Absorption, Distribution and Excretion
Medroxyprogesterone is rapidly absorbed from the gastrointestinal tract after administration, with a bioavailability of 100%. Peak serum concentrations of medroxyprogesterone are 10–15 ng/ml. The elimination time of medroxyprogesterone is 36 hours. Metabolic/Metabolic Products The non-protein-bound portion of medroxyprogesterone is available for metabolism. The primary metabolic pathway for medroxyprogesterone is hydroxylation. Biological Half-Life The reported half-life of medroxyprogesterone is 4 hours.

Protein Binding
Like all progestins, medroxyprogesterone acetate (medroxyprogesterone acetate) is highly bound to plasma proteins. It primarily binds to albumin, but also to other plasma proteins such as sex hormone-binding globulin (SGH) or corticosteroid-binding globulin (CBD). The pharmacokinetics of medroxyprogesterone acetate depend on its degree of plasma protein binding; therefore, this characteristic is a major regulator of its tissue bioavailability.

Breast cancer and steroid metabolizing enzymes: the role of progestogens;

Medrogestone (INN) is a corticosteroid hormone. Medrogestone (INN), also known as 6,17α-dimethyl-6-dehydroprogesterone, is a progestin derived from 17-methylprogesterone. It was originally designed as an alternative to oral contraceptives. Developed by Ayerst Laboratories, it was approved in Canada in 1969, but its approval has since been withdrawn due to post-marketing issues. It has never been approved by the U.S. Food and Drug Administration (FDA). 6,17-Dimethylpregn-4,6-diene-3,20-dione is a synthetic progestin with similar effects to progesterone. It is used to treat menstrual disorders and has also been used to treat benign prostatic hyperplasia and endometrial cancer.

---

Drug Indications
Medrogestone is indicated for adjuvant therapy in postmenopausal women to induce endometrial shedding, treat secondary amenorrhea, induce menstruation, and treat dysfunctional uterine bleeding in adult and adolescent women.
Mechanism of Action Medroxyprogesterone acetate is a progestin, and therefore its mechanism of action is similar to that of progestins. These molecules are steroid hormones that bind to and activate progesterone receptors. Its action may involve inhibiting the secretion of gonadotropins from the anterior pituitary gland, thereby inhibiting testosterone secretion. Medroxyprogesterone acetate has a structure similar to testosterone, allowing it to bind to androgen receptor proteins in prostate cells. Administration of medroxyprogesterone acetate reduces the response of tumor cells to endogenous hormones due to a decrease in hormone steroid receptors; this effect translates into cytotoxicity or antiproliferative activity. Pharmacodynamics Medroxyprogesterone acetate was developed as a more effective and orally active alternative to progesterone. In preclinical trials, its progestin activity was shown to be four times that of progesterone, with a duration of action similar to that of 17-hydroxyprogesterone. Medroxyprogesterone acetate also maintained pregnancy and inhibited ovulation in ovariectomized rats. Medroxyprogesterone acetate, used alone or in combination with Premarin, can prevent pregnancy, and ovarian weight gain is suppressed in almost 100% of subjects. Medroxyprogesterone acetate does not produce any androgenic effects, but has significant anti-androgenic effects. It does not exhibit estrogenic effects, nor does it cause changes in organ weight or histological appearance of the adrenal or thymus glands, nor does it exhibit any anti-inflammatory effects.

C23H32O2

340.5

340.24

977-79-7

9949848

Typically exists as solid at room temperature

1.08g/cm3

467.2ºC at 760mmHg

144-146ºC

173.7ºC

1.549

5.279

0

2

1

25

714

6

O=C1C=C2C(C)=C[C@H]3[C@@H]4CC[C@@](C(C)=O)(C)[C@@]4(C)CC[C@@H]3[C@@]2(C)CC1

HCFSGRMEEXUOSS-JXEXPEPMSA-N

InChI=1S/C23H32O2/c1-14-12-17-18(21(3)9-6-16(25)13-20(14)21)7-11-23(5)19(17)8-10-22(23,4)15(2)24/h12-13,17-19H,6-11H2,1-5H3/t17-,18+,19+,21-,22-,23+/m1/s1

(8R,9S,10R,13S,14S,17S)-17-acetyl-6,10,13,17-tetramethyl-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one

AY-62022 Medrogesterone Medrogestone

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

---

Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

View More

Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

---

Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

View More

Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

---

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

---

 (Please use freshly prepared in vivo formulations for optimal results.)