| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Glucuronide and sulfate conjugates of pregnanediol and pregnanediolone are excreted in urine and bile. Progesterone metabolites excreted in bile may undergo enterohepatic circulation or be excreted in feces. Progesterone metabolites are primarily excreted by the kidneys. |
|---|---|
| References | |
| Additional Infomation |
Allylestrenol is a steroid derived from estradiol. It is a synthetic steroid with progesterone activity and is widely sold in Europe, including Russia and many other European countries. It is also sold in Japan, Hong Kong, India, Bangladesh, Indonesia, and most of Southeast Asia, but notably, it is not sold in the United States and Canada. Allylestrenol is a synthetic steroid with progesterone activity.
Drug Indications Allylestrenol was originally designed to prevent miscarriage and preterm birth and has been investigated for the treatment of benign prostatic hyperplasia in men. Mechanism of Action The structure and function of Allylestrenol are similar to those of progesterone. Progesterone has the same pharmacological effects as progestins. Progesterone can bind to progesterone receptors and estrogen receptors. Target cells include the female reproductive tract, mammary glands, hypothalamus, and pituitary gland. After progestins (such as progesterone) bind to their receptors, they slow the release frequency of gonadotropin-releasing hormone (GnRH) from the hypothalamus and inhibit the pre-ovulatory surge of luteinizing hormone (LH). In women with adequate estrogen levels, progesterone transforms the proliferative endometrium into the secretory endometrium. Progesterone is crucial for the development of decidual tissue and is essential for improving endometrial receptivity, which is conducive to embryo implantation. After implantation, progesterone plays a role in maintaining pregnancy. In addition, progesterone stimulates the growth of mammary alveolar tissue and relaxes uterine smooth muscle. It has almost no estrogenic or androgenic activity. Pharmacodynamics Allylestrenol is a progestin with a structure related to progesterone and has been used to treat threatened and recurrent miscarriages, as well as to prevent preterm birth. However, it is no longer recommended except in cases of confirmed progesterone deficiency. For patients with threatened miscarriage due to progesterone deficiency, the recommended dose is 5 mg orally three times daily for 5 to 7 days. |
| Molecular Formula |
C21H32O
|
|---|---|
| Molecular Weight |
300.4782
|
| Exact Mass |
300.245
|
| CAS # |
432-60-0
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| PubChem CID |
235905
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
405.4±44.0 °C at 760 mmHg
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| Melting Point |
78 - 81ºC
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| Flash Point |
170.6±20.7 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.553
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| LogP |
6.64
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
22
|
| Complexity |
492
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
O([H])[C@@]1(C([H])([H])C([H])=C([H])[H])C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C([H])([H])C([H])([H])C([H])([H])[C@]4([H])[C@@]3([H])C([H])([H])C([H])([H])[C@@]21C([H])([H])[H]
|
| InChi Key |
ATXHVCQZZJYMCF-XUDSTZEESA-N
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| InChi Code |
InChI=1S/C21H32O/c1-3-12-21(22)14-11-19-18-9-8-15-6-4-5-7-16(15)17(18)10-13-20(19,21)2/h3,6,16-19,22H,1,4-5,7-14H2,2H3/t16-,17+,18+,19-,20-,21-/m0/s1
|
| Chemical Name |
(8R,9S,10R,13S,14S,17R)-13-methyl-17-prop-2-enyl-2,3,6,7,8,9,10,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ol
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~166.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3280 mL | 16.6400 mL | 33.2801 mL | |
| 5 mM | 0.6656 mL | 3.3280 mL | 6.6560 mL | |
| 10 mM | 0.3328 mL | 1.6640 mL | 3.3280 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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