17A-Hydroxyprogesterone   中文名称: 羟孕酮

Absorption, Distribution and Excretion
...DURATION OF ACTION IS LONGER /THAN PROGESTERONE/, BUT ITS ONSET OF ACTION IS SLOWER. SINGLE INJECTION OF SOLN OF HYDROXYPROGESTERONE CAPROATE IN OIL WILL EXERT PROGESTATIONAL EFFECTS FOR 1-2 WK. /CAPROATE/
ABOUT 50-60% OF ADMIN RADIOACTIVE PROGESTERONE APPEARS IN URINE & ABOUT 10% IN FECES. ... WHEN PROGESTERONE IS GIVEN FOR PROLONGED PERIOD, DURING LUTEAL PHASE OF CYCLE, OR DURING PREGNANCY, LARGER PROPORTION (25-30%) APPEARS IN URINE AS PREGUANEDIOL. /PROGESTERONE/
RATE OF TURNOVER OF ENDOGENOUS PROGESTERONE IS UNUSUALLY RAPID, T/2 IN BLOOD BEING FEW MIN, & DOUBTLESS EXOGENOUS MATERIAL IS HANDLED IN SAME WAY. SMALL AMT...IS STORED IN BODY FAT... PRESUMABLY, ABSORPTION FROM INTESTINAL TRACT IS PROMPT, BUT COMPD IS RAPIDLY TRANSFORMED DURING PASSAGE THROUGH LIVER... /PROGESTERONE/

---

Metabolism / Metabolites
17alpha-hydroxy-progesterone has known human metabolites that include 17Beta-21-dihydroxyprogesterone.
17alpha-hydroxy-progesterone is a known human metabolite of progesterone.

Interactions
...ESTROGEN ENHANCED SUPPRESSIVE EFFECT OF PROGESTIN & LED TO GENERAL USE OF MIXTURE OF TWO. /PROGESTINS/

17alpha-hydroxyprogesterone is a 17alpha-hydroxy steroid that is the 17alpha-hydroxy derivative of progesterone. It has a role as a metabolite, a progestin, a human metabolite and a mouse metabolite. It is a 17alpha-hydroxy steroid, a 17alpha-hydroxy-C21-steroid and a tertiary alpha-hydroxy ketone. It is functionally related to a progesterone.
Hydroxyprogesterone is a Progestin.
Hydroxyprogesterone has been reported in Homo sapiens and Vitex agnus-castus with data available.
Hydroxyprogesterone is a physiological progestin that is produced during glucocorticoid and steroid hormone synthesis and is increased during the third trimester of pregnancy. Hydroxyprogesterone binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.
It serves as an intermediate in the biosynthesis of hydrocortisone and gonadal steroid hormones. It is derived from progesterone via 17-hydroxylase, a P450c17 enzyme, or from 17-hydroxypregnenolone via 3β-hydroxysteroid dehydrogenase/Δ5-4 isomerase. 17-Hydroxyprogesterone is a natural progestin and in pregnancy increases in the third trimester primarily due to fetal adrenal production. This hormone is primarily produced in the adrenal glands and to some degree in the gonads, specifically the corpus luteum of the ovary. Normal levels are 3-90 ng/dl in children, and in women, 15-70 ng/dl prior to ovulation, and 35-290 ng/dl during the luteal phase. Measurements of levels of 17-hydroxyprogesterone are useful in the evaluation of patients with suspected congenital adrenal hyperplasia as the typical enzymes that are defective, namely 21-hydroxylase and 11β-hydroxylase, lead to a build-up of 17OHP. In contrast, the rare patient with 17α-hydroxylase deficiency will have very low or undetectable levels of 17OHP. 17OHP levels can also be used to measure contribution of progestational activity of the corpus luteum during pregnancy as progesterone but not 17OHP is also contributed by the placenta.
A metabolite of PROGESTERONE with a hydroxyl group at the 17-alpha position. It serves as an intermediate in the biosynthesis of HYDROCORTISONE and GONADAL STEROID HORMONES.
See also: Hydroxyprogesterone Caproate (active moiety of); 17beta-Hydroxyprogesterone (annotation moved to).

---

Mechanism of Action
ADMIN OF ESTROGEN & PROGESTIN, AS CONTAINED IN COMBINATION OR SEQUENTIAL PREPN, COULD INTERFERE WITH FERTILITY IN ANY ONE OF SEVERAL WAYS. HOWEVER, IT IS CLEAR THAT, AS CURRENTLY USED, MIXTURE INHIBITS OVULATION. ...CONTINUED ACTION OF PROGESTERONE SERVES TO INHIBIT RELEASE OF LH. /PROGESTINS/
IT ACTS AS ANTIGONADOTROPHIC AGENT ON ANTERIOR PITUITARY INHIBITING FSH RELEASE &, THUS, FOLLICULAR GROWTH, ESTROGEN PRODUCTION, & ESTRUS. IT ALSO INHIBITS LH RELEASE, THUS PREVENTING OVULATION, CORPORA LUTEA FORMATION, & FURTHER PROGESTERONE SECRETION. BY INHIBITING LH...HOLDS PROGESTERONE LEVELS IN CHECK.

