-8-21(19,3)17(16)6-9-22(18,23)4/h5,8,11-12,16-18H,6-7,9-10H2,1-4H3/t16-,17+,18+,21-,22+,23+/m1/s1
SMILES Code
CC([C@@]1(OC(C)=O)CC[C@@]2([H])[C@]3([H])C=C(Cl)C4=CC(C=C[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
to be determined
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
Biological target:
Delmadinone acetate is a progesterone with antiestrogen and antiandrogen activity.
In vivo activity:
The objective of this study was to characterise the effects of delmadinone acetate on the pituitary-adrenal axis, glucose tolerance and growth hormone concentration in normal male dogs and dogs with benign prostatic hyperplasia. Delmadinone acetate was administered to six normal male dogs and seven dogs with benign prostatic hyperplasia at recommended dose rates (1.5 mg/kg subcutaneously at 0, 1 and 4 weeks). A substantial suppression of basal and 2 h post-ACTH plasma cortisol secretion was demonstrated after one dose in all dogs given delmadinone acetate. Individual responses after the second and third administration varied between recovery in adrenal responsiveness to continued suppression. Plasma ACTH concentration was also diminished after one treatment.
Reference: Aust Vet J. 1998 Aug;76(8):555-60. https://pubmed.ncbi.nlm.nih.gov/9741725/
|
Solvent |
mg/mL |
mM |
| Solubility |
| H2O |
6.1 |
15.07 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
402.92
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:
1. Lange K, Cordes EK, Hoppen HO, Günzel-Apel AR. Determination of concentrations of sex steroids in blood plasma and semen of male dogs treated with delmadinone acetate or finasteride. J Reprod Fertil Suppl. 2001;57:83-91. PMID: 11787194. 2. Court EA, Watson AD, Church DB, Emslie DR. Effects of delmadinone acetate on pituitary-adrenal function, glucose tolerance and growth hormone in male dogs. Aust Vet J. 1998 Aug;76(8):555-60. doi: 10.1111/j.1751-0813.1998.tb10216.x. PMID: 9741725.
In vivo protocol:
1. Lange K, Cordes EK, Hoppen HO, Günzel-Apel AR. Determination of concentrations of sex steroids in blood plasma and semen of male dogs treated with delmadinone acetate or finasteride. J Reprod Fertil Suppl. 2001;57:83-91. PMID: 11787194. 2. Court EA, Watson AD, Church DB, Emslie DR. Effects of delmadinone acetate on pituitary-adrenal function, glucose tolerance and growth hormone in male dogs. Aust Vet J. 1998 Aug;76(8):555-60. doi: 10.1111/j.1751-0813.1998.tb10216.x. PMID: 9741725.
1: Court EA, Watson AD, Church DB, Emslie DR. Effects of delmadinone acetate on pituitary-adrenal function, glucose tolerance and growth hormone in male dogs. Aust Vet J. 1998 Aug;76(8):555-60. doi: 10.1111/j.1751-0813.1998.tb10216.x. PMID: 9741725.
2: Albouy M, Sanquer A, Maynard L, Eun HM. Efficacies of osaterone and delmadinone in the treatment of benign prostatic hyperplasia in dogs. Vet Rec. 2008 Aug 9;163(6):179-83. doi: 10.1136/vr.163.6.179. PMID: 18689779.
3: Marshall FJ. Use of delmadinone acetate. Vet Rec. 1979 Jun 2;104(22):511-2. doi: 10.1136/vr.104.22.511-a. PMID: 90422.
4: Kempker K, Güssow A, Neiger R. Transienter, sekundärer Hypoadrenokortizismus nach Behandlung mit Delmadinonacetat (Tardastrex®) bei einem zwei Jahre alten Rüden [Transient, secondary hypoadrenocorticism after treatment with delmadinone acetate (Tardastrex®) in a two year old male dog]. Schweiz Arch Tierheilkd. 2016 Mar;158(3):193-7. German. doi: 10.17236/sat00056. PMID: 27518315.
