79561-22-1
6-D-Ala-10-D-gly-LHRH-ethylamide
CAS: 79561-22-1
Molecular Formula: C56H78N16O12
79561-22-1 - Names and Identifiers
79561-22-1 - Physico-chemical Properties
| Molecular Formula | C56H78N16O12 |
| Molar Mass | 1167.32 |
| Solubility | DMSO: ≥ 58 mg/mL |
| Appearance | powder |
| Storage Condition | −20°C |
| Physical and Chemical Properties | This product is White freeze-dried loose mass or powder. Figure 1 shows alarelin |
| Use | Treatment of endometriosis |
79561-22-1 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 60 - May impair fertility |
| Safety Description | S53 - Avoid exposure - obtain special instructions before use. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| WGK Germany | 3 |
79561-22-1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.777 ml | 3.884 ml | 7.767 ml |
| 5 mM | 0.155 ml | 0.777 ml | 1.553 ml |
| 10 mM | 0.078 ml | 0.388 ml | 0.777 ml |
| 5 mM | 0.016 ml | 0.078 ml | 0.155 ml |
Last Update：2024-01-02 23:10:35
79561-22-1 - Reference Information
| Overview | gonadophin release hormoneanalogue(GnRH-A), it is a synthetic nonapeptide analog of gonadotropin releasing hormone (GnRH), and its efficacy is 15 times that of the parent. It can stimulate the pituitary to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH) at the initial stage of administration, causing a transient increase in ovarian-derived steroid hormones; Repeated administration can inhibit the pituitary to release LH and FSH, the level of estradiol in the blood is decreased to achieve the effect of drug ovariectomy, and the expression of ras, neu and myc in endometrial carcinoma is regulated. Clinically, it is mainly used to promote ovulation, treat infertility caused by abnormal ovarian function, endometriosis and uterine fibroids, and improve the pregnancy rate. |
| pharmacological action | This product is a synthetic nonapeptide analog of gonadotropin releasing hormone (GnRH), it can stimulate the pituitary to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH) at the initial stage of administration, causing a transient increase in ovarian-derived steroid hormones; Repeated administration can inhibit the pituitary to release LH and FSH, the level of estradiol in the blood is decreased to achieve the effect of drug ovariectomy. This inhibitory effect can be used to treat hormone dependent diseases such as endometriosis. |
| mechanism of action | by detecting the expression of Smad2/3 and Smad7, which are key mediators in the TGF-β/smads signal transduction pathway, it is suggested that TGF-β1/smads signal transduction pathway may be an important pathway in the pathogenesis of endometrial carcinoma. Alarelin may inhibit the occurrence and development of endometrial carcinoma by up-regulating Smad2/3 and down-regulating Smad7 protein expression. |
| pharmacokinetics | This product is absorbed rapidly after intramuscular injection in rats, and the blood concentration reaches its peak value in about 20 minutes, the decrease of blood drug concentration was in accordance with the two compartment model. When intramuscular injection was administered, t1/2α was about 0.2 h, and t1/2β was about 1.8 h. When administered intravenously, t1/2α is 0.08 h and t1/2β is about 1.2 h. Its bioavailability can reach about 80%. And plasma protein binding rate of 27% ~ 35%, the highest tissue distribution in the kidney, followed by the liver, gonad and pituitary, drugs can be secreted from the bile, within 24 h in vivo completely metabolic decomposition, and all from the urine and feces, of which 80% from the urine. |
| Application | clinically, it is mainly used for ovulation induction, treatment of infertility caused by abnormal ovarian function, endometriosis and uterine fibroids and improve pregnancy rate. Figure 2: alarelin |
| usage and dosage | subcutaneous or intramuscular injection, start treatment for menstrual cramps d1 ~ d2, 150 μg/time, qd, or as directed by a physician. The formulation was dissolved in 2 ml sterile physiological saline immediately prior to use. Endometriosis 3~6 months for a course of treatment. |
| adverse reactions | symptoms due to low estrogen status, such as hot flashes, night sweats, vaginal dryness or mood changes, individual patients with skin rash, after stopping can disappear. |
| note | 1. Pregnant women, lactating women and unexplained vaginal bleeding are contraindicated. 2. Allergy to GnRH or its analogs is contraindicated. 3. In addition to the sudden withdrawal in patients with infertility caused by endometriosis, the rest of the patients need to be gradually withdrawn. 4. If there is bleeding during medication, the dose can be adjusted to 200 μg/d on Counseling. 5. The course of treatment is generally not more than 6 months to prevent bone loss. |
| size packaging | powder for injection: 25 μg/vial, 10/pack; 150 μg/vial, 10 cigarettes/box. Figure 3: alarelin acetate |
| Main reference material | [1] gu Hanying. Alarelin [J]. Chinese Journal of new drugs, 1999,(08):546. [2] Li Runlian, Zhang ternary. Inhibitory effect of alarelin combined with 5-FU on human endometrial carcinoma xenografts in nude mice [J]. China Practical Medicine, 2010,5(20):3-4. [3] Li Runlian, Zhang ternary. Inhibitory effect of alarelin on human endometrial carcinoma xenografts in nude mice [J]. Medical information, 2010,5(02):309-311. [4] Wei suacheng, Dong Jiangling, Xie Kun, Wei Min, Zhang Jie, Wang Jiangchuan. Effects of active immunization with alarelin on the expression of pituitary GnRHR, FSHR and LHR and the distribution of ovarian GnRHR in sheep [J]. Jiangsu Journal of Agricultural Sciences, 2012,28(01):114-120. [5] Zhang Xinglin. Effect and mechanism of alarelin on the growth of human endometrial carcinoma cells in nude mice [J]. Shanxi Medical University, 2013. |
Last Update：2024-04-09 21:11:58
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Product Name: Alarelin (Acetate) Visit Supplier Webpage Request for quotationCAS: 79561-22-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: 6-D-Ala-10-D-gly-LHRH-ethylamide Request for quotation
CAS: 79561-22-1
Tel: +86-21-56795779
Email: charles7788@worldyachem.com
Mobile: +86-13651600618
QQ: 2850607228
Wechat: 13651600618
WhatsApp: +8613651600618
CAS: 79561-22-1
Tel: +86-21-56795779
Email: charles7788@worldyachem.com
Mobile: +86-13651600618
QQ: 2850607228
Wechat: 13651600618
WhatsApp: +8613651600618
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