---

Therapeutic Uses
THERAPEUTIC USES. ...CONTRACEPTION...FUNCTIONAL UTERINE BLEEDING... DYSMENORRHEA...PREMENSTRUAL TENSION...ENDOMETRIOSIS...THREATENED & HABITUAL ABORTION...EVALUATION OF OVARIAN FUNCTION & DIAGNOSIS OF PREGNANCY...SUPPRESSION OF POST-PARTUM LACTATION...ENDOMETRIAL CARCINOMA. /PROGESTINS/
CHEMOTHERAPEUTIC AGENTS USEFUL IN NEOPLASTIC DISEASE: HYDROXYPROGESTERONE CAPROATE (DELALUTIN) FOR ENDOMETRIUM, RENAL CELL, BREAST, PROSTATE. /CAPROATE/
...IN METASTATIC & RECURRENT ENDOMETRIAL CARCINOMA. THEY PRODUCE REMISSIONS FOR PROLONGED PERIODS IN ABOUT 25% OF PT WHEN METASTASES ARE CONFINED TO PULMONARY AREA. LARGER DOSES...WHEN DISEASE RECURS IN OSSEOUS, INTRA-ABDOMINAL, OR PELVIC SITES. ...USED PARENTERALLY IN RENAL CARCINOMA. /PROGESTAGEUS/
WHEN USED TO REGULATE IRREGULAR ESTRUS CYCLE, IT IS USUALLY COMBINED WITH ESTROGEN. /CAPROATE/
For more Therapeutic Uses (Complete) data for 17ALPHA-HYDROXYPROGESTERONE (15 total), please visit the HSDB record page.

---

Drug Warnings
VET: AVOID BREEDING TREATED ANIMALS UNTIL SECOND POST-TREATMENT ESTRUS CYCLE. SEVERE PYOMETRA-LIKE SYNDROMES HAVE OCCURRED IN TREATED ANIMALS DEPRIVED OF NORMAL ESTRUS STIMULATING EFFECTS ON UTERINE ENDOMETRIUM...
WHETHER TAKING ORAL CONTRACEPTIVES OF PROGESTIN-ESTROGEN TYPE PRODUCED HIGHER INCIDENCE OF OCULAR & OPHTHALMO-NEUROLOGIC DISEASES THAN WOULD OCCUR SPONTANEOUSLY IN UNMEDICATED WOMEN OR IN PREGNANT WOMEN WAS NOT ANSWERED CONCLUSIVELY... /PROGESTINS/
CONTRAINDICATIONS TO THEIR USE ARE THROMBOEMBOLIC DISORDERS OR PAST HISTORY OF THESE CONDITIONS, MARKEDLY IMPAIRED HEPATIC FUNCTION, KNOWN OR SUSPECTED CARCINOMA OF BREAST OR OTHER ESTROGEN-DEPENDENT NEOPLASIA, & UNDIAGNOSED GENITAL BLEEDING. /ORAL CONTRACEPTIVES/

C21H30O3

330.46

330.219

68-96-2

6238

White to off-white solid powder

1.2±0.1 g/cm3

482.9±45.0 °C at 760 mmHg

276°C

260.0±25.2 °C

0.0±2.8 mmHg at 25°C

1.560

2.89

54.37

1

3

1

24

635

6

O([H])[C@]1(C(C([H])([H])[H])=O)C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C(C([H])([H])C([H])([H])[C@]4(C([H])([H])[H])[C@@]3([H])C([H])([H])C([H])([H])[C@@]21C([H])([H])[H])=O

DBPWSSGDRRHUNT-CEGNMAFCSA-N

InChI=1S/C21H30O3/c1-13(22)21(24)11-8-18-16-5-4-14-12-15(23)6-9-19(14,2)17(16)7-10-20(18,21)3/h12,16-18,24H,4-11H2,1-3H3/t16-,17+,18+,19+,20+,21+/m1/s1

(8R,9S,10R,13S,14S,17R)-17-Acetyl-17-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one

Hydroxyprogesterone 17A-Hydroxyprogesterone

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 本产品在运输和储存过程中需避光。

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

DMSO : ~50 mg/mL (~151.30 mM)
H2O : < 0.1 mg/mL

配方 1 中的溶解度: ≥ 2.5 mg/mL (7.57 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

---

配方 2 中的溶解度: ≥ 2.5 mg/mL (7.57 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液添加到 900 μL 玉米油中并混合均匀。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。