5: Lange K, Cordes EK, Hoppen HO, Günzel-Apel AR. Determination of concentrations of sex steroids in blood plasma and semen of male dogs treated with delmadinone acetate or finasteride. J Reprod Fertil Suppl. 2001;57:83-91. PMID: 11787194.
6: Fry PD. Use of delmadinone acetate in pseudopregnancy in the bitch. Vet Rec. 1980 Mar 29;106(13):297. doi: 10.1136/vr.106.13.297-a. PMID: 6156535.
7: Kent JS. Implant pellets I: effects of compression pressure on in vivo dissolution of delmadinone acetate pellets. J Pharm Sci. 1976 Jan;65(1):89-92. doi: 10.1002/jps.2600650118. PMID: 56437.
8: Tao Y, Paula R, Stolker AA, Chen D, Yuan Z. Simultaneous determination of seven gestagens in kidney fats by Ultra Performance Convergence Chromatography tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 15;988:143-8. doi: 10.1016/j.jchromb.2015.02.034. Epub 2015 Mar 2. PMID: 25777477.
9: Romagnoli S. Progestins to control feline reproduction: Historical abuse of high doses and potentially safe use of low doses. J Feline Med Surg. 2015 Sep;17(9):743-52. doi: 10.1177/1098612X15594987. PMID: 26323797.
10: Ficus HJ, Jöchle W. Erwünschte und unerwünschte Gestagenwirkungen bei der Hündin. Berücksichtigung bei der Entwicklung eines neuen Gestagens, Delmadinonazetat [Desirable and undesirable gestagen effects in a bitch, with reference to the development of a new gestagen, delmadinone acetate]. Tierarztl Prax. 1975;3(2):231-41. German. PMID: 53910.
11: Barbon AR, Ordóñez IA, Haworth P, Glendewar G, Routh A, Pocknell A. DIAGNOSIS AND MANAGEMENT OF BENIGN PROSTATIC HYPERPLASIA IN A PIED TAMARIN (SAGUINUS BICOLOR). J Zoo Wildl Med. 2016 Jun;47(2):609-13. doi: 10.1638/2015-0215.1. PMID: 27468035.
12: Malone E, Dowling G, Elliott C, Kennedy G, Regan L. Confirmatory method for the determination of various acetylgestagens in animal kidney fat using liquid chromatography-tandem mass spectrometry. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2009 May;26(5):672-82. doi: 10.1080/02652030802642110. PMID: 19680939.
13: Read RA, Bryden S. Urethral bleeding as a presenting sign of benign prostatic hyperplasia in the dog: a retrospective study (1979-1993). J Am Anim Hosp Assoc. 1995 May-Jun;31(3):261-7. doi: 10.5326/15473317-31-3-261. PMID: 7543358.
14: Meisl D, Hubler M, Arnold S. Der Progesteronantagonist Aglépristone (Alizine) zur Behandlung der fibroepithelialen Hyperlasie der Mamma bei der Katze [Treatment of fibroepithelial hyperplasia (FEH) of the mammary gland in the cat with the progesterone antagonist Aglépristone (Alizine)]. Schweiz Arch Tierheilkd. 2003 Mar;145(3):130-6. German. doi: 10.1024/0036-7281.145.3.130. PMID: 12677773.
15: Taha MB, Noakes DE, Allen WE. The effect of some exogenous hormones on seminal characteristics, libido and peripheral plasma testosterone concentrations in the male beagle. J Small Anim Pract. 1981 Sep;22(9):587-95. doi: 10.1111/j.1748-5827.1981.tb01415.x. PMID: 6172663.
16: Janssens LA. De behandeling van schijndracht bij de teef met bromocriptine (Parlodel) [Bromocriptine (Parlodel) in the treatment of pseudo-pregnancy in bitches (author's transl)]. Tijdschr Diergeneeskd. 1981 Aug 1;106(15):767-70. Dutch. PMID: 6169173.
