Leuprolide Acetate 醋酸亮氨酸脯氨酸
CAS 74381-53-6 MFCD00167544
化学结构图
SMILES: CC(=O)O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1
化学属性
| Mol. Formula | C59H84N16O12.C2H4O2 |
|---|---|
| Mol. Weight | 1269.473 |
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | Leuprolide Acetate |
|---|---|
| Synonym | LEUP; A43818; Abbott 43818; TAP144; Leuprorelin; Leuprorelin Acetate; Brand names: ELIGARD; Lupron; Lupron Depot. Leuprolide acetate Leuprolide acetate salt Lupron TAP-144 des-Gly10-[D-Leu6]-LH-RH ethylamide |
| MDL Number | MFCD00167544 |
| PubChem Substance ID | 24896252 |
| CAS Number | 74381-53-6 |
| Chemical Name Translation | 醋酸亮氨酸脯氨酸 |
| Beilstein Registry Number | 5570787 |
| Formula | C61H88N16O14 |
| IUPAC Name | Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate |
| InChIKey | RGLRXNKKBLIBQS-XNHQSDQCSA-N |
| InChI | InChI=1S/C59H84N16O12.C2H4O2/c1-6-63-57(86)48-14-10-22-75(48)58(87)41(13-9-21-64-59(60)61)68-51(80)42(23-32(2)3)69-52(81)43(24-33(4)5)70-53(82)44(25-34-15-17-37(77)18-16-34)71-56(85)47(30-76)74-54(83)45(26-35-28-65-39-12-8-7-11-38(35)39)72-55(84)46(27-36-29-62-31-66-36)73-50(79)40-19-20-49(78)67-40;1-2(3)4/h7-8,11-12,15-18,28-29,31-33,40-48,65,76-77H,6,9-10,13-14,19-27,30H2,1-5H3,(H,62,66)(H,63,86)(H,67,78)(H,68,80)(H,69,81)(H,70,82)(H,71,85)(H,72,84)(H,73,79)(H,74,83)(H4,60,61,64);1H3,(H,3,4)/t40-,41-,42-,43+,44-,45-,46-,47-,48-;/m0./s1 |
| Canonical SMILES | CC(O)=O.O=C([C@H](CC1)NC1=O)N[C@@H](CC2=CN=CN2)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CO)C(N[C@@H](CC5=CC=C(O)C=C5)C(N[C@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCC/N=C(N)\N)C(N6[C@H](C(NCC)=O)CCC6)=O)=O)=O)=O)=O)=O)=O |
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分类
- {SNA} Androgen Modulators, Antitumor Agents, Bioactive Small Molecules, Cancer Research, Cell Biology, Cell Signaling and Neuroscience, L, LH-RH, Neuropeptides, Peptides and Proteins, Peptides for Cell Biology, Releasin
- Androgen Modulators, Antitumor Agents, Bioactive Small Molecules, Cancer Research, Cell Biology, Cell Signaling and Neuroscience, L, LH-RH, Neuropeptides, Peptides and Proteins, Peptides for Cell Biology, Releasing Factors, Therapy Adjuncts, Tumor Growth Regulation
产品应用
- Leuprolide acetate is the acetate salt of a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors. Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
相关文献及参考
- Zheng, Y, et al., Permeability and absorption of leuprolide from various intestinal regions in rabbits and rats. Int. J. Pharmacol. 185 , 83, (1999) 摘要
- Goto, T., et al., Gonadotropin-releasing hormone agonist has the ability to induce increased matrix metalloproteinase (MMP)-2 and membrane type 1-MMP expression in corpora lutea, and structural luteolysis in rats. J. Endocrinol. 161 , 393-402, (1999) 摘要
- Ogawa, T., et al., Leuprolide, a gonadotropin-releasing hormone agonist, enhances colonization after spermatogonial transplantation into mouse testes. Cell 30 , 583-588, (1998) 摘要
- Ravivarapu, H.B., et al., Sustained suppression of pituitary-gonadal axis with an injectable, in situ forming implant of leuprolide acetate. J. Pharm. Sci. 89 , 732-741, (2000) 摘要
- Imai, A., et al., Fas and Fas ligand system may mediate antiproliferative activity of gonadotropin-releasing hormone receptor in endometrial cancer cells. Int. J. Oncol. 13 , 97-100, (1998) 摘要
- Merck 14 ,5457
安全信息
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S569,1990
{TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S569,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S569,1990
TY
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S569,1990
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE : 24 ug/kg SEX/DURATION : female 4 week(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Newborn - sex ratio REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S589,19
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE : 24 ug/kg SEX/DURATION : female 1 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S589,1990
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE : 72 ug/kg SEX/DURATION : male 8 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - other effects on male Endocrine - changes in luteinizing hormone REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 3),S589,1990
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